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Provided are methods of inhibiting CYP17 in a mammal, such as a human, that include administering an effective amount of at least one CYP17 inhibitor, such as VN/124-1, VN/125-1, VN/85-1, VN/87-1 and/or VN/108-1 to the mammal. Also provided are methods of down regulating androgen receptor (AR) protein expression and methods of antagonizing AR in a mammal that include administering to the mammal an effective amount of at least one active ingredient selected from VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Also provided are methods of treating prostate cancer and methods of suppressing or preventing prostate tumor growth by administering such compounds to a mammal.

Titel:	ANDROGEN RECEPTOR INACTIVATION CONTRIBUTES TO ANTITUMOR EFFICACY OF CYP17 INHIBITORS IN PROSTATE CANCER
Autor/in / Beteiligte Person:	Njar, Vincent C.O. ; Brodie, Angela
Link:	Zum Volltext
Veröffentlichung:	2011
Medientyp:	Patent
Sonstiges:	Nachgewiesen in: USPTO Patent Applications Sprachen: English Document Number: 20110105445 Publication Date: May 5, 2011 Appl. No: 12/921932 Application Filed: March 12, 2009 Assignees: University of Maryland, Baltimore (Baltimore, MD, US) Claim: 1. (canceled) Claim: 2. (canceled) Claim: 3. (canceled) Claim: 4. (canceled) Claim: 5. A method of down regulating androgen receptor protein expression in a mammal comprising: administering to said mammal an effective amount of at least one active ingredient selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 6. The method of claim 5, wherein said at least one active ingredient comprises VN/124-1. Claim: 7. The method of claim 5, wherein said at least one active comprises two or more active ingredients selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 8. The method of claim 5, wherein the mammal is a human. Claim: 9. The method of claim 5, wherein said method comprises a method of down regulating androgen receptor protein expression in LNCaP or LAPC4 cells. Claim: 10. A method of antagonizing androgen receptor in a mammal comprising: administering to said mammal an effective amount of at least one active ingredient selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 11. The method of claim 10, wherein said at least one active ingredient comprises VN/124-1. Claim: 12. The method of claim 10, wherein said at least one active comprises two or more active ingredients selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 13. The method of claim 10, wherein the mammal is a human. Claim: 14. A method of suppressing tumor growth in a mammal having at least one prostate tumor, comprising: administering to said mammal an effective amount of at least one active ingredient selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 15. The method of claim 14, wherein said at least one active ingredient comprises VN/124-1. Claim: 16. The method of claim 14, wherein said at least one active comprises two or more active ingredients selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 17. The method of claim 14, wherein the mammal is a human. Claim: 18. The method of claim 14, wherein said tumor is an LAPC4 human prostate tumor. Claim: 19. The method of claim 14, further comprising castrating said mammal. Claim: 20. The method of claim 14, further comprising administering one or more anti-tumor agents to said mammal. Claim: 21. A method of treating a mammal having prostate cancer, comprising: administering to said mammal an effective amount of at least one active ingredient selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 22. The method of claim 21, wherein said at least one active ingredient comprises VN/124-1. Claim: 23. The method of claim 21, wherein said at least one active comprises two or more active ingredients selected from the group consisting of VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Claim: 24. The method of claim 21, wherein the mammal is a human. Claim: 25. The method of claim 21, further comprising administering one or more anti-cancer agents to said mammal. Claim: 26. (canceled) Claim: 27. (canceled) Claim: 28. (canceled) Claim: 29. (canceled) Current U.S. Class: 514/170 Current International Class: 61; 61

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ANDROGEN RECEPTOR INACTIVATION CONTRIBUTES TO ANTITUMOR EFFICACY OF CYP17 INHIBITORS IN PROSTATE CANCER