BCL-XL INHIBITOR ANTIBODY-DRUG CONJUGATES AND METHODS OF USE THEREOF

JP2023553811A5Pending Publication Date: 2024-12-13NOVARTIS AG +1
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Application Number
JP2023531000
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2020-11-24
Filing Date
2021-11-23
Publication Date
2024-12-13

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Abstract

Disclosed are antibody-drug conjugates that bind to human oncology targets. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure further relates to methods and compositions for use in treating cancer by administering the antibody-drug conjugates provided herein. Also disclosed are linker-drug conjugates comprising a Bcl-xL inhibitor drug moiety and methods for making the same.
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Claims

1. Antibody-drug conjugate of formula (1): A-(L-D) ｐ (1) [In the formula, Ab is an antibody or an antigen-binding fragment thereof; L is a linker that covalently attaches Ab to D; p is an integer from 1 to 16; D is a group of formula (I) covalently attached to said linker L: 【Chemistry 1】 or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any one of these, wherein: ・R １ and R ２ are each independently hydrogen; hydroxyl or C １ ~C ６ Linear or branched C optionally substituted with alkoxy groups １ ~C ６ Alkyl; C ３ ~C ６ Cycloalkyl; trifluoromethyl; heterocycloalkyl group is linear or branched C １ ~C ６ Optionally substituted with alkyl groups, linear or branched C １ ~C ６ represents a group selected from alkylene-heterocycloalkyl; Or R １ and R ２ together with the carbon atom carrying these groups, ３ ~C ６ Forming a cycloalkylene group, ・R ３ is hydrogen; ３ ~C ６ Cycloalkyl; linear or branched C １ ~C ６ Alkyl; -X １ -NR ａ R ｂ ;-X １ -N ＋ R ａ R ｂ R ｃ ;-X １ -O-R ｃ ;-X １ -COOR ｃ ;-X １ -PO(OH) ２ ;-X １ -SO ２ (OH); -X １ -N ３ , and: 【Chemistry 2】 represents a group selected from ・R ａ and R ｂ are each independently hydrogen; heterocycloalkyl; phenyl is a straight or branched C １ ~C ６ -SO optionally substituted with alkyl ２ -phenyl; linear or branched C optionally substituted by 1 or 2 hydroxyl groups １ ~C ６ Alkyl; C １ ~C ６ Alkylene-SO ２ OH;C １ ~C ６ Alkylene-SO ２ O － ; C １ ~C ６ Alkylene-COOH; １ ~C ６ Alkylene-PO(OH) ２ ; C １ ~C ６ Alkylene -NR ｄ R ｅ ; C １ ~C ６ Alkylene-N ＋ R ｄ R ｅ R ｆ phenyl is C １ ~C ６ C optionally substituted by an alkoxy group １ ~C ６ alkylene-phenyl; Base: 【Chemistry 3】 represents a group selected from Or R ａ and R ｂ together with the nitrogen atom bearing these groups form ring B １ forming Or R ａ , R ｂ , and R ｃ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・R ｃ , R ｄ , R ｅ , R ｆ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, Or R ｄ and R ｅ together with the nitrogen atom bearing these groups form ring B ２ It is formed, Or R ｄ , R ｅ , and R ｆ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・Het １ teeth, 【Chemistry 4】 represents a group selected from ・Het ２ teeth, 【Chemistry 5】 represents a group selected from ・A １ is -NH-, -N(C １ ~C ３ alkyl), O, S, or Se; ・A ２ is N, CH, or C(R ５ ) and ・G is -C(O)OR Ｇ３ , -C(O)NR Ｇ１ R Ｇ２ , -C(O)R Ｇ２ , -NR Ｇ１ C(O)R Ｇ２ , -NR Ｇ１ C(O)NR Ｇ１ R Ｇ２ , -OC(O)NR Ｇ１ R Ｇ２ , -NR Ｇ１ C(O)OR Ｇ３ , -C(=NOR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ C(=NCN)NR Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ N.R. Ｇ１ R Ｇ２ , -S(O) ２ R Ｇ３ , -S(O) ２ N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ R Ｇ２ , -NR Ｇ１ C (=NR Ｇ２ ) N.R. Ｇ１ R Ｇ２ , -C(=S)NR Ｇ１ R Ｇ２ , -C(=NR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , as well as hydroxyl groups, halogens, -NO ２ and C optionally substituted by -CN １ ~C ６ alkyl, wherein -R Ｇ１ and R Ｇ２ each occurrence independently represents hydrogen, C optionally substituted by 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, C ３ ~C ６ Cycloalkyl, phenyl, and -(CH ２ ) １～４ - phenyl; -R Ｇ３ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, C ３ ~C ６ Cycloalkyl, phenyl, and -(CH ２ ) １～４ -phenyl; or R Ｇ１ and R Ｇ２ Each of them, together with the atom to which it is bonded, is C ３ ~C ８ forming a heterocycloalkyl; or alternatively, G is 【Chemistry 6】 wherein R Ｇ４ is hydrogen, C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, and C ３ ~C ６ cycloalkyl), ・R ４ represents a hydrogen, fluorine, chlorine or bromine atom, a methyl, hydroxyl or methoxy group, ・R ５ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl; C ２ ~C ６ Alkenyl; C ２ ~C ６ represents a group selected from: alkynyl; halogen; or -CN, ・R ６ teeth, hydrogen; -C ２ ~C ６ Alkenyl; -X ２ -O-R ７ ; 【Chemistry 7】 -X ２ -NSO ２ -R ７ ; -C=C(R ９ )-Y １ -O-R ７ ; C ３ ~C ６ Cycloalkyl; C optionally substituted with a hydroxyl group ３ ~C ６ Heterocycloalkyl; C ３ ~C ６ Cycloalkylene-Y ２ -R ７ ; C ３ ~C ６ Heterocycloalkylene-Y ２ -R ７ Groups, and Linear or branched C １ ~C ６ Heteroarylene-R optionally substituted with an alkyl group ７ base represents a group selected from ・R ７ is a linear or branched C １ ~C ６ Alkyl group; ３ ~C ６ ) Cycloalkylene-R ８ or R ７ teeth: 【Chemistry 8】 wherein Cy represents a group selected from ３ ~C ８ represents cycloalkyl, ・R ８ is hydrogen; linear or branched C １ ~C ６ Alkyl, -NR' ａ R' ｂ -NR' ａ -CO-OR' ｃ -NR' ａ -CO-R' ｃ ;-N ＋ R' ａ R' ｂ R' ｃ ;-O-R' ｃ -NH-X' ２ -N ＋ R' ａ R' ｂ R' ｃ ;-O-X' ２ -NR' ａ R' ｂ , -X' ２ -NR' ａ R' ｂ , -NR' ｃ -X' ２ -N ３ , and: 【Chemistry 9】 represents a group selected from ・R ９ is a linear or branched C １ ~C ６ Alkyl, trifluoromethyl, hydroxyl, halogen, and C １ ~C ６ represents a group selected from alkoxy, ・R １０ is hydrogen, fluorine, chlorine, bromine, -CF ３ and methyl, ・R １１ is hydrogen, C １ ~C ３ Alkylene-R ８ , -O-C １ ~C ３ Alkylene-R ８ , —CO—NR ｈ R ｉ and -CH=CH-C １ ~C ４ Alkylene -NR ｈ R ｉ , -CH=CH-CHO,C ３ ~C ８ Cycloalkylene -CH ２ -R ８ , and C ３ ~C ８ Heterocycloalkylene -CH ２ -R ８ represents a group selected from ・R １２ and R １３ each independently represents a hydrogen atom or a methyl group, ・R １４ and R １５ are each independently a hydrogen atom or a methyl group, or R １４ and R １５ together with the carbon atom carrying these groups form a cyclohexyl; ・R ｈ and R ｉ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, X １ and X ２ are each independently selected from trifluoromethyl, hydroxyl, halogen, and C １ ~C ６ Linear or branched C optionally substituted with one or two groups selected from alkoxy １ ~C ６ represents an alkylene group, ・X' ２ is a linear or branched C １ ~C ６ represents alkylene, ・R' ａ and R' ｂ are each independently hydrogen; heterocycloalkyl; phenyl is a straight or branched C １ ~C ６ -SO optionally substituted with alkyl ２ -phenyl; 1 or 2 hydroxyl or C １ ~C ６ Linear or branched C optionally substituted with alkoxy groups １ ~C ６ Alkyl; C １ ~C ６ Alkylene-SO ２ OH;C １ ~C ６ Alkylene-SO ２ O － ; C １ ~C ６ Alkylene-COOH; １ ~C ６ Alkylene-PO(OH) ２ ; C １ ~C ６ Alkylene-NR' ｄ R' ｅ ; C １ ~C ６ Alkylene-N ＋ R' ｄ R' ｅ R' ｆ ; C １ ~C ６ Alkylene -O-C １ ~C ６ Alkylene-OH; Phenyl is hydroxyl or C １ ~C ６ C optionally substituted by an alkoxy group １ ~C ６ alkylene-phenyl; and 【Chemistry 10】 represents a group selected from or R' ａ and R' ｂ together with the nitrogen atom bearing these groups form ring B ３ It is formed, or R' ａ , R' ｂ and R' ｃ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・R' ｃ , R' ｄ , R' ｅ , R' ｆ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, or R' ｄ and R' ｅ together with the nitrogen atom bearing these groups form ring B ４ It is formed, or R' ｄ , R' ｅ and R' ｆ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・Y １ is a linear or branched C １ ~C ４ represents alkylene, ・Y ２ represents bonding, -O-, -O-CH ２ -, -O-CO-, -O-SO ２ -, -CH ２ -, -CH ２ -O, -CH ２ -CO-, -CH ２ -SO ２ -, -C ２ H ５ -, -CO-, -CO-O-, -CO-CH ２ -, -CO-NH-CH ２ -, -SO ２ -, -SO ２ -CH ２ -, -NH-CO-, or -NH-SO ２ - and represents m is 0, 1, or 2, p is 1, 2, 3, or 4; ・B １ , B ２ , B ３ , and B ４ are, independently of each other, C ３ ~C ８ represents a heterocycloalkyl group, which may be (i) a monocyclic or bicyclic group, including fused, bridged, or spiro ring systems; (ii) may contain, in addition to the nitrogen atom, one or two heteroatoms independently