IP Library Granted Patent US 12,016,847
Granted Patent B2
US 12,016,847 · App. 17/653,717 · Granted Jun 25, 2024

Methods of treating prostate cancer

Inventors: Martina Malatesta (San Francisco, CA); Ellen Hope Filvaroff (San Francisco, CA)
Assignee: Bristol-Myers Squibb Company
A61K31/437A61P35/00
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Quick Facts
Patent No.
US 12,016,847
App. No.
17/653,717
Granted
Jun 25, 2024
Kind
B2
Abstract

The present application relates generally to methods for treating prostate cancer with substituted tricyclic derivative is 2-[3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-5-[(S)-(oxan-4-yl)(phenyl)methyl]-5H-pyrido[3,2-b]indol-7-yl]propan-2-ol as a bromodomain inhibitor, or the pharmaceutically acceptable salt thereof.

Claims (20)

1. A method of treating prostate cancer in a subject in need thereof comprising administering to the subject a therapeutically effective amount of Compound A having the structure,

or a pharmaceutically acceptable salt thereof, and wherein the prostate cancer is castration resistant prostate cancer (CPRC), neuroendocrine prostate cancer (NEPC), anti-androgen resistant prostate cancer, or any combination thereof.

2. The method of claim 1 , wherein the prostate cancer is metastatic.

3. The method of claim 1 , wherein the prostate cancer to be treated is in an advanced stage.

4. The method of claim 1 , wherein the prostate cancer to be treated has metastasized to regions of the subject's body other than the prostate gland.

5. The method of claim 1 , wherein the prostate cancer to be treated has re-occurred in the subject following a significant period of remission.

6. The method of claim 1 , wherein the prostate cancer is castration resistant prostate cancer (CPRC).

7. The method of claim 6 , wherein the castration resistant prostate cancer (CPRC) is an androgen receptor (AR) independent disease characterized by neuroendocrine phenotype with a low or absent AR expression.

8. The method of claim 1 , wherein the prostate cancer is neuroendocrine prostate cancer (NEPC).

9. The method of claim 1 , wherein the method results in substantially inducing cell cycle arrest of the prostate cancer.

10. The method of claim 9 , wherein “substantially” is defined as at least about 50% cell cycle arrest of the prostate cancer.

11. The method of claim 1 , wherein the method results in completely inducing cell cycle arrest of the prostate cancer.

12. The method of claim 1 , wherein the method induces apoptosis of androgen independent cancer cells.

13. The method of claim 12 , wherein the method results in inducing about 20% or more apoptosis of the androgen independent cancer cells.

14. The method of claim 1 , wherein:

the method results in from about 70% to about 99% reduction of cancer cell proliferation.

15. The method of claim 1 , wherein:

the method results in from about 40% to about 99% reduction of tumor size.

16. The method of claim 1 , wherein the compound, or a pharmaceutically acceptable salt thereof, is adapted for oral administration.

17. The method of claim 16 , wherein the compound, or a pharmaceutically acceptable salt thereof, is in the form of a tablet, pill, sachet, or capsule of hard of soft gelatin.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 6, 2022
From: MALATESTA, MARTINA; FILVAROFF, ELLEN HOPE
To: BRISTOL-MYERS SQUIBB COMPANY
Reel/Frame 059862/0580 →
Continuity (2)
Provisional Application 63160319 · Mar 12, 2021
Related Publication 20220296574A1 · Sep 22, 2022