Exhibit 99.1
Repare Therapeutics Unveils Two Programs Expected to Enter Clinical Trials in 2024: RP-1664, an Oral PLK4 Inhibitor, and RP-3467, an Oral Polq Inhibitor
RP-1664 demonstrated potent and selective inhibition of PLK4 and synthetic lethality in TRIM37-high
tumor cells in preclinical studies
RP-3467 demonstrated complete, sustained regressions
preclinically in combination with PARPi, and compelling anti-tumor activity in combination with radioligand therapy (RLT) and chemotherapy
Company expects to initiate clinical trials of RP-1664 in 1H 2024 and
RP-3467 in 2H 2024
Repare to host conference call and webcast today at 8:00 a.m. ET
CAMBRIDGE, Mass. & MONTREAL (BUSINESS WIRE) November 15, 2023 Repare Therapeutics Inc. (Repare or the
Company) (Nasdaq: RPTX), a leading clinical-stage precision oncology company, today disclosed polo-like kinase 4 (PLK4) as the target of its RP-1664 development program and reported comprehensive
preclinical data for both RP-1664 and the Companys Polq inhibitor, RP-3467.
RP-1664 is a potential first-in-class,
selective, oral PLK4 inhibitor that is synthetic lethal with TRIM37 amplification or overexpression in solid tumors. Tumors rely on PLK4 for survival in the presence of high levels of TRIM37. Preclinical studies demonstrate RP-1664 drives potent synthetic lethality in TRIM37-high tumor models, both in vitro and in vivo. Elevated TRIM37 is a feature found across a range of solid tumors and in nearly all high-grade
neuroblastomas.
RP-3467 is a potential
best-in-class inhibitor of DNA polymerase theta, or Polq. Polq is a synthetic
lethal target associated with homologous recombination deficiency (HRD) tumors, including those with BRCA1/2 mutations or other genomic alterations. Data suggest that RP-3467 works synergistically with
therapies that result in double stranded DNA breaks, such as PARP inhibition, radioligand therapy and multiple chemotherapies and antibody-drug conjugates (ADCs). Additionally, initial data suggest that
Polq inhibition may interfere with mechanisms central to the development of PARPi resistance.
We are
excited to announce the initial clinical approach for RP-1664 based on highly compelling preclinical data supporting its potential for treating TRIM37-high tumors, said Lloyd M. Segal, President and CEO
of Repare. We are also pleased to share preclinical data from our RP-3467 program supporting its significant potential across multiple high-value therapeutic opportunities. These programs represent our
third and fourth internally developed clinical candidates and provide further confirmation of Repares powerful discovery platform. We look forward to advancing both RP-1664 and RP-3467 into Phase 1 clinical trials in 2024.
RP-1664 Highlights
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RP-1664 is a highly potent, selective and bioavailable PLK4 inhibitor
that is synthetic lethal with TRIM37 gain of function. |