Dr. David Parkinson reports
ESSA PHARMA PRESENTS THERAPEUTIC POTENTIAL OF EPI-7386 AT 32ND EORTC-NCI-AACR SYMPOSIUM
Essa Pharma Inc. has presented new preclinical data on Essa's clinical candidate, EPI-7386, at the 32nd EORTC-NCI-AACR annual symposium on molecular targets and cancer therapeutics (ENA).
In an oral poster presentation titled, "The preclinical characterization of the N-terminal domain androgen receptor inhibitor, EPI-7386, for the treatment of prostate cancer," was published on Oct. 24.
The studies highlight new information about EPI-7386, including:
-
In an in vitro cellular thermal shift assay (CETSA), EPI-7386 was shown to physically interact with the both the full-length and the splice variant (AR-V7) form of the androgen receptor (AR).
-
In an in vitro full-length AR-driven cellular model (LNCaP), RNAseq data were analyzed by pathway enrichment analysis. EPI-7386 demonstrates largely similar modulation of AR-regulated genes compared with enzalutamide, but with additional unique elements.
-
EPI-7386 exhibits superior activity to enzalutamide in the AR-V7-driven cellular models LNCaP95 and 22Rv1 by modulating AR-driven gene expression with or without the addition of an external androgen.
"Previously, we presented in vitro data demonstrating that EPI-7386 binds to the full-length androgen receptor and can inhibit the transcription of AR-regulated genes. These new data demonstrate that EPI-7386 can also physically interact with the splice variant form, AR-V7, of the androgen receptor and inhibit its activity. The importance of this interaction with AR-V7 is seen through the superior transcriptional inhibition of AR-regulated genes by EPI-7386 compared to enzalutamide in the AR-V7-driven cell models LNCaP95 and 22Rv1. Together, these data provide important new insights into mechanistic aspects related to the binding and utility of EPI-7386 against AR-V7 splice-variant driven prostate cancer models. The data further strengthen the rationale for studying EPI-7386 in men with prostate cancer resistant to current anti-androgens," said Dr. David R. Parkinson, president and chief executive officer.
About Essa Pharma Inc.
Essa is a clinical-stage pharmaceutical company focused on developing novel and proprietary therapies for the treatment of castration-resistant prostate cancer in patients whose disease is progressing despite treatment with current therapies. Essa's proprietary aniten compounds bind to the N-terminal domain of the androgen receptor, inhibiting AR-driven transcription and the AR signalling pathway in a unique manner which bypasses the drug resistance mechanisms associated with current anti-androgens. The company is currently conducting a phase 1 study of EPI-7386 in patients with metastatic castration-resistant prostate cancer (mCRPC), who are failing current standard-of-care therapies.
We seek Safe Harbor.
© 2024 Canjex Publishing Ltd. All rights reserved.