selected from oxygen, sulfur, and nitrogen; or (iii) may contain fluorine, bromine, chlorine, linear or branched C １ ~C ６ Alkyl, hydroxyl, -NH ２ , oxo, or piperidinyl; In the formula, R ３ and R ８ one of the groups, when present, is covalently attached to said linker, where the valency of the atom is not exceeded by one or more of the substituents attached thereto; or D is a group of formula (II) covalently attached to said linker L: 【Chemistry 11】 or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any one of the foregoing, wherein n is 0, 1, or 2, ----- represents a single or double bond, ・A ４ and A ５ represent, independently of one another, a carbon or nitrogen atom, Z １ represents a bond, -N(R)-, or -O-, where R is hydrogen or a linear or branched C １ ~C ６ represents alkyl), ・R １ is hydrogen; hydroxyl or C １ ~C ６ Linear or branched C optionally substituted with alkoxy groups １ ~C ６ Alkyl; C ３ ~C ６ Cycloalkyl; trifluoromethyl; heterocycloalkyl group is linear or branched C １ ~C ６ Optionally substituted with alkyl groups, linear or branched C １ ~C ６ represents a group selected from alkylene-heterocycloalkyl; ・R ２ represents hydrogen or methyl; ・R ３ is hydrogen; linear or branched C １ ~C ４ Alkyl; -X １ -NR ａ R ｂ ;-X １ -N ＋ R ａ R ｂ R ｃ ;-X １ -O-R ｃ ;-X １ -COOR ｃ ;-X １ -PO(OH) ２ ;-X １ -SO ２ (OH); -X １ -N ３ , and: 【Chemistry 12】 represents a group selected from ・R ａ and R ｂ are each independently hydrogen; heterocycloalkyl; phenyl is a straight or branched C １ ~C ６ -SO optionally substituted with alkyl ２ -phenyl; linear or branched C optionally substituted by 1 or 2 hydroxyl groups １ ~C ６ Alkyl; C １ ~C ６ Alkylene-SO ２ OH;C １ ~C ６ Alkylene-SO ２ O － ; C １ ~C ６ Alkylene-COOH; １ ~C ６ Alkylene-PO(OH) ２ ; C １ ~C ６ Alkylene -NR ｄ R ｅ ; C １ ~C ６ Alkylene-N ＋ R ｄ R ｅ R ｆ phenyl is C １ ~C ６ C optionally substituted by an alkoxy group １ ~C ６ alkylene-phenyl; and 【Chemistry 13】 represents a group selected from Or R ａ and R ｂ together with the nitrogen atom bearing these groups form ring B １ forming Or R ａ , R ｂ , and R ｃ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・R ｃ , R ｄ , R ｅ , R ｆ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, Or R ｄ and R ｅ together with the nitrogen atom bearing these groups form ring B ２ It is formed, Or R ｄ , R ｅ , and R ｆ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・Het １ teeth, 【Chemistry 14】 represents a group selected from ・Het ２ teeth, 【Chemistry 15】 represents a group selected from ・A １ is -NH-, -N(C １ ~C ３ alkyl), O, S, or Se; ・A ２ is N, CH, or C(R ５ ) and ・G is -C(O)OR Ｇ３ , -C(O)NR Ｇ１ R Ｇ２ , -C(O)R Ｇ２ , -NR Ｇ１ C(O)R Ｇ２ , -NR Ｇ１ C(O)NR Ｇ１ R Ｇ２ , -OC(O)NR Ｇ１ R Ｇ２ , -NR Ｇ１ C(O)OR Ｇ３ , -C(=NOR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ C(=NCN)NR Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ N.R. Ｇ１ R Ｇ２ , -S(O) ２ R Ｇ３ , -S(O) ２ N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ R Ｇ２ , -NR Ｇ１ C (=NR Ｇ２ ) N.R. Ｇ１ R Ｇ２ , -C(=S)NR Ｇ１ R Ｇ２ , -C(=NR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , as well as hydroxyl groups, halogens, -NO ２ and C optionally substituted by -CN １ ~C ６ alkyl, wherein -R Ｇ１ and R Ｇ２ each occurrence independently represents hydrogen, C optionally substituted by 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, C ３ ~C ６ Cycloalkyl, phenyl, and -(CH ２ ) １～４ - phenyl; -R Ｇ３ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, C ３ ~C ６ Cycloalkyl, phenyl, and -(CH ２ ) １～４ -phenyl; or R Ｇ１ and R Ｇ２ Each of them, together with the atom to which it is bonded, is C ３ ~C ８ forming a heterocycloalkyl; or alternatively, G is 【Chemistry 16】 wherein R Ｇ４ is hydrogen, C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, and C ３ ~C ６ cycloalkyl), ・R ４ represents a hydrogen, fluorine, chlorine or bromine atom, a methyl, hydroxyl or methoxy group, ・R ５ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl; C ２ ~C ６ Alkenyl; C ２ ~C ６ represents a group selected from: alkynyl; halogen; or -CN, ・R ６ teeth, hydrogen; -C ２ ~C ６ Alkenyl; -X ２ -O-R ７ ; 【Chemistry 17】 -X ２ -NSO ２ -R ７ ; -C=C(R ９ )-Y １ -O-R ７ ; C ３ ~C ６ Cycloalkyl; C optionally substituted with a hydroxyl group ３ ~C ６ Heterocycloalkyl; C ３ ~C ６ Cycloalkylene-Y ２ -R ７ ; C ３ ~C ６ Heterocycloalkylene-Y ２ -R ７ Groups, and Linear or branched C １ ~C ６ Heteroarylene-R optionally substituted with an alkyl group ７ base represents a group selected from ・R ７ is a linear or branched C １ ~C ６ an alkyl group; or (C ３ ~C ６ ) Cycloalkylene-R ８ or R 7 represents: 【Chemistry 18】 wherein Cy represents a group selected from ３ ~C ８ represents cycloalkyl, ・R ８ is hydrogen; linear or branched C １ ~C ６ Alkyl, -NR' ａ R' ｂ -NR' ａ -CO-OR' ｃ -NR' ａ -CO-R' ｃ ;-N ＋ R' ａ R' ｂ R' ｃ ;-OR'c;-NH-X' ２ -N ＋ R' ａ R' ｂ R' ｃ ;-O-X' ２ -NR' ａ R' ｂ , -X' ２ -NR' ａ R' ｂ , -NR' ｃ -X' ２ -N ３ , and: 【Chemistry 19】 represents a group selected from ・R ９ is a linear or branched C １ ~C ６ Alkyl, trifluoromethyl, hydroxyl, halogen, and C １ ~C ６ represents a group selected from alkoxy, ・R １０ is hydrogen, fluorine, chlorine, bromine, -CF ３ and methyl, ・R １１ is hydrogen, halogen, C １ ~C ３ Alkylene-R ８ , -O-C １ ~C ３ Alkylene-R ８ , —CO—NR ｈ R ｉ , -CH=CH-C １ ~C ４ Alkylene -NR ｈ R ｉ , -CH=CH-CHO,C ３ ~C ８ Cycloalkylene -CH ２ -R ８ , and C ３ ~C ８ Heterocycloalkylene -CH ２ -R ８ represents a group selected from ・R １２ and R １３ each independently represents a hydrogen atom or a methyl group, ・R １４ and R １５ are each independently a hydrogen atom or a methyl group, or R １４ and R １５ together with the carbon atom carrying these groups form a cyclohexyl; ・R ｈ and R ｉ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, X １ is trifluoromethyl, hydroxyl, halogen, and C １ ~C ６ Linear or branched C optionally substituted with one or two groups selected from alkoxy １ ~C ４ represents an alkylene group, X ２ is trifluoromethyl, hydroxyl, halogen, and C １ ~C ６ Linear or branched C optionally substituted with one or two groups selected from alkoxy １ ~C ６ represents an alkylene group, ・X' ２ is a linear or branched C １ ~C ６ represents alkylene, ・R' ａ and R' ｂ are each independently hydrogen; heterocycloalkyl; phenyl is a straight or branched C １ ~C ６ -SO optionally substituted with alkyl ２ -phenyl; 1 or 2 hydroxyl or C １ ~C ６ Linear or branched C optionally substituted with alkoxy groups １ ~C ６ Alkyl; C １ ~C ６ Alkylene-SO ２ OH;C １ ~C ６ Alkylene-SO ２ O － ; C １ ~C ６ Alkylene-COOH; １ ~C ６ Alkylene-PO(OH) ２ ; C １ ~C ６ Alkylene-NR' ｄ R' ｅ ; C １ ~C ６ Alkylene-N ＋ R' ｄ R' ｅ R' ｆ ; C １ ~C ６ Alkylene -O-C １ ~C ６ Alkylene-OH; Phenyl is hydroxyl or C １ ~C ６ C optionally substituted by an alkoxy group １ ~C ６ alkylene-phenyl; and 【Chemistry 20】 represents a group selected from or R' ａ and R' ｂ together with the nitrogen atom bearing these groups form ring B ３ It is formed, or R' ａ , R' ｂ and R' ｃ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・R' ｃ , R' ｄ , R' ｅ , R' ｆ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, or R' ｄ and R' ｅ together with the nitrogen atom bearing these groups form ring B ４ It is formed, or R' ｄ , R' ｅ and R' ｆ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・Y １ is a linear or branched C １ ~C ４ represents alkylene, ・Y ２ represents bonding, -O-, -O-CH ２ -, -O-CO-, -O-SO ２ -, -CH ２ -, -CH ２ -O, -CH ２ -CO-, -CH ２ -SO ２ -, -C ２ H ５ -, -CO-, -CO-O-, -CO-CH ２ -, -CO-NH-CH ２ -, -SO ２ -, -SO ２ -CH ２ -, -NH-CO-, or -NH-SO ２ - and represents m is 0, 1, or 2, p is 1, 2, 3, or 4; ・B １ , B ２ , B ３ , and B ４ are, independently of each other, C ３ ~C ８ represents a heterocycloalkyl group, which (i) may be a monocyclic or bicyclic group, including fused rings, bridged rings, or spiro ring systems; (ii) may contain, in addition to the nitrogen atom, one or two heteroatoms independently selected from oxygen, sulfur, and nitrogen; or (iii) may contain fluorine, bromine, chlorine, linear or branched C １ ~C ６ Alkyl, hydroxyl, -NH ２ , oxo, or piperidinyl; In the formula, R ３ and R ８ One of the groups, when present, is covalently attached to said linker, where the valency of the atom is not exceeded by one or more of the substituents attached thereto.

