Showing posts with label androgen receptor antagonist. Show all posts
Showing posts with label androgen receptor antagonist. Show all posts

Wednesday, May 1, 2013

Androgen receptors found to be a potential target in breast cancer

In continuation of my update on Enzalutamide


We know that, The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone  in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor...

Estrogen and progesterone receptors, and the gene HER2 - these are the big three markers and/or targets in breast cancer. Evidence presented at the AACR Annual Meeting 2013 adds a fourth: androgen receptors.

"This is a continuing line of work with all evidence pointing toward the addition of the androgen receptor as potential target and useful marker in all of the major subtypes of breast cancer," says Jennifer Richer, PhD, investigator at the University of Colorado Cancer Center and co-director of the CU Cancer Center Tissue Processing and Procurement Core.

 The finding of androgen receptors (AR) as a potential target in breast cancer is especially important in light of its prevalence in breast cancers that don't express other hormone receptor targets or have developed resistance to treatments that target estrogen dependence. Overall, approximately 77 percent of breast cancers are positive for AR, including 88 percent of cancers that are estrogen receptor positive, 59 percent of those that are HER2 positive, and 20-32 percent of triple negative breast cancers.....

Friday, October 12, 2012

FDA approves Enzalutamide (XTANDI Capsules)



Enzalutamide (marketed as Xtandi and formerly known as MDV3100) is an androgen receptor antagonist drug developed by the pharmaceutical company Medivation for the treatment of castration-resistant prostate cancer  currently in phase 3 clinical trials. Medivation has reported up to an 89% decrease in prostate specific antigen serum levels after a month of taking the medicine. Early preclinical studies also suggest that enzalutamide inhibits breast cancer cell growth. In August of 2012, the U.S. Food and Drug Administration approved enzalutamide (see structure) for the treatment of castration-resistant prostate cancer......
 
Approved Drugs > Enzalutamide (XTANDI Capsules)