molecules of the month


oral PKMYT1 inhibitor

three Ph. I studies currently ongoing

initial screen of 560 known kinase inhibitors

J. Med. Chem.

Repare Therapeutics, Inc., Ville St- Laurent, CA

RP-6306 Chemical Structure oral PKMYT1 inhibitor - Repare Therapeutics, Inc., Ville St- Laurent, CA
5 mins read

Context. RP-6306 is an oral protein kinase, membrane-associated tyrosine/threonine 1 (PKMYT1) Inhibitor being developed for various solid tumors. PKMYT1, together with WEE1, make up the WEE family of serine/threonine kinases, which have been implicated in the progression of several cancers, especially solid tumors. At least 4 WEE1 inhibitors have entered clinical development; notable among them is Zentalis’ ZN-c3, which we previously featured, and AstraZeneca’s adavosertib (AZD1775; formerly MK1775), which is the leading candidate and has been evaluated in >60 trials. AstraZeneca recently pulled the plug on adavosertib, likely due to bone marrow and gut-related toxicities, raising questions on whether the other WEE1 inhibitors may meet a similar fate. The potential first-in-class agent RP-6306 was found in preclinical studies to be…

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