2. (i) p is an integer from 1 to 6, (ii) p is an integer from 2 to 4; (iii) p is 2 or 4; or The antibody-drug conjugate of claim 1, wherein (iv) p is determined by liquid chromatography-mass spectrometry (LC-MS).

3. (i) L is Binding group; at least one bridging spacer group; and at least one cleavable group, optionally including at least one cleavable group including a pyrophosphate group and / or a self-immolative group; or (ii) the linker L is Binding group; at least one bridging spacer group; A peptide group; and At least one cleavable group The antibody-drug conjugate of claim 1 or 2, comprising:

4. -(LD) is a compound represented by the formula (A): 【Chemistry 21】 In the formula: R １ is a linking group; L １ is a bridging spacer group; E is a cleavable group; The antibody-drug conjugate according to claim 3.

5. (1) The bonding group represented by R 1 is (i) formed from at least one reactive group selected from a maleimide group, a thiol group, a cyclooctyne group, and an azide group; and optionally a) the maleimide group has the structure: 【Chemistry 22】 having b) the azide group has the structure: -N=N ＋ = N － having c) the cyclooctyne group has the structure: 【Chemistry 23】 wherein 【Chemistry 24】 is the binding to said antibody or antigen-binding fragment thereof; or d) the cyclooctyne group has the structure: 【Chemistry 25】 wherein 【Chemistry 26】 is binding to said antibody or antigen-binding fragment thereof; or (ii) 【Chemical 27】 having a formula comprising: 【Chemistry 28】 is binding to said antibody or antigen-binding fragment thereof; or (iii) 【Chemical formula 29】 Selected from: [In the formula, 【Chemistry 30】 is a bond to said antibody or antigen-binding fragment thereof, wherein 【Chemistry 31】 is the bond to the bridging spacer group. (2) The bridging spacer group represented by L 1 is (i) contains a polyoxyethylene (PEG) group; (ii) comprises a PEG group selected from PEG1, PEG2, PEG3, PEG4, PEG5, PEG6, PEG7, PEG8, PEG9, PEG10, PEG11, PEG12, PEG13, PEG14, and PEG15; (iii) containing a -CO-CH 2 -CH 2 -PEG12 group; (iv) containing a butanoyl, pentanoyl, hexanoyl, heptanoyl, or octanoyl group; (v) a hexanoyl group; (vi) a -CO-CH 2 -CH 2 -PEG12 group; or (vii) is conjugated to a cleavable group; optionally, said cleavable group is -pyrophosphate-CH 2 -CH 2 -NH 2 -; and / or (3) The cleavable group represented by E is (i) contains a pyrophosphate group; (ii) containing the group: 【Chemistry 32】 (iii) conjugated to a Bcl-xL inhibitor (D) The antibody-drug conjugate according to claim 4.

6. -(L-D) is a compound of the formula (B): 【Chemical 33】 It is expressed as During the ceremony, R １ is a linking group; L １ is a bridging spacer; Lp is a peptide group containing 1 to 6 amino acid residues, or Lp is the group 【Chemical 34】 Including; E is a cleavable group; L ２ is a bridging spacer; m is 0 or 1; D is a Bcl-xL inhibitor; The antibody-drug conjugate of claim 1.

7. (1) The linking group is (i) formed from at least one reactive group selected from a maleimide group, a thiol group, a cyclooctyne group, and an azide group; and optionally a) the maleimide group has the structure: 【Chemistry 35】 having b) the azide group has the structure: -N=N + =N - ; c) the cyclooctyne group has the structure: 【Chemical 36】 wherein 【Chemical 37】 is binding to said antibody or antigen-binding fragment thereof; or (ii) the linking group is 【Chemical Formula 38】 having a formula comprising: 【Chemical Formula 39】 is binding to said antibody or antigen-binding fragment thereof; (2) At least one type of bridging spacer is (i) comprising a PEG group, optionally wherein the PEG group is selected from PEG1, PEG2, PEG3, PEG4, PEG5, PEG6, PEG7, PEG8, PEG9, PEG10, PEG11, PEG12, PEG13, PEG14, and PEG15; or (ii) *-C(O)-CH ２ -CH ２ -PEG1-**, *-C(O)-CH ２ -PEG3-**, *-C(O)-CH ２ -CH ２ -PEG12**, *-NH-CH ２ -CH ２ -PEG1-**, polyhydroxyalkyl group, *-C(O)-N(CH ３ )-CH ２ -CH ２ -N(CH ３ )-C(O)-**, and *-C(O)-CH ２ -CH ２ -PEG12-NH-C(O)CH ２ -CH ２ -**, wherein ** represents the point of direct or indirect attachment of said at least one cross-linking spacer to said linking group, and * represents the point of direct or indirect attachment of said at least one cross-linking spacer to said peptide group; (3) L 1 is selected from *-C(O)-CH 2 -CH 2 -PEG1-**, *-C(O)-CH 2 -PEG3-**, *-C(O)-CH 2 -CH 2 -PEG12**, *-NH-CH 2 -CH 2 -PEG1-**, and a polyhydroxyalkyl group, where ** indicates the point of direct or indirect attachment of L 1 to R 1 and * indicates the point of direct or indirect attachment of L 1 to Lp, and / or (4) m is 1 and L 2 is —C(O)—N(CH 3 )—CH 2 —CH 2 —N(CH 3 )—C(O)—. The antibody-drug conjugate according to claim 6.

