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XL495: PKMYT1 Inhibitor

XL495 is a novel, orally bioavailable, and potent small molecule inhibitor of protein kinase membrane-associated tyrosine/threonine 1 (PKMYT1) that was discovered and is being developed by Exelixis.
Molecular structure shown is an artistic rendering.
PKMYT1 plays a crucial role in regulating the cell cycle and is involved in signaling pathways related to DNA damage repair. Inhibition of PKMYT1 has been shown in mouse xenograft models to be synthetically lethal in tumors with genomic alteration or when combined with cytotoxic agents that cause or enhance replication stress.
Phase 1 dose-escalation, dose-finding, and expansion study of XL495 alone and combination in locally advanced or metastatic solid tumors.
Cohort Expansions
For more information, visit
clinicaltrials.gov/study/NCT06630247
This website includes information on investigational uses of compounds that have not been approved by the U.S. Food and Drug Administration (FDA). Safety and efficacy of investigational compounds and/or investigational uses of approved products have not been established. The information presented should not be construed as a recommendation for use.
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