On May 4, 2019 ESSA Pharma Inc. (Nasdaq: EPIX; TSX-V: EPI), a pharmaceutical company focused on developing novel therapies for the treatment of prostate cancer, reported new preclinical data on ESSA’s lead Investigational New Drug ("IND") candidate at the 2019 American Urological Association ("AUA") Annual Meeting (Press release, ESSA, MAY 4, 2019, View Source [SID1234535723]).
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In an oral poster presentation, "A New Generation of N-terminal Domain Androgen Receptor Inhibitors in Castration-Resistant Prostate Cancer Models", a deeper preclinical characterization of EPI-7386 was presented. The studies demonstrate that, pre-clinically, EPI-7386:
Displays similar in vitro IC50 potency compared to the ‘lutamide class of antiandrogens in an in vitro androgen receptor (AR) inhibition assay.
Shows in vitro activity in several enzalutamide-resistant prostate cancer cell models in which enzalutamide is resistant.
Exhibits a favorable metabolic profile across three preclinical animal species, which suggests that EPI-7386 will have high exposure and a long half-life in humans.
Provides similar antitumor activity to enzalutamide in the enzalutamide-sensitive LNCaP prostate cancer xenograft model.
Provides superior antitumor activity to enzalutamide, as a single agent or in combination with enzalutamide, in the enzalutamide-resistant VCaP prostate cancer xenograft model.
AR inhibition with both an N-terminal domain inhibitor (EPI-7386) and a ligand binding domain inhibitor (enzalutamide), induces deeper and more consistent anti-tumor responses in the enzalutamide-resistant VCaP xenograft model.
"The variety of in vitro and in vivo studies examining both antiandrogen sensitive models and antiandrogen-resistant xenograft mouse models show a favorable preclinical profile of EPI-7386. From this and an aggregate of other preclinical data, we nominated EPI-7386 as the IND candidate to be used in the clinic in mCRPC patients failing current antiandrogen therapy. EPI-7386 represents a novel approach to targeting the androgen receptor, one of the most validated targets in oncology," said Dr. David R. Parkinson, President & Chief Executive Officer. "We look forward to providing further details of the preclinical profile of EPI-7386 later in the year as we move close to our anticipated IND filing in the first quarter of 2020."