EPI-8207 / ESSA Pharma - LARVOL DELTA

ESSA Pharma Presents Preclinical Data for its First Generation Androgen Receptor N-Terminal Domain Degrader at the 34th EORTC-NCI-AACR Symposium (PRNewswire) - "ESSA Pharma...announced the presentation of preclinical data for its lead first generation androgen receptor ('AR') ANITen bAsed Chimera ('ANITAC'™) N-terminal domain ('NTD') degrader in a poster session at the 34th EORTC-NCI-AACR Annual Symposium on Molecular Targets and Cancer Therapeutics in Barcelona, Spain. The preclinical data demonstrate that 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'). In addition, EPI-8207 exhibits high potency in inhibiting AR-dependent transcription."

Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Updated Results from the Phase 1/2 Study of ESSA's Lead Candidate EPI-7386 in Combination with Enzalutamide Highlighted at the 29th Annual Prostate Cancer Foundation Scientific Retreat (PRNewswire) - "Two additional posters will be presented at the conference highlighting updated results from the first-in-human Phase 1a dose escalation study of EPI-7386 as a monotherapy in mCRPC patients failing current second-generation antiandrogens and preclinical data on ESSA's first-in-class N-terminal domain androgen receptor protein degrader ('ANITAC'™) program."

P1 data • Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Androgen receptor (AR) N-terminal domain degraders can degrade AR full length and AR splice variants in CRPC preclinical models (AACR 2022) - "However, we recently demonstrated that EPI-7386, an AR NTD small molecule inhibitor, inhibits AR activity by binding to Tau5 region of the NTD. In summary, we report preclinical data on the first generation of ANITAC molecules, that can be orally bioavailable and show activity against forms of AR expressed in late stage CRPC patients."

Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AR

ESSA Pharma Announces the Presentation of Preclinical Data for its First Generation of Androgen Receptor N-Terminal Domain Degraders (PRNewswire) - "ESSA Pharma...announced the presentation of preclinical data for its first generation of androgen receptor (AR) ANITen bAsed Chimera (ANITAC) N-terminal domain (NTD) degraders at the 2022 American Association for Cancer Research (AACR) Annual Meeting....Orally bioavailable ANITAC degraders can eliminate full length, mutant and splice variant forms of AR that are expressed in castration-resistant prostate cancer (CRPC) patients. ANITAC degraders inhibit AR-dependent transcription and reduce viability of AR-dependent prostate cancer cells."

Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • Urothelial Cancer