Targeted amatoxin conjugate for the treatment of solid tumors

A technology of amanita toxin and conjugate, which is applied in the directions of antitumor drugs, drug combinations, medical preparations of inactive ingredients, etc.

Pending Publication Date: 2020-11-24
HEIDELBERG PHARMA RES GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, applicants have recognized that there is still room for improvement in the

Method used

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  • Targeted amatoxin conjugate for the treatment of solid tumors
  • Targeted amatoxin conjugate for the treatment of solid tumors
  • Targeted amatoxin conjugate for the treatment of solid tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0065] According to yet another embodiment, the linker comprises a motif selected from the group consisting of:

[0066] ·Val Ala

[0067] ·Val Cit

[0068] ·Val Lys

[0069] ·Val Arg

[0070] ·Phe Lys Gly Pro Leu Gly

[0071] ·Ala Ala Pro Val

[0072] · β-glucuronide

[0073] · β-galactoside.

[0074] According to yet another embodiment, the reactive group Y in the linker is at least one selected from the following:

[0075] ·Maleimide

[0076] 3,4-Diphenylsulfanyl-maleimide

[0077] 4,5-bis(2-pyridyl-sulfanyl)-1,2-dihydropyridazine-3,6-dione

[0078] ·DBCO

[0079] ·DIBO

[0080] ·HIPS

[0081] 2-(4-Hydroxyphenyl)-5-(methylsulfonyl)-1,3,4-oxadiazole

[0082] ·APN

[0083] ·Succinimide

[0084] ·Succinimidyl carbamate

[0085] ·Bromoacetamide

[0086] ·Iodoacetamide

[0087] According to yet another embodiment, the linker comprises a p-aminobenzene ValAla maleimidopropyl motif.

[0088]

[0089] According to yet another embodiment...

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Abstract

The present invention relates to an amatoxin-linker construct comprising an amatoxin according to formula (I) wherein: R1 and R2 are each -OH, R3 is NH2, or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R4 is H or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R5 is absent or =O, wherein R3 and R4 cannot be the same, for use in the manufacture of a binding moiety-toxin conjugate for the treatment of a solid tumor, and a respective binding moiety-toxin conjugate for the treatment of a solid tumor.

Description

[0001] field of invention [0002] The present application relates to targeted amanitin conjugates for the treatment of solid tumors. [0003] Background of the invention [0004] The treatment of solid tumors is an ongoing challenge that has seen little progress over the past few decades. Although considerable new treatment modalities have been developed recently, further improvements are still needed to increase the survival rate and improve the quality of life of patients with solid tumors. [0005] One promising therapeutic modality is antibody-drug conjugates, in which a highly toxic entity with cell-killing capacity is coupled to a target-binding entity that shuttles the toxin to the site of disease. [0006] Applicants have in the past developed so-called ATACs, ie, Antibody-Targeted Abotin Conjugates, in which abotin toxins are conjugated to highly target-specific antibodies. Amanitine is an eight amino acid bicyclic peptide that occurs naturally in several species of...

Claims

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Application Information

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IPC IPC(8): A61K47/68A61P35/00A61P35/02
CPCA61K47/6831A61K47/6855A61K47/6867A61K47/6869A61K38/12A61K47/65A61K47/6871A61P35/00
Inventor C·米勒W·西蒙C·卢茨S·维尔纳-西蒙T·黑希勒M·库尔克A·帕尔
Owner HEIDELBERG PHARMA RES GMBH
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