On May 3, 2021 Repare Therapeutics Inc. ("Repare" or the "Company") (Nasdaq: RPTX), a leading clinical-stage precision oncology company enabled by its proprietary synthetic lethality (SL) approach to the discovery and development of novel therapeutics, reported the first patient has been dosed in the Company’s Phase 1 clinical trial of RP-6306, a first-in-class small molecule product candidate targeting PKMYT1, which is a novel target that Repare discovered to be synthetic lethal with CCNE1 amplification and other genomic mutations to treat CCNE1-amplified, FBXW7-altered and other PKMYT1 inhibitor-sensitive cancers (Press release, Repare Therapeutics, MAY 3, 2021, View Source [SID1234579022]).

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"The dosing of the first patient in this RP-6306 trial marks a key milestone in Repare’s development of targeted cancer therapeutics. We are pleased to have initiated this trial six months ahead of what we projected at our IPO launch last June," said Lloyd M. Segal, President and Chief Executive Officer of Repare. "Patients with tumors carrying CCNE1, FBXW7 and certain other genetic alterations we have identified as sensitive to PKMYT1 inhibition have few treatment options available, and the incidence of these cancers is rising. This Phase 1 trial will assess the safety and tolerability of RP-6306, as well as dosing schedule, to inform Repare’s planned Phase 2 program."

The Phase 1 multi-center clinical trial is expected to enroll approximately 70 patients with recurrent tumors characterized by specific genomic alterations predicted by Repare’s SNIPRx platform to render sensitivity to RP-6306. The primary goal of the Phase 1 clinical trial is to assess preliminary safety and tolerability in patients and to establish the recommended Phase 2 dose and dosing schedule for RP-6306 for evaluation in further trials. Subject to completion and review of the Phase 1 clinical trial, the Company expects to advance RP-6306, both as monotherapy and in combination with chemotherapies and other treatment modalities, into proof-of-concept studies in 2022, targeting a variety of patient populations, including those with tumors with CCNE1 amplification, FBXW7 loss or other alterations identified through Repare’s proprietary STEP2 screens.

About RP-6306

RP-6306 is a first-in-class, selective, orally available inhibitor of PKMYT1 that was discovered and developed entirely in-house by Repare. Through Repare’s SNIPRx screen campaign for targets that are SL with CCNE1 amplification, the Company identified and validated this novel SL gene that has the characteristics of a therapeutic target. Repare has developed novel and selective inhibitors against PKMYT1, which demonstrated compelling pre-clinical anti-tumor activity alone and in combination with certain anticancer agents, and subsequently announced the advancement of a clinical candidate to this potential, first-in-class program.