8. (i) the peptide group comprises 1-6, 1-4, 1-3, or 1-2 amino acid residues, optionally selected from L-glycine (Gly), L-valine (Val), L-citrulline (Cit), L-cysteic acid (sulfo-Ala), L-lysine (Lys), L-isoleucine (Ile), L-phenylalanine (Phe), L-methionine (Met), L-asparagine (Asn), L-proline (Pro), L-alanine (Ala), L-leucine (Leu), L-tryptophan (Trp), and L-tyrosine (Tyr); (ii) the peptide group comprises Val-Cit, Val-Ala, Val-Lys, and / or Sulfo-Ala-Val-Ala; (iii) the peptide group is 【Chemistry 40】 Selected from: The antibody-drug conjugate according to claim 6 or 7.

9. 9. The antibody-drug conjugate of any one of claims 6 to 8, wherein (i) the cleavable group comprises a pyrophosphate and / or a self-immolative group; (ii) the cleavable group comprises a self-immolative group; or (iii) the cleavable group comprises a para-aminobenzyl-carbamate, para-aminobenzyl-ammonium, para-amino-(sulfo)benzyl-ammonium, para-amino-(sulfo)benzyl-carbamate, para-amino-(alkoxy-PEG-alkyl)benzyl-carbamate, para-amino-(polyhydroxycarboxytetrahydropyranyl)alkyl-benzyl-carbamate, or para-amino-(polyhydroxycarboxytetrahydropyranyl)alkyl-benzyl-ammonium.

10. m is 0 or 1, or m is 1 and the bridging spacer is 【Chemistry 41】 The antibody-drug conjugate of any one of claims 6 to 9, comprising:

11. (1)-(L-D) is 【Chemistry 42-1】 【Chemistry 42-2】 【Chemistry 42-3】 【Chemistry 42-4】 【Chemistry 42-5】 or (2)-(L-D) is 【Chemistry 43-1】 【Chemistry 43-2】 【Chemistry 43-3】 【Chemistry 43-4】 【Chemistry 43-5】 【Chemistry 43-6】 【Chemistry 43-7】 【Chemistry 43-8】 comprising a formula selected from During the ceremony, 【Chemistry 44】 The antibody-drug conjugate of any one of claims 6 to 10, wherein:

12. (1)-(L-D) is a compound represented by the formula (C): 【Chemistry 45】 In the formula: R １ is a linking group; L １ is a bridging spacer; Lp is a peptide group containing 1 to 6 amino acids; D is a Bcl-xL inhibitor; G １ -L ２ - A is a self-immolative spacer; L ２ is a bond, methylene, neopentylene, or C ２ ~C ３ alkenylene; A is a bond, -OC(=O)-*, 【Chemistry 46】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; L ３ is a spacer moiety; R ２ is a hydrophilic moiety, or (2)-(L-D) is a compound of the formula (D): 【Chemistry 47】 The During the ceremony, R １ is a linking group; L １ is a bridging spacer; Lp is a peptide group containing 1 to 6 amino acids; A is a bond, -OC(=O)-*, 【Chemistry 48】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; L ３ is a spacer moiety; R ２ is a hydrophilic moiety, The antibody-drug conjugate according to claim 1 or 2.

13. (A) (1) L １ teeth, 【Chemistry 49】 or *-CH(OH)CH(OH)CH(OH)CH(OH)CH(OH)-**, wherein each n is an integer from 1 to 12; １ * indicates the point of direct or indirect attachment to Lp; １ The ** in the is R １ indicating the point of direct or indirect attachment to; (2) L １ teeth, 【Chemistry 50】 wherein n is an integer from 1 to 12, or n is 1 or n is 12, and wherein L １ * indicates the point of direct or indirect attachment to Lp; １ The ** in the is R １ indicating the point of direct or indirect attachment to; (3) L １ teeth, 【Chemistry 51】 where n is an integer from 1 to 12, and L １ * indicates the point of direct or indirect attachment to Lp; １ The ** in the is R １ indicating the point of direct or indirect attachment to; (4) L １ teeth, 【Chemistry 52】 wherein L １ * indicates the point of direct or indirect attachment to Lp; １ The ** in the is R １ indicating the point of direct or indirect attachment to; (5) L １ teeth, *-C(=O)(CH ２ ) ｍ O(CH ２ ) ｍ -**;*-C(=O)((CH ２ ) ｍ O) ｔ (CH ２ ) ｎ -**;*-C(=O)(CH ２ ) ｍ -**;*-C(=O)NH((CH ２ ) ｍ O) ｔ (CH ２ ) ｎ -**;*-C(=O)O(CH ２ ) ｍ SSC(R ３ ) ２ (CH ２ ) ｍ C(=O)NR ３ (CH ２ ) ｍ NR ３ C(=O)(CH ２ ) ｍ -**;*-C(=O)O(CH ２ ) ｍ C(=O)NH(CH ２ ) ｍ -**;*-C(=O)(CH ２ ) ｍ NH(CH ２ ) ｍ -**;*-C(=O)(CH ２ ) ｍ NH(CH ２ ) ｎ C(=O)-**;*-C(=O)(CH ２ ) ｍ X １ (CH ２ ) ｍ -**;*-C(=O)((CH ２ ) ｍ O) ｔ (CH ２ ) ｎ X １ (CH ２ ) ｎ -**;*-C(=O)(CH ２ ) ｍ NHC(=O)(CH ２ ) ｎ -**;*-C(=O)((CH ２ ) ｍ O) ｔ (CH ２ ) ｎ NHC(=O)(CH ２ ) ｎ -**;*-C(=O)(CH ２ ) ｍ NHC(=O)(CH ２ ) ｎ X １ (CH ２ ) ｎ -**;*-C(=O)((CH ２ ) ｍ O) ｔ (CH ２ ) ｎ NHC(=O)(CH ２ ) ｎ X １ (CH ２ ) ｎ -**;*-C(=O)((CH ２ ) ｍ O) ｔ (CH ２ ) ｎ C(=O)NH(CH ２ ) ｍ -**;*-C(=O)(CH ２ ) ｍ C(R ３ ) ２ -**, or -C(=O)(CH ２ ) ｍ C(=O)NH(CH ２ ) ｍ -**, where L １ * indicates the point of direct or indirect attachment to Lp; １ The ** in the is R １ indicating the point of direct or indirect attachment to; X １ teeth, 【Chemistry 53】 and each m is independently selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; each n is independently selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; each t is independently selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, and 30; Each R ３ is H and C １ ~C ６ independently selected from alkyl, (B)(1) R 2 is a polyethylene glycol, a polyalkylene glycol, a polyol, a polysarcosine, a saccharide, an oligosaccharide, a polypeptide, 1 to 3 【Chemical 54】 or a hydrophilic moiety comprising a C 2 -C 6 alkyl substituted with 1 to 2 substituents independently selected from -OC(=O)NHS(O) 2 NHCH 2 CH 2 OCH 3 , -NHC(=O)C 1-4 alkylene-P(O)(OCH 2 CH 3 ) 2 , and a -COOH group; (2) R 2 is 【Chemistry 55】 [wherein n is an integer from 1 to 6] 【Chemistry 56】 is; (3) The hydrophilic portion represented by R 2 is (i) the part: 【Chemistry 57】 where n is an integer from 3 to 25; and R is H, -CH3, or -CH2CH2C(=O)OH; or (ii) Formula: 【Chemistry 58】 a polyethylene glycol of the formula: wherein R is H, -CH 3 , -CH 2 CH 2 NHC(=O)OR a , -CH 2 CH 2 NHC(=O)R a , or -CH 2 CH 2 C(=O)OR a ; R' is OH, -OCH 3 , -CH 2 CH 2 NHC(=O)OR a , -CH 2 CH 2 NHC(=O)R a , or -OCH 2 CH 2 C(=O)OR a ; wherein R a is H, or C 1-4 alkyl optionally substituted with either OH or C 1-4 alkoxyl; and each of m and n is independently an integer from 2 to 25. Contains; or (4) The hydrophilic portion represented by R 2 is 【Chemical Formula 59】 Contains; and / or (C)(i) L 3 is the structure 【Chemistry 60】 a spacer moiety having the formula: During the ceremony, W is -CH 2 -, -CH 2 O-, -CH 2 N(R b )C(=O)O-, -NHC(=O)C(R b ) 2 NHC(=O)O-, -NHC(=O)C(R b ) 2 NH-, -NHC(=O)C(R b ) 2 NHC(=O)-, -CH 2 N(X-R 2 )C(=O)O-, -C(=O)N(X-R 2 )-, -CH 2 N(X-R 2 )C(=O)-, -C(=O)NR b -, -C(=O)NH-, -CH 2 NR b C(=O)-, -CH 2 NR b C(=O)NH-, -CH 2 NR b C(=O)NR b -, -NHC(=O)-, -NHC(=O)O-, -NHC(=O)NH-, -OC(=O)NH-, -S(O) 2 NH-, -NHS(O) 2 -, -C(=O)-, -C(=O)O-, or -NH-, where each R b is independently selected from H, C 1 -C 6 alkyl, and C 3 -C 8 cycloalkyl; X is a bond, triazolyl, or -CH2-triazolyl-; wherein X is connected to R 2 ; or (ii) L 3 is the structure 【Chemistry 61】 a spacer moiety having the formula: During the ceremony, W is -CH 2 -, -CH 2 O-, -CH 2 N(R b )C(=O)O-, -NHC(=O)C(R b ) 2 NHC(=O)O-, -NHC(=O)C(R b ) 2 NH-, -NHC(=O)C(R b ) 2 NHC(=O)-, -CH 2 N(X-R 2 )C(=O)O-, -C(=O)N(X-R 2 )-, -CH 2 N(X-R 2 )C(=O)-, -C(=O)NR b -, -C(=O)NH-, -CH 2 NR b C(=O)-, -CH 2 NR b C(=O)NH-, -CH 2 NR b C(=O)NR b -, -NHC(=O)-, -NHC(=O)O-, -NHC(=O)NH-, -OC(=O)NH-, -S(O) 2 NH-, -NHS(O) 2 -, -C(=O)-, -C(=O)O-, or -NH-, where each R b is independently selected from H, C 1 -C 6 alkyl, and C 3 -C 8 cycloalkyl; X is -CH 2 -triazolyl-C 1-4 alkylene-OC(O)NHS(O) 2 NH-, -C 4-6 cycloalkylene-OC(O)NHS(O) 2 NH-, -(CH 2 CH 2 O) n -C(O)NHS(O) 2 NH-, -(CH 2 CH 2 O) n -C(O)NHS(O) 2 NH-(CH 2 CH 2 O) n -, -CH 2 -triazolyl-C 1-4 alkylene-OC(O)NHS(O) 2 NH-(CH 2 CH 2 O) n -, -C 4-6 cycloalkylene-OC(O)NHS(O) 2 NH-(CH 2 CH 2 O) n -, where each n is independently 1, 2, or 3, and where X is connected to R 2 ; The antibody-drug conjugate of claim 12.

