IP Library Granted Patent US 10,987,334
Granted Patent B2
US 10,987,334 · App. 16/051,042 · Granted Apr 27, 2021

Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs)

Inventors: Ramesh Narayanan (Cordova, TN); Thamarai Ponnusamy (Memphis, TN)
Assignee: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
A61K31/277A61K31/167A61K31/404A61K31/4704A61P35/00A61K9/0014A61K9/0019A61K9/0024A61K9/0053A61K9/02A61K9/06A61K9/08A61K9/10A61K9/107A61K9/1605A61K9/4866
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Quick Facts
Patent No.
US 10,987,334
App. No.
16/051,042
Granted
Apr 27, 2021
Kind
B2
Abstract

This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4/6 (CDK 4/6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), abemaciclib (Vorzenio)), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; and/or treating a subject suffering from ER mutant expressing breast cancer, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Claims (15)

1. A method of treating a subject suffering from ER mutant expressing breast cancer, comprising a step of administering to said subject a selective androgen receptor modulator (SARM) compound represented by a structure of formula II:

wherein

X is O;

G is O;

T is OH;

R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, CH 2 F, CHF 2 , CF 3 , CF 2 CF 3 , aryl, phenyl, halogen, alkenyl or OH;

R 1 is CH 3 ;

Z is NO 2 or CN;

Y is CF 3 , F, Br, Cl, I, or CN;

Q is CN, alkyl, halogen, NHCOR, NHCOOR, CONHR, NHCSCH 3 , NHCSCF 3 , or NHCSR;

wherein said ER mutant expressing breast cancer is Y537S mutation expressing breast cancer, and wherein said treating does not include preventing.

2. The method of claim 1 , comprising administering an optical isomer, a racemic mixture, a metabolite, a pharmaceutically acceptable salt, a pharmaceutical product, a hydrate, an N-oxide, or a crystal of said selective androgen receptor modulator, or any combination thereof.

3. The method of claim 1 , wherein said administering comprises intravenously, intraarterially, or intramuscularly injecting to said subject said pharmaceutical product in liquid form; subcutaneously implanting in said subject a pellet containing said pharmaceutical product; orally administering to said subject said pharmaceutical product in a liquid or solid form; or topically applying to the skin surface of said subject said pharmaceutical product.

4. The method of claim 2 , wherein said pharmaceutical product is a pellet, a tablet, a capsule, a solution, a suspension, an emulsion, an elixir, a gel, a cream, a suppository or a parenteral formulation.

5. The method of claim 1 , wherein said SARM compound is represented by a structure of Formula:

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 9, 2020
From: ONCTERNAL THERAPEUTICS, INC.
To: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
Reel/Frame 054318/0958 →
CHANGE OF NAME Recorded Jul 4, 2019
From: GTX, INC.
To: ONCTERNAL THERAPEUTICS, INC
Reel/Frame 049679/0298 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 24, 2018
From: NARAYANAN, RAMESH; PONNUSAMY, THAMARAI
To: GTX, INC.
Reel/Frame 046955/0694 →
Continuity (9)
Continuation In Part 15371104 · Dec 6, 2016
Continuation In Part 15075373 · Mar 21, 2016
Continuation In Part 14798208 · Jul 13, 2015
Continuation In Part 14293632 · Jun 2, 2014
Continuation In Part 13953492 · Jul 29, 2013
Continuation In Part 13789005 · Mar 7, 2013
Provisional Application 61726274 · Nov 14, 2012
Provisional Application 61671366 · Jul 13, 2012
Related Publication 20190111010A1 · Apr 18, 2019