Repare's RP-6306 is a first-in-class small molecule being developed as a selective PKMYT1 inhibitor that preferentially kills tumor cells overexpressing CCNE1

Aug 11, 2022 · RP-6306 inhibits CCNE1-amplified tumor cell growth in several preclinical xenograft models. The first-in-class clinical candidate RP-6306 is currently being evaluated in Phase 1 clinical trials for treatment of various solid tumors.

Jun 6, 2024 · The FDA granted fast track designation to lunresertib (RP-6306) with camonsertib (RP-3500) for treating adult patients with platinum-resistant ovarian cancer harboring CCNE1 amplifications, FBXW7 mutations, or PPP2R1A mutations, aiming to expedite the development of …

Lunresertib (RP-6306) is a first-in-class inhibitor of the membrane-associated tyrosine- and threonine-specific Cdc2-inhibitory kinase (PKMYT1) that disrupts the G2/M checkpoint leading to premature mitosis and catastrophic DNA damage in the context of Cyclin E1 O/E

Ł Lunresertib (RP-6306) is a clinical stage, potent and selective oral inhibitor of PKMYT1, with single agent activity in CCNE1 -amp preclinical models Ł As CDK1 activity is also restricted by the activity of the ATR kinase through inhibition

The purpose of this study is to find the highest dose of the investigational drug RP-6306 that can be used in advanced solid tumors containing certain genetic changes and which have come back or continued to grow despite prior treatment.

It is currently in phase 1/2 clinical trials, both as monotherapy or in combination with camonsertib, an ATR inhibitor. [2] ^ Szychowski J, Papp R, Dietrich E, Liu B, Vallée F, Leclaire ME, et al. (August 2022). "Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306".

RP-6306 is a first-in-class highly potent and selective PKMYT1 inhibitor currently in clinical trials as a single agent (NCT04855656) and in combination with gemcitabine and irinotecan-based therapy (NCT05147350 and NCT05147272).

lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects.

RP-6306 inhibits CCNE1-amplified tumor cell growth in several preclinical xenograft models. The first-in-class clinical candidate RP-6306 is currently being evaluated in Phase 1 clinical trials for treatment of various solid tumors.