14. (1) The linking group is formed by a reaction involving at least one reactive group. (2) The bonding group is a first reactive group attached to the linker; a second reactive group that is attached to the antibody or antigen-binding fragment thereof or is an amino acid residue of the antibody; and optionally, (i) at least one of the reactive groups is Thiol, Maleimide, Haloacetamides, Azide, Alkynes, Cyclooctene, Triarylphosphines, oxanobornadiene, Cyclooctyne, Diaryltetrazines, Monoaryltetrazines, Norbornene, aldehyde, Hydroxylamine, Hydrazine, NH 2 -NH-C(=O)-, Ketones, vinyl sulfone, Aziridine, Amino acid residues, 【Chemistry 62】 , -ONH 2 , -NH 2 , 【Chemistry 63】 , -N3, 【Chemistry 64】 , -SH, -SR 3 , -SSR 4 , -S(=O) 2 (CH=CH 2 ), -(CH 2 ) 2 S(=O) 2 (CH=CH 2 ), -NHS(=O) 2 (CH=CH 2 ), -NHC(=O)CH 2 Br, -NHC(=O)CH 2 I, 【Chemistry 65】 , -C(O)NHNH 2 , 【Hua 66-1】 【Hua 66-2】 Includes [In the formula, Each R 3 is independently selected from H and C 1 -C 6 alkyl; each R 4 is 2-pyridyl or 4-pyridyl; each R 5 is independently selected from H, C 1 -C 6 alkyl, F, Cl, and —OH; each R 6 is independently selected from H, C 1 -C 6 alkyl, F, Cl, -NH 2 , -OCH 3 , -OCH 2 CH 3 , -N(CH 3 ) 2 , -CN, -NO 2 , and -OH; each R 7 is independently selected from H, C 1-6 alkyl, fluoro, benzyloxy substituted with —C(═O)OH, benzyl substituted with —C(═O)OH, C 1-4 alkoxy substituted with —C(═O)OH, and C 1-4 alkyl substituted with —C(═O)OH; and / or (ii) the first reactive group and the second reactive group are Thiols and maleimides, Thiols and haloacetamides, Thiols and vinyl sulfones, Thiols and aziridines, Azides and alkynes, Azide and cyclooctyne, Azide and cyclooctene, Azides and triarylphosphines, Azides and oxanobornadienes, diaryltetrazines and cyclooctenes, Monoaryltetrazines and norbornenes, Aldehydes and hydroxylamines, Aldehydes and hydrazines, Aldehydes and NH 2 —NH—C(═O)—, Ketones and hydroxylamines, Ketones and hydrazines, Ketones and NH 2 —NH—C(═O)—, Hydroxylamine and 【Chemistry 67】 、 Amines and 【Chemistry 68】 ,or CoA or CoA analog and serine residue Contains, or (3) The bonding group is 【Chemistry 69-1】 【Chemistry 69-2】 【Chemistry 69-3】 【Chemistry 69-4】 【Chemistry 69-5】 【Chemistry 69-6】 【Chemistry 69-7】 【Chemistry 69-8】 【Chemistry 69-9】 and disulfides. [In the formula, R 32 is H, C 1-4 alkyl, phenyl, pyrimidine, or pyridine; R 35 is H, C 1-6 alkyl, phenyl, or C 1-4 alkyl substituted with 1-3 -OH groups; each R 7 is independently selected from H, C 1-6 alkyl, fluoro, benzyloxy substituted with -C(=O)OH, benzyl substituted with -C(=O)OH, C 1-4 alkoxy substituted with -C(=O)OH, and C 1-4 alkyl substituted with -C(=O)OH; R 37 is independently selected from H, phenyl, and pyridine; q is 0, 1, 2, or 3; R 8 is H or methyl; R 9 is H, —CH 3 , or phenyl; The antibody-drug conjugate according to any one of claims 3 to 13. Claim 15: (1) The peptide group represented by Lp comprises 1 to 4, or 1 to 3, or 1 or 2 amino acid residues, optionally selected from L-glycine (Gly), L-valine (Val), L-citrulline (Cit), L-cysteic acid (sulfo-Ala), L-lysine (Lys), L-isoleucine (Ile), L-phenylalanine (Phe), L-methionine (Met), L-asparagine (Asn), L-proline (Pro), L-alanine (Ala), L-leucine (Leu), L-tryptophan (Trp), and L-tyrosine (Tyr); (2) the peptide group represented by Lp comprises Val-Cit, Phe-Lys, Val-Ala, Val-Lys, Leu-Cit, Sulfo-Ala-Val, and / or Sulfo-Ala-Val-Ala; and / or (3) The peptide group represented by Lp is 【Chemistry 70】 Selected from The antibody-drug conjugate according to any one of claims 12 to 14.

