adavosertib + 5-fluorouracil

**Adavosertib + 5-fluorouracil** is a combination of two pharmaceutical agents: adavosertib, a selective small molecule inhibitor of WEE1 kinase, and 5-fluorouracil, a pyrimidine analogue antimetabolite. Adavosertib targets WEE1 kinase, leading to abrogation of the G2/M cell cycle checkpoint, which forces cells harboring DNA damage into mitosis, thereby promoting cell death, especially in p53-mutant cancer cells. 5-fluorouracil inhibits thymidylate synthase and incorporates into RNA and DNA, disrupting synthesis and function, resulting in cytotoxicity. The combination is being investigated for its synergistic anti-tumor activity in cancers with p53 mutations, notably pancreatic ductal adenocarcinoma and colorectal cancer. Preclinical studies show the combination leads to increased double-stranded DNA breaks, cell cycle arrest, caspase-dependent apoptosis, and reduced proliferation relative to either agent alone[1][2][3].

Other names

adavosertib + 5-FUAZD1775 + 5-fluorouracilMK-1775 + 5-fluorouracil