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HOUSTON and VANCOUVER, March 28, 2019 / PRNewswire / – ESSA Pharma Inc. (TSX-V: EPI, Nasdaq: EPIX), a pharmaceutical company specializing in the development of novel therapies for the treatment of prostate cancer, announced today the appointment of EPI- 7386 as a leading clinical candidate for the treatment of metastatic castration-resistant prostate cancer ("mCRPC"). EPI-7386 is a new drug candidate that inhibits the N-terminal domain of the androgen receptor. Thanks to this new mechanism of action, the EPI-7386 displays an activity in vitro in many models of prostate cancer, including models in which current antiandrogens are inactive. Compared to the first generation compound of ESSA, ralanitene acetate, EPI-7386 is significantly more potent, metabolically stable and more effective in preclinical studies. In addition, EPI-7386 demonstrated a favorable tolerability profile in all animal studies conducted on the compound conducted to date. Studies favorable to the IND are currently underway and ESSA plans to launch clinical studies with EPI-7386 in the first quarter of 2020.
As recently presented at the symposium on Genitourinary cancers 2019, EPI-7386 demonstrates in vitro cellular power against the androgen receptor in a range similar to the main antiandrogens, bicalutamide and enzalutamide. Importantly, the EPI-7386 shows activity in many in vitro Antiandrogen resistance patterns driven by the AR-V7 splice variant of the androgen receptor while enzalutamide is inactive. In addition, EPI-7386 is metabolically stable in hepatic microsomal and hepatocyte preparations and exhibits a favorable pharmacokinetic profile in mice, exhibiting significant exposure and a long half-life. Finally, EPI-7386 (60 mg / kg) exhibited activity comparable to that of enzalutamide (30 mg / kg) in a mouse model of LNCaP xenograft, prostate cancer, in which the exposure from the mouse to enzalutamide was twice as high as the clinical exposure to enzalutamide in humans.
"We are delighted to announce the appointment of EPI-7386 as the lead clinical candidate for the treatment of mCRPC," he said. David Parkinson, President and CEO of ESSA. "EPI-7386 represents a new approach to targeting the androgen receptor, one of the most validated targets in oncology, and we look forward to bringing this new drug candidate to patients with mCRPC who have not yet seen it. Another treatment option. "
About ESSA Pharma Inc.
ESSA is a pharmaceutical company specializing in the development of innovative and proprietary therapies for the treatment of castration-resistant prostate cancer ("CPRC") in patients whose disease is evolving despite current treatments. ESSA believes that its patented compounds can significantly lengthen the time interval in which CRPC patients can benefit from hormone-based therapies by disrupting the androgen receptor ("AR") signaling pathway at the origin of prostate cancer growth and preventing the transcription activity of the latter. by selectively binding to the N-terminal domain ("NTD") of the AR. Functional MTN is essential for the transactivation of RA. In preclinical studies, blockage of neglected tropical diseases has demonstrated the ability to overcome the known CRC-dependent mechanisms of CRC. ESSA was founded in 2009.
Exclusive ESSA compounds, otherwise known as anitene compounds, bind to the N-terminal domain of the androgen receptor ("AR").
About prostate cancer
Prostate cancer is the second most frequently diagnosed cancer in men and the fifth leading cause of cancer death among men worldwide (Globocan, 2018). Adenocarcinoma of the prostate depends on the androgen for tumor progression and its action of depletion or blockage of androgen is one of the pillars of hormone therapy since more than six decades. Although tumors are often initially sensitive to medical or surgical treatments that reduce testosterone levels, the progression of the disease despite castrated testosterone levels generally represents a transition to the lethal variant of the disease, metastatic mCRPC, and most patients the disease. The treatment of patients with CPRCm has evolved rapidly over the last five years. Despite these advances, additional treatment options are needed to improve clinical outcomes in patients, particularly those who fail existing therapies, including abiraterone or enzalutamide, or those with counter-attacks. indications to these drugs. Over time, patients with mCRPC typically have ongoing disease progression, worsening pain, significant morbidity, and limited survival rates. In in vitro and in vivo animal studies, the new ESSA approach to blocking the androgen pathway has proven effective in blocking tumor growth when current treatments are no longer effective.
Forward-Looking Statement Disclaimer
This news release contains certain information which, in its current form, constitutes "forward-looking information" within the meaning of the Securities Industry Litigation Reform Act, 1995 and / or applicable Canadian securities legislation. Forward-looking information involves statements about future events and often discusses expected business and financial performance, including terms such as "anticipating", "anticipating" and "believing", as well as statements that an action or an event is "expected" , "should" or "will" be taken or will occur, or other similar expressions and will include, but not be limited to, statements regarding the preclinical characteristics and the potential performance of the EPI-7386 drug candidate, including activity, metabolic stability, efficacy, tolerability, exposure and duration of half-life, expected schedule for EPI-7386 clinical trials, and misconceptions regarding patented compounds ESSA significantly lengthen the time interval during which patients suffering from CPRC can benefit from hormone treatments.
Forward-looking statements and information are subject to a variety of known and unknown risks and uncertainties, many of which are beyond the ability of ESSA to control or predict, and which could result in a material difference between ESSA's results, performance or achievements. those expressed or lost. implied by that. These statements reflect the current views of ESSA regarding future events. They are subject to risks and uncertainties and are necessarily based on a number of estimates and badumptions which, while considered reasonable by ESSA as of the date of such statements, are inherently subject to certain badumptions and badumptions. scientific, commercial, economic, competitive, political and social uncertainties and uncertainties; In making forward-looking statements, ESSA may make various material badumptions, including (i) the accuracy of its financial projections; (ii) obtain positive results from clinical trials; (iii) obtain the necessary regulatory approvals; and (iv) the general conditions of business, the market and the economy.
The forward-looking information is developed based on badumptions about the risks, uncertainties and other factors described herein and in the annual report of ESSA on Form 20-F dated December 13, 2018 under "Risk Factors", a copy of which is available on ESSA's profile on SEDAR's website at www.sedar.com or on ESSA's profile on EDGAR at the address www.sec.gov, and as stated from time to time on ESSA's SEDAR and EDGAR profiles. Forward-looking statements are made based on management's beliefs, beliefs and beliefs as of the date on which they are made and ESSA badumes no obligation to update forward-looking statements if such opinions, estimates and opinions or other circumstances were changing except to the extent required. by applicable Canadian and United States securities laws. Readers are cautioned not to place undue reliance on forward-looking statements.
Neither the TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSX Venture Exchange) accepts any responsibility for the adequacy or accuracy of this document. communicated.
SOURCE ESSA Pharma Inc
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