16. -(LD) is a compound of the formula: （１） 【Chemistry 71】 A compound of the formula: R is H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemical Formula 72】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （２） 【Chemical Formula 73】 A compound of the formula: R is H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemical 74】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （３） 【Chemistry 75】 A compound of the formula: R is H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemical 76】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （４） 【Chemical 77】 A compound of the formula: Each R is H, —CH ３ , and -CH ２ CH ２ C(═O)OH; A is a bond, -OC(=O)-*, 【Chemical 78】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （５） 【Chemical 79】 A compound of the formula: Each R is H, —CH ３ , or -CH ２ CH ２ C(═O)OH; A is a bond, -OC(=O)-*, 【Chemistry 80】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （６） 【Chemistry 81】 A compound of the formula: Xa is -CH ２ --, --OCH ２ --, --NHCH ２ - or -NRCH ２ -, and each R is independently H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemistry 82】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （７） 【Chemistry 83】 A compound of the formula: R is H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemistry 84】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （８） 【Chemistry 85】 A compound of the formula: Xb is -CH ２ --, --OCH ２ --, --NHCH ２ - or -NRCH ２ -, and each R is independently H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemistry 86】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （９） 【Chemistry 87】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 88】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （１０） 【Chemistry 89】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 90】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （１１） 【Chemistry 91】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 92】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （１２） 【Chemistry 93】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 94】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （１３） 【Chemistry 95】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 96】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （１４） 【Chemistry 97】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 98】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; （１５） 【Chemistry 99】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 100】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; compound; or （１６） 【Chemistry 101】 A compound of the formula: Each R is independently H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemistry 102】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; Compound, or （１７） 【Chemistry 103】 A compound of the formula: Each R is independently H, -CH ３ , or -CH ２ CH ２ C(=O)OH; A is a bond, -OC(=O)-*, 【Chemistry 104】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; n is an integer from 2 to 24; D is a Bcl-xL inhibitor; Compound, or （１８） 【Chemistry 105】 A compound of the formula: A is a bond, -OC(=O)-*, 【Chemistry 106】 , -OC(=O)N(CH ３ ) CH ２ CH ２ N (CH ３ )C(=O)-*, or -OC(=O)N(CH ３ ) C(R ａ ) ２ C(R ａ ) ２ N (CH ３ )C(=O)-*, In the formula, each R ａ is H, C １ ~C ６ Alkyl, and C ３ ~C ８ cycloalkyl, where the * in A indicates the point of attachment to D; D is a Bcl-xL inhibitor; Compound, or （１９） -(L-D) is 【Chemistry 107-1】 【Chemistry 107-2】 【Chemistry 107-3】 【Chemistry 107-4】 【Chemistry 107-5】 【Chemistry 107-6】 【Chemistry 107-7】 【Chemistry 107-8】 【Chemistry 107-9】 【Chemistry 107-10】 【Chemistry 107-11】 【Chemistry 107-12】 【Chemistry 107-13】 【Chemistry 107-14】 【Chemistry 107-15】 【Chemistry 107-16】 The antibody-drug conjugate of any one of claims 12 to 15, which is formed from a compound selected from: (1) A is a bond and / or R is -CH 2 or -CH 2 -CH 2 -COOH; or (2) A is -OC(=O)* and / or R is -CH2 or -CH2-CH2-COOH; The antibody-drug conjugate according to any one of claims 12 to 16.

18. D comprises a compound of formula (II), wherein A in formula (II) １ and A ５ Both represent nitrogen atoms, R １ is a linear or branched C １～６ alkyl; R ２ The antibody-drug conjugate of any one of claims 1 to 17, wherein: is H; n is 1; and represents a single bond.

19. G is -C(O)OR Ｇ３ , -C(O)NR Ｇ１ R Ｇ２ , -C(O)R Ｇ２ , -NR Ｇ１ C(O)R Ｇ２ , -NR Ｇ１ C(O)NR Ｇ１ R Ｇ２ , -OC(O)NR Ｇ１ R Ｇ２ , -NR Ｇ１ C(O)OR Ｇ３ , -C(=NOR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ C(=NCN)NR Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ N.R. Ｇ１ R Ｇ２ , -S(O) ２ R Ｇ３ , -S(O) ２ N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ R Ｇ２ , -NR Ｇ１ C (=NR Ｇ２ ) N.R. Ｇ１ R Ｇ２ , -C(=S)NR Ｇ１ R Ｇ２ , -C(=NR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , halogen, -NO ２ and -CN, -R Ｇ１ and R Ｇ２ each occurrence independently represents hydrogen, C optionally substituted by 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, C ３ ~C ６ Cycloalkyl, phenyl, and -(CH ２ ) １～４ - phenyl; -R Ｇ３ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, C ３ ~C ６ Cycloalkyl, phenyl, and -(CH ２ ) １～４ -phenyl; or R Ｇ１ and R Ｇ２ Each of them, together with the atom to which it is bonded, is C ３ ~C ８ forming a heterocycloalkyl; or alternatively, G is 【Chemistry 108】 wherein R Ｇ４ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ Alkyl, C ２ ~C ６ Alkenyl, C ２ ~C ６ Alkynyl, and C ３ ~C ６ cycloalkyl, The antibody-drug conjugate according to any one of claims 1 to 18.

