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CAS Insight

molecules of the month

RP-3500

ATR kinase inhibitor

phase I/IIa candidate for advanced solid tumors

from lipid-kinase inhibitor scaffold

Molecular Cancer Therapeutics

Repare Therapeutics, Saint-Laurent, CAN

Chemical structure of molecule RP-3500
1 min read

RP-3500 is an oral ATR kinase inhibitor and Ph. II clinical candidate for advanced solid tumors with ATRi-sensitizing mutations, alone or in combination with talazoparib (PARPi) or gemcitabine. Reviewer Anthony Vaganos says, “An ATR molecule (ceralasertib) is in clinical trials but studies in two different tumors in combination with PARP inhibitors were recently terminated or recommended for closure (see DUETTE, NCT04239014), so a key question will be did Repare design this molecule for combination and if so, will it be able to overcome ceralasertib’s failings? Or was this drug designed more for monotherapy? Ceralasertib does have a broad development program so the story definitely isn’t over yet.” It is possible that different subsets of tumors may respond better to ATR…


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