TRACON Pharmaceuticals Retains Global Rights to TRC253 Following Completion of a Phase 1/2 Trial
TRACON has initiated an out-licensing process to identify a corporate partner to develop and commercialize TRC253 in
“While TRC253 is as active as Xtandi in prostate cancer cell lines and in patient-derived xenograft models, we determined during clinical development that the F877L androgen receptor mutation TRC253 was designed to treat was far less common than predicted, and the product candidate was not highly active in prostate cancer patients with acquired resistance to Xtandi or Erleada. Given the preclinical data that suggest TRC253 may be as active as Xtandi in an earlier line setting, we believe TRC253 can be developed and commercialized successfully in
In a Phase 1/2 trial, TRC253 was dosed to 72 patients with metastatic castrate resistant prostate cancer who had progressed on prior treatment that included the wild type AR inhibitor Xtandi or Erleada, including patients with F877L androgen receptor mutation. The recommended Phase 2 dose of 280 mg orally per day was well tolerated with grade 1 QTc prolongation being the most common adverse event. The PSA response rate in 63 patients evaluable for efficacy, including patients with the AR F877L mutation, patients with other point mutations of the AR or patients with another basis for resistance to Xtandi or Erleada, was 8%. Seventeen of 63 patients (27%) had stable disease for more than five months (and for as long as 12 months). TRC253 is as active as Xtandi in preclinical models of prostate cancer (Bush TL et al, Cancer Res
About TRC253 (formerly JNJ-63576253)
TRC253 is a novel, orally bioavailable small molecule discovered and developed by Janssen that is a potent, high affinity competitive inhibitor of the androgen receptor (AR). TRC253 is also a pan-inhibitor of multiple AR mutations, including the F877L mutation. The AR F877L mutation results in an alteration in the ligand binding domain that confers resistance to current AR inhibitors.
Activation of the AR is crucial for the growth of prostate cancer at all stages of the disease. Therapies targeting the AR have demonstrated clinical efficacy by extending time to disease progression, and in some cases, the survival of patients with metastatic castration-resistant prostate cancer. However, resistance to these agents is often observed and several molecular mechanisms of resistance have been identified, including amplification, overexpression or mutation of the AR.
TRC253 is intended to address resistance mechanisms to current AR inhibitors by specifically targeting mutations in the AR ligand binding domain. TRC253 also potently inhibits signalling through the wild type AR. These susceptible AR mutations have been identified using circulating tumor DNA assays, potentially allowing for selected patient biomarker-directed therapy. TRACON completed initial Phase 1 and Phase 2 clinical trials for the treatment of men with prostate cancer, following the completion of IND-enabling studies by Janssen.
TRACON develops targeted therapies for cancer utilizing a capital efficient product development platform. The Company’s clinical-stage pipeline includes: Envafolimab, a subcutaneous PD-L1 single-domain antibody being developed for the treatment of sarcoma; TRC253, a small molecule drug being developed of the treatment of prostate cancer; TRC102, a small molecule drug being developed for the treatment of lung cancer; and TJ004309, a CD73 antibody being developed for the treatment of advanced solid tumors. TRACON is actively seeking additional corporate partnerships whereby it leads
Statements made in this press release regarding matters that are not historical facts are “forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995. Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward‐looking statements. Such statements include, but are not limited to, statements regarding TRACON's plans to further develop its product candidates, including TRC253, plans to seek a partner for the development and commercialization of TRC253 in
Chief Business Officer
Source: TRACON Pharmaceuticals, Inc.