20. (1) D is represented by formula (IA) or formula (IIA): 【Chemistry 109】 or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any one of these, wherein Z １ represents a bond or -O-; ・R ３ is hydrogen; ３ ~C ６ Cycloalkyl; linear or branched C １ ~C ６ Alkyl; -X １ -NR ａ R ｂ ;-X １ -N ＋ R ａ R ｂ R ｃ and -X １ -O-R ｃ represents a group selected from ・R ａ and R ｂ are each independently hydrogen; linear or branched C optionally substituted with one or two hydroxyl groups; １ ~C ６ Alkyl; and C １ ~C ６ Alkylene-SO ２ O － represents a group selected from ・R ｃ is hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, ・Het ２ teeth, 【Chemistry 110】 represents a group selected from ・A １ is -NH-, -N(C １ ~C ３ alkyl), O, S, or Se; ・A ２ is N, CH, or C(R ５ ) and ・G is -C(O)OH, -C(O)OR Ｇ３ , -C(O)NR Ｇ１ R Ｇ２ , -C(O)R Ｇ２ , -NR Ｇ１ C(O)R Ｇ２ , -NR Ｇ１ C(O)NR Ｇ１ R Ｇ２ , -OC(O)NR Ｇ１ R Ｇ２ , -NR Ｇ１ C(O)OR Ｇ３ , -C(=NOR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ C(=NCN)NR Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ N.R. Ｇ１ R Ｇ２ , -S(O) ２ R Ｇ３ , -S(O) ２ N.R. Ｇ１ R Ｇ２ , -NR Ｇ１ S (O) ２ R Ｇ２ , -NR Ｇ１ C (=NR Ｇ２ ) N.R. Ｇ１ R Ｇ２ , -C(=S)NR Ｇ１ R Ｇ２ , -C(=NR Ｇ１ ) N.R. Ｇ１ R Ｇ２ , hydroxyl group, halogen, -NO ２ and C optionally substituted by -CN １ ~C ６ alkyl, wherein -R Ｇ１ and R Ｇ２ each occurrence independently represents hydrogen and C optionally substituted with 1 to 3 halogen atoms; １ ~C ６ selected from the group consisting of alkyl; -R Ｇ３ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ is alkyl; or R Ｇ１ and R Ｇ２ Each of them, together with the atom to which it is bonded, is C ３ ~C ８ forming a heterocycloalkyl; ・R ４ represents a hydrogen, fluorine, chlorine or bromine atom, a methyl, hydroxyl or methoxy group, ・R ５ is C optionally substituted with 1 to 3 halogen atoms １ ~C ６ represents a group selected from alkyl; halogen; or -CN, ・R ６ teeth, -X ２ -O-R ７ and Linear or branched C １ ~C ６ Heteroarylene-R optionally substituted with an alkyl group ７ base represents a group selected from ・R ７ is a linear or branched C １ ~C ６ Alkyl groups; and (C ３ ~C ６ ) Cycloalkylene-R ８ represents a group selected from or: R 7 is 【Chemistry 111】 wherein Cy represents a group selected from ３ ~C ８ represents cycloalkyl; ・R ８ is hydrogen; linear or branched C １ ~C ６ Alkyl, -NR' ａ R' ｂ -NR' ａ -CO-OR' ｃ -NR' ａ -CO-R' ｃ ;-N ＋ R' ａ R' ｂ R' ｃ ;-O-R' ｃ -NH-X' ２ -N ＋ R' ａ R' ｂ R' ｃ ;-O-X' ２ -NR' ａ R' ｂ ;-X' ２ -NR' ａ R' ｂ : -NR' ｃ -X' ２ -N ３ , and: 【Chemistry 112】 represents a group selected from ・R １０ is hydrogen, fluorine, chlorine, bromine, -CF ３ and methyl, ・R １１ is hydrogen, C １ ~C ３ Alkylene-R ８ , -O-C １ ~C ３ Alkylene-R ８ , —CO—NR ｈ R ｉ and -CH=CH-C １ ~C ４ Alkylene -NR ｈ R ｉ , -CH=CH-CHO,C ３ ~C ８ Cycloalkylene -CH ２ -R ８ , and C ３ ~C ８ Heterocycloalkylene -CH ２ -R ８ represents a group selected from ・R １２ and R １３ each independently represents a hydrogen atom or a methyl group, ・R １４ and R １５ are each independently a hydrogen atom or a methyl group, or R １４ and R １５ together with the carbon atom carrying these groups form a cyclohexyl; ・R ｈ and R ｉ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, X １ and X ２ are each independently trifluoromethyl, hydroxyl, halogen, C １ ~C ６ Linear or branched C optionally substituted with one or two groups selected from alkoxy １ ~C ６ represents an alkylene group, ・X' ２ is a linear or branched C １ ~C ６ represents alkylene, ・R' ａ and R' ｂ are each independently hydrogen; heterocycloalkyl; phenyl is a straight or branched C １ ~C ６ -SO optionally substituted with alkyl ２ -phenyl; 1 or 2 hydroxyl or C １ ~C ６ Linear or branched C optionally substituted with alkoxy groups １ ~C ６ Alkyl; C １ ~C ６ Alkylene-SO ２ OH;C １ ~C ６ Alkylene-SO ２ O － ; C １ ~C ６ Alkylene-COOH; １ ~C ６ Alkylene-PO(OH) ２ ; C １ ~C ６ Alkylene-NR' ｄ R' ｅ ; C １ ~C ６ Alkylene-N ＋ R' ｄ R' ｅ R' ｆ ; C １ ~C ６ Alkylene -O-C １ ~C ６ Alkylene-OH; Phenyl is hydroxyl or C １ ~C ６ C optionally substituted by an alkoxy group １ ~C ６ alkylene-phenyl; and 【Chemistry 113】 represents a group selected from or R' ａ and R' ｂ together with the nitrogen atom bearing these groups form ring B ３ It is formed, or R' ａ , R' ｂ and R' ｃ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, ・R' ｃ , R' ｄ , R' ｅ , R' ｆ are each independently hydrogen or a linear or branched C １ ~C ６ represents an alkyl group, or R' ｄ and R' ｅ together with the nitrogen atom bearing these groups form ring B ４ It is formed, or R' ｄ , R' ｅ and R' ｆ The nitrogen atom having these groups together forms a bridge C ３ ~C ８ forming a heterocycloalkyl, m is 0, 1, or 2, p is 1, 2, 3, or 4; ・B ３ and B ４ are, independently of each other, C ３ ~C ８ represents a heterocycloalkyl group, which (i) may be a monocyclic or bicyclic group, including fused rings, bridged rings, or spiro ring systems; (ii) may contain, in addition to the nitrogen atom, one or two heteroatoms independently selected from oxygen, sulfur, and nitrogen; or (iii) may contain fluorine, bromine, chlorine, linear or branched C １ ~C ６ Alkyl, hydroxyl, -NH ２ , oxo, or piperidinyl; or (2) D is a compound of formula (IB), (IC), (IIB), or (IIC): 【Chemistry 114】 or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any one of the foregoing, wherein With respect to formula (IB) or (IC), R 3 represents a group selected from hydrogen; linear or branched C 1 -C 6 alkyl; -X 1 -NR a R b ; -X 1 -N + R a R b R c ; and -X 1 -O-R c ; With respect to formula (IIB) or (IIC), Z 1 represents a bond and R 3 represents hydrogen; or Z 1 represents --O-- and R 3 represents --X 1 --NR a R b ; R a and R b independently of one another represent a group selected from hydrogen; linear or branched C 1 -C 6 alkyl optionally substituted by one or two hydroxyl groups; and C 1 -C 6 alkylene -SO 2 O - ; R c represents hydrogen or a linear or branched C 1 -C 6 alkyl group; R 6 represents -X 2 -O-R 7 or a heteroarylene-R 7 group optionally substituted by a linear or branched C 1 -C 6 alkyl group; R 7 is 【Chemistry 115】 represents a group selected from R 8 represents a group selected from -NR' a R' b ; -O-X' 2 -NR' a R' b ; and -X' 2 -NR' a R' b , R 10 represents fluorine; R 12 and R 13 each independently represent a hydrogen atom or a methyl group; R 14 and R 15 are each independently a hydrogen atom or a methyl group; X 1 and X 2 independently of one another represent a linear or branched C 1 -C 6 alkylene radical optionally substituted by one or two radicals selected from trifluoromethyl, hydroxyl, halogen, C 1 -C 6 alkoxy, X' 2 represents a linear or branched C 1 -C 6 alkylene; R' a and R' b independently of one another represent a group selected from hydrogen; linear or branched C 1 -C 6 alkyl optionally substituted by one or two hydroxyl or C 1 -C 6 alkoxy groups; C 1 -C 6 alkylene-NR' d R' e ; or R' a and R' b together with the nitrogen atom to which they belong form a ring B 3 ; R' d and R' e are each independently a hydrogen atom or a linear or branched C 1 -C 6 alkyl group; B 3 represents a C 3 -C 8 heterocycloalkyl group, which (i) may be a monocyclic or bicyclic group including fused rings, bridged rings, or spiro ring systems, (ii) may contain, in addition to the nitrogen atom, one or two heteroatoms independently selected from oxygen and nitrogen, and (iii) may be substituted by one or two groups selected from fluorine, bromine, chlorine, linear or branched C 1 -C 6 alkyl, hydroxyl, and oxo; An antibody-drug conjugate according to any one of claims 1 to 17.

21. (i) R ７ is a linear or branched C １ ~C ６ Alkyl group; ３ ~C ６ ) Cycloalkylene-R ８ or R 7 is: 【Chemistry 116】 wherein Cy represents a C 3 -C 8 cycloalkyl; (ii) R 7 is 【Chemistry 117】 represents a group selected from (iii) R 7 is the following group: 【Chemistry 118】 Represents; (iv) R 7 is 【Chemistry 119】 represents a group selected from (v) R 8 is 【Chemistry 120】 represents a group selected from the group consisting of 【Chemistry 121】 represents a bond to the linker, and / or (vi) B 3 represents a C 3 -C 8 heterocycloalkyl group selected from a pyrrolidinyl group, a piperidinyl group, a piperazinyl group, a morpholinyl group, an azepanyl group, and a 4,4-difluoropiperidin-1-yl group; The antibody-drug conjugate according to any one of claims 1 to 20.

22. (1) D is the following bonded to L: 【Table 1-1】 【Table 1-2】 【Table 1-3】 【Table 1-4】 【Table 1-5】 【Table 1-6】 【Table 1-7】 【Table 1-8】 【Table 1-9】 【Table 1-10】 【Table 1-11】 or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any one of these, or (2) D is, 【Table 2-1】 【Table 2-2】 【Table 2-3】 【Table 2-4】 【Table 2-5】 【Table 2-6】 【Table 2-7】 【Table 2-8】 【Table 2-9】 【Table 2-10】 【Table 2-11】 or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any one of these, An antibody-drug conjugate according to any one of claims 1 to 17.

