lunresertib

Lunresertib (RP-6306) is a first-in-class, orally bioavailable small molecule inhibitor of the protein kinase PKMYT1. Developed by Repare Therapeutics, it selectively targets and inhibits PKMYT1, a kinase involved in regulating the cell cycle through phosphorylation of CDK1. By blocking PKMYT1 activity, lunresertib disrupts cell division and preferentially kills tumor cells with specific genetic alterations such as CCNE1 amplification or loss of FBXW7 and PPP2R1A function. This mechanism exploits synthetic lethality in cancer cells with these genomic changes. Lunresertib is being investigated primarily for advanced solid tumors—including ovarian, uterine (especially those with TP53 mutations), breast (ER+/HER2-, triple-negative), lung, kidney, pancreatic, colon/rectal, head and neck/oral cancers—and has shown early efficacy both as monotherapy and in combination regimens in Phase 1 clinical trials[1][2][3][4][5][7].

Brand names

lunresertib

Other names

PKMYT1 inhibitorPKMYT-1 inhibitorPKMYT 1 inhibitor