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COMPOSITIONS AND METHODS FOR TREATING CASTRATION-RESISTANT PROSTATE CANCER

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  • Publication Date:
    September 28, 2023
  • معلومة اضافية
    • Document Number:
      20230302021
    • Appl. No:
      18/187866
    • Application Filed:
      March 22, 2023
    • نبذة مختصرة :
      This present disclosure teaches a method for treating or delaying castration-resistant prostate cancer (CRPC) comprising co-administering to a subject in need of relief from said cancer a therapeutically effective amount of a sterol-O-acyltransferase 1 (SOAT1) inhibitor together with a therapeutically effective amount of one or more androgen receptor inhibitors/antagonists. Examples of inhibitor/antagonist of androgen receptor and androgen biosynthesis include enzalutamide and abiraterone; and examples of SOAT1 inhibitors include avasimibe. Pharmaceutical compositions and methods of uses for the treatment of CRPCs are within the scope of this disclosure.
    • Claim:
      1. A method for treating or delaying castration-resistant prostate cancer (CRPC) comprising co-administering to a subject in need of relief from said cancer a therapeutically effective amount of a sterol-O-acyltransferase 1 (SOAT1) inhibitor together with a therapeutically effective amount of one or more inhibitors/antagonists of androgen receptor of androgen biosynthesis.
    • Claim:
      2. The method according to claim 1, wherein said androgen receptor inhibitor/antagonist comprises enzalutamide, bicalutamide, apalutamide, flutamide, nilutamide, darolutamide, and clascoterone, or a pharmaceutically acceptable salt thereof.
    • Claim:
      3. The method according to claim 1, wherein said androgen receptor inhibitor/antagonist is enzalutamide, or a pharmaceutically acceptable salt thereof.
    • Claim:
      4. The method according to claim 1, wherein said androgen biosynthesis inhibitor/antagonist is abiraterone, or a pharmaceutically acceptable salt thereof.
    • Claim:
      5. The method according to claim 1, wherein said CRPC is an androgen receptor inhibitor-resistant CRPC.
    • Claim:
      6. The method according to claim 5, wherein said CRPC androgen receptor inhibitor-resistant CRPC is an enzalutamide-resistant CRPC.
    • Claim:
      7. The method according to claim 1, wherein said CRPC is an androgen biosynthesis inhibitor-resistant CRPC.
    • Claim:
      8. The method according to claim 7, wherein said CRPC androgen biosynthesis antagonist-resistant CRPC is an abiraterone-resistant CRPC.
    • Claim:
      9. The method according to claim 1, wherein said SOAT1 inhibitor comprises avasimibe (CI-1011), CI-976, CP113,818, pactimibe, NTE-122, F-1394, PD140296, PD128042, PD132301-2, octimibate, DuP128, 58-035, HL-004, SMP-500, CL-277,082, SKF-99085, CS-505, eflucimibe (F12511), E5324, FR145237, CL277,082, YM-17E, FR129169, K-604, pyrocarbonate, beauveriolides I, and methanol extracts of Saururus chinensis root containing saucerneol B and manassantin B, or a pharmaceutically acceptable salt thereof.
    • Claim:
      10. The method according to claim 1, wherein said SOAT1 inhibitor is avasimibe, or a pharmaceutically acceptable salt thereof.
    • Claim:
      11. The method according to claim 1, wherein said androgen receptor inhibitor/antagonist and said SOAT1 inhibitor are combined first and administered consequently.
    • Claim:
      12. The method according to claim 1, wherein said androgen receptor inhibitor/antagonist and said SOAT1 inhibitor are formulated separately and administered consequently.
    • Claim:
      13. A pharmaceutical composition comprising a SOAT1 inhibitor and an inhibitor/antagonist of androgen receptor or androgen biosynthesis, together with one or more pharmaceutically acceptable diluents, excipients, or carriers.
    • Claim:
      14. The pharmaceutical composition according to claim 13, wherein said androgen receptor inhibitor/antagonist comprises enzalutamide, bicalutamide, apalutamide, flutamide, nilutamide, darolutamide, and clascoterone, or a pharmaceutically acceptable salt thereof.
    • Claim:
      15. The pharmaceutical composition according to claim 13, wherein said androgen receptor inhibitor/antagonist is enzalutamide, or a pharmaceutically acceptable salt thereof.
    • Claim:
      16. The pharmaceutical composition according to claim 13, wherein said androgen biosynthesis inhibitor/antagonist is abiraterone, or a pharmaceutically acceptable salt thereof.
    • Claim:
      17. The pharmaceutical composition according to claim 13, wherein said CRPC is an androgen receptor inhibitor-resistant CRPC.
    • Claim:
      18. The pharmaceutical composition according to claim 17, wherein said CRPC androgen receptor inhibitor-resistant CRPC is an enzalutamide-resistant CRPC.
    • Claim:
      19. The pharmaceutical composition according to claim 13, wherein said CRPC is an androgen biosynthesis inhibitor-resistant CRPC.
    • Claim:
      20. The pharmaceutical composition according to claim 19, wherein said CRPC androgen biosynthesis antagonist-resistant CRPC is an abiraterone-resistant CRPC.
    • Claim:
      21. The pharmaceutical composition according to claim 13, wherein said SOAT1 inhibitor comprises avasimibe (CI-1011), CI-976, CP113,818, pactimibe, NTE-122, F-1394, PD140296, PD128042, PD132301-2, octimibate, DuP128, 58-035, HL-004, SMP-500, CL-277,082, SKF-99085, CS-505, eflucimibe (F12511), E5324, FR145237, CL277,082, YM-17E, FR129169, K-604, pyrocarbonate, beauveriolides I, and methanol extracts of Saururus chinensis root containing saucerneol B and manassantin B, or a pharmaceutically acceptable salt thereof.
    • Claim:
      22. The pharmaceutical composition according to claim 13, wherein said SOAT1 inhibitor is avasimibe, or a pharmaceutically acceptable salt thereof.
    • Current International Class:
      61; 61; 61; 61
    • الرقم المعرف:
      edspap.20230302021