23. The antibody-drug conjugate of any one of claims 1 to 17, wherein -(LD) is formed from a compound selected from the following, or an enantiomer, diastereoisomer, and / or a pharma- ceutically acceptable salt of any of these: 【Table 3-1】 【Table 3-2】 【Table 3-3】 【Table 3-4】 【Table 3-5】 【Table 3-6】 【Table 3-7】 【Table 3-8】 【Table 3-9】 【Table 3-10】 【Table 3-11】 【Table 3-12】 【Table 3-13】 【Table 3-14】 【Table 3-15】 【Table 3-16】 【Table 3-17】 【Table 3-18】 【Table 3-19】 【Table 3-20】 【Table 3-21】 【Table 3-22】 【Table 3-23】 【Table 3-24】 【Table 3-25】 【Table 3-26】 【Table 3-27】 【Table 3-28】 【Table 3-29】 【Table 3-30】 【Table 3-31】 【Table 3-32】 【Table 3-33】 【Table 3-34】 【Table 3-35】 【Table 3-36】 【Table 3-37】 【Table 3-38】 【Table 3-39】 【Table 3-40】 【Table 3-41】 【Table 3-42】 【Table 3-43】 【Table 3-44】 【Table 3-45】 【Table 3-46】 【Table 3-47】 【Table 3-48】 【Table 3-49】 【Table 3-50】 【Table 3-51】 【Table 3-52】 【Table 3-53】 【Table 3-54】 【Table 3-55】 24. (i) the antibody or antigen-binding fragment thereof binds to a target antigen on a cancer cell; (ii) the antibody or antigen-binding fragment thereof binds to a target antigen on a cancer cell, and the target antigen is selected from BCMA, CD33, HER2, CD38, CD48, CD79b, PCAD, CD74, CD138, SLAMF7, CD123, CLL1, FLT3, CD7, CKIT, CD56, DLL3, DLK1, B7-H3, EGFR, CD71, EPCAM, FOLR1, ENPP3, MET, AXL, SLC34A2, Nectin4, TROP2, LIV1, CD46, MSLN, F3, MUC16, SLC39A6, TFRC, TACSTD2, and GPNMB; (iii) the antibody or antigen-binding fragment thereof binds to a target antigen on a cancer cell, and the target antigen is selected from EGFR, CD7, HER2, EPCAM, FOLR1, ENPP3, MET, AXL, SLC34A2, Nectin4, MSLN, F3, MUC16, SLC39A6, TFRC, TACSTD2, and GPNMB; (iv) the antibody or antigen-binding fragment thereof binds to a target antigen on a cancer cell, and the target antigen is EGFR, CD7, or HER2; (v) the antibody or antigen-binding fragment thereof is an anti-EGFR antibody or antigen-binding fragment thereof; (vi) the antibody or antigen-binding fragment thereof is an anti-EGFR antibody or antigen-binding fragment thereof, and the anti-EGFR antibody or antigen-binding fragment thereof is (a) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 92, and a light chain variable region comprising the amino acid sequence of SEQ ID NO: 93; or (b) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 124, and a light chain variable region comprising the amino acid sequence of SEQ ID NO:

125. Contains; (vii) the antibody or antigen-binding fragment thereof is an anti-CD7 antibody or antigen-binding fragment thereof; (viii) the antibody or antigen-binding fragment thereof is an anti-CD7 antibody or antigen-binding fragment thereof, wherein the anti-CD7 antibody comprises a heavy chain amino acid sequence of SEQ ID NO: 143, and a light chain amino acid sequence of SEQ ID NO: 144; (ix) the antibody or antigen-binding fragment thereof is an anti-HER2 antibody or antigen-binding fragment thereof; (x) the antibody or antigen-binding fragment thereof is an anti-HER2 antibody or antigen-binding fragment thereof, and the antibody or antigen-binding fragment thereof is (a) three heavy chain complementarity determining regions (HCDRs) comprising the amino acid sequences of SEQ ID NO: 39 (HCDR1), SEQ ID NO: 40 (HCDR2), and SEQ ID NO: 41 (HCDR3); and three light chain complementarity determining regions (LCDRs) comprising the amino acid sequences of SEQ ID NO: 42 (LCDR1), SEQ ID NO: 43 (LCDR2), and SEQ ID NO: 44 (LCDR3); and / or (b) the antibody or antigen-binding fragment comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:9, and a light chain variable region comprising the amino acid sequence of SEQ ID NO:10; or (xi) the antibody or antigen-binding fragment thereof is an anti-HER2 antibody or antigen-binding fragment thereof, and the antibody or antigen-binding fragment thereof comprises: (a) an IgG1 heavy chain constant domain or a modified IgG1 heavy chain constant domain, optionally wherein said IgG1 heavy chain constant domain comprises a glutamine (Q) at position 297 or wherein said IgG1 heavy chain constant domain comprises a serine (S) at position 297; and / or (b) the antibody or antigen-binding fragment thereof comprises an Ig kappa light chain constant domain; An antibody-drug conjugate according to any one of claims 1 to 23.

25. 25. A composition comprising multiple copies of the antibody-drug conjugate of any one of claims 1 to 24, wherein the average p of said antibody-drug conjugate in the composition is from about 2 to about 16, from about 2 to about 8, or from about 2 to about 4.

26. A pharmaceutical composition comprising the antibody-drug conjugate of any one of claims 1 to 24 or the composition of claim 25, and a pharma- ceutically acceptable carrier.

27. A therapeutically effective amount of the antibody-drug conjugate of any one of claims 1 to 24, the composition of claim 25, or the pharmaceutical composition of claim 26. (1) A method of treating a subject having or suspected of having cancer; (2) A method for suppressing or inhibiting the growth of a tumor in a subject; (3) a method for suppressing or inhibiting a hematological cancer in a subject; or (4) Methods for inhibiting or slowing the growth of a cancer cell population in a subject A pharmaceutical composition for use in, optionally comprising: a) the cancer is breast cancer, multiple myeloma, plasma cell myeloma, leukemia, lymphoma, sarcoma, gastric cancer, acute myeloid leukemia, bladder cancer, brain cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoid leukemia including acute lymphocytic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, prostate cancer, small cell lung cancer, splenic cancer, or head and neck cancer; b) the tumor is breast cancer, gastric cancer, bladder cancer, brain cancer, cervical cancer, colorectal cancer, esophageal cancer, hepatocellular carcinoma, melanoma, oral cancer, ovarian cancer, non-small cell lung cancer, prostate cancer, small cell lung cancer, or splenic cancer; c) the hematological cancer is chronic lymphocytic leukemia (CLL), follicular lymphoma, mantle cell lymphoma, diffuse large B-cell lymphoma, acute lymphocytic leukemia (ALL), acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), chronic myelogenous leukemia (CML), chronic myelomonocytic leukemia (CMML), acute monocytic leukemia (AMoL), Hodgkin's lymphoma, non-Hodgkin's lymphoma, or myelodysplastic syndrome (MDS); or d) the cancer cell population is derived from a tumor or hematological cancer, and optionally the cancer cell population is derived from breast cancer, multiple myeloma, plasma cell myeloma, leukemia, lymphoma, sarcoma, gastric cancer, acute myeloid leukemia, bladder cancer, brain cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoid leukemia including acute lymphocytic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, prostate cancer, small cell lung cancer, splenic cancer, or head and neck cancer; Pharmaceutical compositions.

28. 25. A pharmaceutical composition for use in a method for inhibiting Bcl-xL activity in a cell expressing Bcl-xL, comprising the step of contacting the cell with an antibody-drug conjugate of any one of claims 1 to 24 capable of binding to the cell under conditions in which the antibody-drug conjugate binds to the cell.

29. 27. A pharmaceutical composition for use in a method of determining whether a subject having or suspected of having cancer will be responsive to treatment with an antibody-drug conjugate of any one of claims 1 to 24, a composition of claim 25, or a pharmaceutical composition of claim 26, comprising providing a biological sample from the subject; contacting the sample with an antibody drug conjugate; and detecting binding of the antibody drug conjugate to cancer cells in the sample, optionally comprising: (1) the cancer cells in the sample express a target antigen; (2) the cancer expresses a target antigen; (3) the cancer is a tumor or a blood cancer, and optionally the cancer is breast cancer, multiple myeloma, plasma cell myeloma, leukemia, lymphoma, sarcoma, gastric cancer, acute myeloid leukemia, bladder cancer, brain cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoid leukemia including acute lymphocytic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, prostate cancer, small cell lung cancer, splenic cancer, or head and neck cancer; or (4) The sample is a tissue biopsy sample, a blood sample, or a bone marrow sample. Pharmaceutical compositions.

30. 25. A method of producing an antibody-drug conjugate according to any one of claims 1 to 24, comprising reacting an antibody or antigen-binding fragment with a cleavable linker conjugated to a Bcl-xL inhibitor under conditions that allow conjugation.