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Find Clinical Drug Pipeline Developments & Deals by Essa Pharma
EPI-7386 (masofaniten) is an investigational, highly-selective, oral, small molecule inhibitor of the N-terminal domain of the androgen receptor. It is currently being studied in Combination with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer.
ESSA will conduct a Phase 1 trial evaluating the safety, pharmacokinetics, drug-drug interactions, and preliminary anti-tumor activity of EPI-7386 when administered in combination with either apalutamide or abiraterone acetate plus prednisone in patients with prostate cancer.
EPI-7386 is an investigational, highly-selective, oral, small molecule inhibitor of the N-terminal domain of the androgen receptor. It is currently being studied for CRPC whose tumors have progressed on standard-of-care therapies.
EPI-7386 is an investigational, highly-selective, oral, small molecule inhibitor of the N-terminal domain of the androgen receptor. EPI-7386 is being studied in men with castration-resistant prostate cancer ("CRPC") whose tumors have progressed on standard-of-care therapies.
EPI-8207, an ANITAC, shows robust potency degrading AR, including AR splice variants and clinically relevant AR mutants that can potentially drive disease progression in patients with castration-resistant prostate cancer ("CRPC").
The initial data from 36 patients demonstrate that EPI-7386 was well-tolerated, exhibited a favorable pharmacokinetic profile, and demonstrated initial anti-tumor activity in a heavily pretreated group of patients.
The preclinical results for EPI-7386, demonstrated that ANITAC degraders utilize the ubiquitin proteasome system and can degrade many forms of AR including full length, mutant and splice variants which are often expressed in CRPC patients.
Results from the research indicated that EPI-7386 has an IC50 of 421 nM in LNCaP reporter assays, which is a range that is comparable to most LBD inhibitors; however, this agent differs from known agents in that its antitumor activity was maintained in CRPC models.
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