trc253

TRC253 is an orally bioavailable, high-affinity small molecule antagonist of the androgen receptor (AR), including both wild-type and certain mutant forms. It acts as a competitive inhibitor by binding to AR and preventing androgen-induced activation, thereby blocking AR nuclear translocation and DNA binding. This inhibits transcription of AR-responsive genes involved in prostate cancer cell proliferation. Developed initially by Janssen Pharmaceutica and later by TRACON Pharmaceuticals, its primary indication was for metastatic castration-resistant prostate cancer (mCRPC), particularly in patients with resistance to prior AR inhibitors or with specific AR mutations such as F877L. Clinical development reached phase II but was discontinued for prostate cancer[1][2][3][5][7].

Other names

2110426-27-05-(8-oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrileGNG9GQ9Y27GNG-9GQ9Y27GNG 9GQ9Y27