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Knowledge present PKMYT1 inhibition is a promising therapeutic goal in CCNE1-amplified cancers
RP-6306, a first-in-class, oral PKMYT1 inhibitor, is at present being evaluated in Section 1 scientific trials
CAMBRIDGE, Mass. & MONTREAL — Repare Therapeutics Inc. (“Repare” or the “Firm”) (Nasdaq: RPTX), a number one clinical-stage precision oncology firm, at present introduced that preclinical information demonstrating inhibition of CCNE1-amplified tumor progress in vivo by selective inhibition of PKMYT1 utilizing RP-6306, a first-in-class small molecule candidate focusing on PKMYT1, have been revealed in Nature. SNIPRx®, Repare’s proprietary, genome-wide, CRISPR-based screening strategy, was used to uncover CCNE1 amplification as artificial deadly to PKMYT1 inhibition.
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The article, entitled “CCNE1 amplification is artificial deadly with PKMYT1 kinase inhibition” is accessible at www.nature.com.
“RP-6306 is a first-in-class and extremely selective PKMYT1 inhibitor, and these preclinical information present its capability to focus on CCNE1-amplfied tumors and profoundly inhibit tumor progress,” mentioned Michael Zinda, PhD, EVP and Chief Scientific Officer of Repare. “We’re excited as that is one other instance of the facility of genetic interplay screens to uncover new oncology drug targets, on this case in a mobile mannequin of CCNE1 amplification. This led to the identification of a beforehand uncharacterized vulnerability to PKMYT1 inhibition that spurred the event of RP-6306 by Repare Therapeutics.”
“We’re thrilled that this work demonstrates each the facility of our CRISPR-based SNIPRx platform to uncover novel artificial deadly targets and Repare’s capability to prosecute these targets leading to first-in-class small molecule therapeutics,” mentioned Maria Koehler, MD, PhD, EVP and Chief Medical Officer of Repare. “It’s unusual {that a} new and validated goal is revealed in a prime tier journal concurrent with a launched scientific trial for a candidate drug on that concentrate on, and this speaks volumes concerning the progressive capability of Repare and its collaborators.”
Section 1 scientific trials are at present evaluating RP-6306 as a monotherapy in addition to together with gemcitabine for the remedy of molecularly chosen superior stable tumors. The Firm just lately initiated an extra Section 1 MINOTAUR scientific trial of RP-6306 together with FOLFIRI additionally for the remedy of molecularly chosen superior stable tumors.
This work is the results of a long-standing collaboration between Repare Therapeutics and the laboratory of Daniel Durocher, PhD, a Senior Investigator on the Lunenfeld-Tanenbaum Analysis Institute, a part of Sinai Well being, in Toronto, Canada Dr. Durocher can also be a Professor within the Division of Molecular Genetics on the College of Toronto. Work on CCNE1 within the Durocher laboratory was led by David Gallo, PhD, now a Senior Scientist at Repare and was financially supported by Repare Therapeutics and the Canadian Institutes of Well being Analysis (CIHR).
About Repare Therapeutics’ SNIPRx® Platform
Repare’s SNIPRx® platform is a genome-wide CRISPR-based screening strategy that makes use of proprietary isogenic cell traces to establish novel and recognized artificial deadly gene pairs and the corresponding sufferers who’re probably to learn from the Firm’s therapies based mostly on the genetic profile of their tumors. Repare’s platform allows the event of precision therapeutics in sufferers whose tumors comprise a number of genomic alterations recognized by SNIPRx® screening, with a view to selectively goal these tumors in sufferers probably to realize scientific profit from ensuing product candidates.
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About Repare Therapeutics, Inc.
Repare Therapeutics is a number one clinical-stage precision oncology firm enabled by its proprietary artificial lethality strategy to the invention and growth of novel therapeutics. The Firm makes use of its genome-wide, CRISPR-enabled SNIPRx® platform to systematically uncover and develop extremely focused most cancers therapies targeted on genomic instability, together with DNA harm restore. The Firm’s pipeline consists of its lead product candidate RP-3500, a possible main ATR inhibitor at present in Section 1/2 scientific growth, its second scientific candidate, RP-6306, a PKMYT1 inhibitor at present in Section 1 scientific growth, a Polθ inhibitor program, in addition to eight different early-stage, pre-clinical applications. For extra info, please go to reparerx.com.
SNIPRx® is a registered trademark of Repare Therapeutics Inc.
Ahead-Wanting Statements
This press launch incorporates “forward-looking statements” throughout the that means of the Non-public Securities Litigation Reform Act of 1995. All statements on this press launch aside from statements of historic details are “forward-looking statements. These statements could also be recognized by phrases corresponding to “goals,” “anticipates,” “believes,” “might,” “estimates,” “expects,” “forecasts,” “purpose,” “intends,” “might,” “plans,” “doable,” “potential,” “seeks,” “will” and variations of those phrases or related expressions which are meant to establish forward-looking statements, though not all forward-looking statements comprise these phrases. Ahead-looking statements on this press launch embrace, however usually are not restricted to, statements concerning the scientific growth of the Firm’s pipeline and its analysis and growth applications, and the flexibility of RP-6306 to focus on CCNE1-amplfied tumors and inhibit tumor progress. These forward-looking statements are based mostly on the Firm’s expectations and assumptions as of the date of this press launch. Every of those forward-looking statements entails dangers and uncertainties that would trigger the Firm’s scientific growth applications, future outcomes or efficiency to vary materially from these expressed or implied by the forward-looking statements. Many elements might trigger variations between present expectations and precise outcomes, together with the impacts of the COVID-19 pandemic on the Firm’s enterprise, scientific trials and monetary place, surprising security or efficacy information noticed throughout preclinical research or scientific trials, scientific trial website activation or enrollment charges which are decrease than anticipated, modifications in anticipated or current competitors, modifications within the regulatory surroundings, the uncertainties and timing of the regulatory approval course of, and surprising litigation or different disputes. Different elements which will trigger the Firm’s precise outcomes to vary from these expressed or implied within the forward-looking statements on this press launch are recognized within the part titled “Danger Elements” within the Firm’s Annual Report on Type 10-Okay for the 12 months ended December 31, 2021 filed with the Securities and Change Fee (“SEC”) and the Québec Autorité des Marchés Financiers (“AMF”) on March 1, 2022, and its different paperwork subsequently filed with or furnished to the SEC and AMF. The Firm expressly disclaims any obligation to replace any forward-looking statements contained herein, whether or not on account of any new info, future occasions, modified circumstances or in any other case, besides as in any other case required by regulation.
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References and hyperlinks to web sites have been supplied for comfort, and the knowledge contained on any such web site just isn’t part of, or included by reference into, this press launch. Repare just isn’t chargeable for the contents of any third-party web site.
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Contacts
Repare:
Steve Forte
Chief Monetary Officer
Repare Therapeutics Inc.
information@reparerx.com
Buyers:
Kimberly Minarovich
Argot Companions
repare@argotpartners.com
Media:
David Rosen
Argot Companions
david.rosen@argotpartners.com
212-600-1902
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