Lunresertib — Investigational Agent
Other · Phase 1 · Repare Therapeutics
Mechanism of Action
Lunresertib is a first-in-class, oral, selective inhibitor of PKMYT1 (membrane-associated tyrosine/threonine 1 kinase), which, like WEE1, inhibits CDK1 to restrain mitotic entry. PKMYT1 inhibition is synthetically lethal in tumors with CCNE1 amplification or FBXW7/PPP2R1A mutations, where high Cyclin E activity creates dependence on PKMYT1 to prevent premature, lethal mitosis. Blocking PKMYT1 in these genetically defined tumors triggers unscheduled CDK1 activation, mitotic catastrophe, and apoptosis. Lunresertib is being explored as monotherapy and in combinations that exploit replication…
Investigational Indications
- CCNE1-amplified ovarian cancer
- CCNE1-amplified endometrial cancer
- FBXW7- or PPP2R1A-mutant gynecologic tumors
- Molecularly selected solid tumors