Composition containing a P53 peptide amphiphilic substance and method of use thereof

JP2026518761APending Publication Date: 2026-06-09ELICIO THERAPEUTICS INC
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
ELICIO THERAPEUTICS INC
Filing Date
2024-05-24
Publication Date
2026-06-09

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Abstract

Compounds comprising an albumin-binding domain and a mutant or wild-type p53 peptide, as well as pharmaceutically acceptable salts thereof, are disclosed herein. Furthermore, methods for inducing an immune response in a subject, and methods for inducing an immune response in a subject by administering such compounds, are disclosed herein.
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Claims

1. A compound containing an albumin-binding domain and a mutant p53 peptide, or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide is a 5-50 amino acid fragment of SEQ ID NO: 1, comprising at least one amino acid substitution to the corresponding sequence of SEQ ID NO:

1.

3. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide is a 20-40 amino acid fragment of SEQ ID NO: 1, comprising at least one amino acid substitution to the corresponding sequence of SEQ ID NO:

1.

4. The compound according to claim 3 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide is a 20-30 amino acid fragment of SEQ ID NO: 1, comprising at least one amino acid substitution to the corresponding sequence of SEQ ID NO:

1.

5. The compound according to claim 4 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide is a 30-amino acid fragment of SEQ ID NO: 1, comprising at least one amino acid substitution to the corresponding sequence of SEQ ID NO:

1.

6. The compound according to any one of claims 1 to 5 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide comprises at least one of the amino acid substitutions listed in Table 1.

7. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide consists of the amino acid sequence YMCNSSCMGGMNWRPILTIILEDS (SEQ ID NO: 2).

8. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide consists of the amino acid sequence YMCNSSCMGGMNQRPILTIITLEDS (SEQ ID NO: 3).

9. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide comprises the 10-amino acid fragment of SEQ ID NO: 2 or 3.

10. The compound according to claim 9 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide comprises the amino acid sequence NWRPILTIIT (SEQ ID NO: 46) or NQRPPILTIIT (SEQ ID NO: 47).

11. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide comprises the 10, 18, or 25 amino acid fragment of SEQ ID NO: 2 or 3.

12. The compound according to claim 11 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide comprises the amino acid sequence NSSCMGGGMNWRPILTIIT (SEQ ID NO: 48) or NSSCMGGGMNQRPPILTIIT (SEQ ID NO: 49).

13. The aforementioned mutant p53 peptide 【Chemistry 1】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

14. The aforementioned mutant p53 peptide 【Chemistry 2】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

15. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the mutant p53 peptide consists of the amino acid sequence of NSFEVVCACPGRDWRTEENLRKKGEPHH (SEQ ID NO: 114) or a fragment thereof.

16. The aforementioned mutant p53 peptide 【Transformation 3】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

17. The aforementioned mutant p53 peptide 【Chemistry 4】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

18. The aforementioned mutant p53 peptide 【Transformation 5】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

19. The aforementioned mutant p53 peptide 【Transformation 6】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

20. The aforementioned mutant p53 peptide 【Transformation 7】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

21. The aforementioned mutant p53 peptide 【Transformation 8】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

22. The aforementioned mutant p53 peptide 【Chemistry 9】 A compound according to claim 1, or a pharmaceutically acceptable salt thereof, comprising the amino acid sequence or a fragment thereof.

23. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide contains the sequence MAIYKQSQHMTEVVRRCPHHERCSSDGLAP (SEQ ID NO: 100) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

24. The compound according to claim 23 or a pharmaceutically acceptable salt thereof, wherein the fragment comprises the sequence AIYKQSQHM (Sequence ID 101).

25. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide includes the sequence EGNLRVEYLDDRNTFRHSVVVPPCEPPEVGSD (SEQ ID NO: 102), or a fragment thereof, or a pharmaceutically acceptable salt thereof.

26. The compound according to claim 25 or a pharmaceutically acceptable salt thereof, wherein the fragment comprises the sequence EYLDDRNTF (SEQ ID NO: 103).

27. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide comprises the sequence YLDDRNTFRHSVVVPYEPPEVGSDCTTIHYN (SEQ ID NO: 104) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

28. The compound according to claim 27 or a pharmaceutically acceptable salt thereof, wherein the fragment comprises the sequence VVPYEPPEV (SEQ ID NO: 105).

29. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide comprises the sequence TTIHYNYMCNSSCMGGMNRRPILTIITLEDSSGNL (SEQ ID NO: 106) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

30. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide contains the sequence EDSSGLLGRNSFEVRVCACPGRDRRTEEENLRKK (SEQ ID NO: 107) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

31. The compound according to claim 30 or a pharmaceutically acceptable salt thereof, wherein the fragment comprises the sequence LLGRNSFEV (SEQ ID NO: 108).

32. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide comprises the sequence RLGFLHSGTAKSVTC (SEQ ID NO: 109) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

33. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide contains the sequence STPPPGTRV (SEQ ID NO: 110) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

34. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide contains the sequence TYPALNKMF (SEQ ID NO: 111) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

35. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide includes the sequence RMPEAAPPV (SEQ ID NO: 112) or a fragment thereof, or a pharmaceutically acceptable salt thereof.

36. A compound comprising an albumin-binding domain and the p53 peptide, wherein the p53 peptide comprises the sequence TEDPGPDEAPRMPEAAPPVAAPAPAAPTPAA (SEQ ID NO: 121), or a fragment thereof, or a pharmaceutically acceptable salt thereof.

37. The compound according to any one of claims 1 to 36, or a pharmaceutically acceptable salt thereof, wherein the peptide comprises an N-terminal modification.

38. The compound according to claim 37 or a pharmaceutically acceptable salt thereof, wherein the N-terminal modification is the addition of acetylcysteine.

39. The compound according to claim 37 or a pharmaceutically acceptable salt thereof, wherein the N-terminal modification is the addition of a desaminocysteine ​​homolog.

40. The compound according to claim 39 or a pharmaceutically acceptable salt thereof, wherein the desaminocysteine ​​homolog is 3-mercaptopropionic acid or mercaptoacetic acid.

41. The compound according to any one of claims 1 to 40, or a pharmaceutically acceptable salt thereof, wherein the albumin-binding comprises a lipid.

42. The compound according to claim 41 or a pharmaceutically acceptable salt thereof, wherein the lipid is a diacyl lipid.

43. The compound according to claim 42 or a pharmaceutically acceptable salt thereof, wherein the diacyllipid comprises an acyl chain containing 12 to 30 hydrocarbon units, 14 to 25 hydrocarbon units, 16 to 20 hydrocarbon units, or 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30 hydrocarbon units.

44. The compound according to claim 42 or 43, or a pharmaceutically acceptable salt thereof, wherein the lipid is 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE).

45. The peptide in question is the following lipid: 【Chemistry 10】 A compound according to any one of claims 1 to 44 or a pharmaceutically acceptable salt thereof, which is bonded to a salt thereof or linked by a linker, wherein X is O or S.

46. The compound according to claim 45 or a pharmaceutically acceptable salt thereof, wherein the linker is selected from the group consisting of a hydrophilic polymer, a series of hydrophilic amino acids, polysaccharides, and oligonucleotides, or a combination thereof.

47. The compound according to claim 46 or a pharmaceutically acceptable salt thereof, wherein the linker contains an "N" polyethylene glycol unit and N is 24 to 50.

48. The compound according to claim 47 or a pharmaceutically acceptable salt thereof, wherein the linker comprises PEG24-amide-PEG24.

49. A method for inducing an immune response in a subject, comprising administering to the subject a compound according to any one of claims 1 to 48 or a pharmaceutically acceptable salt thereof.

50. The method according to claim 49, further comprising administering an adjuvant to the subject.

51. The method according to claim 49 or 50, wherein the compound or a pharmaceutically acceptable salt thereof is administered subcutaneously, intramuscularly, intravenously, or transmucosally.

52. The method according to any one of claims 49 to 51, wherein the subject is a mammal.

53. The method according to claim 52, wherein the subject is a human.

54. A compound comprising an albumin-binding domain and a p53 peptide or a mutant p53 peptide, or a pharmaceutically acceptable salt thereof, for use in a method of inducing an immune response in a subject, comprising administering to the subject a compound comprising a compound according to any one of claims 1 to 48.

55. The compound or a pharmaceutically acceptable salt thereof for use according to claim 54, further comprising administering an adjuvant to the subject.

56. The compound or a pharmaceutically acceptable salt thereof for use according to claim 54 or 55, formulated for subcutaneous, intramuscular, intravenous, or transmucosal administration.

57. The compound or a pharmaceutically acceptable salt thereof for use according to any one of claims 54 to 56, wherein the subject is a mammal.

58. The compound or a pharmaceutically acceptable salt thereof for use according to claim 57, wherein the subject is a human.

59. A pharmaceutical composition comprising a compound according to any one of claims 1 to 48 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

60. A kit comprising a compound according to any one of claims 1 to 48 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 59, and instructions for administration.