prexasertib + fluorouracil

A combination of **prexasertib**, a selective small molecule inhibitor of checkpoint kinase 1 (**CHK1**), and **fluorouracil** (also known as 5-fluorouracil, 5-FU), a pyrimidine analog and antimetabolite chemotherapeutic. **Prexasertib** disrupts DNA damage checkpoint signaling and blocks cell cycle arrest in response to DNA damage, amplifying DNA damage and inducing cell death, especially in cancer cells with defective p53 pathway. **Fluorouracil** is incorporated into RNA and DNA, disrupting synthesis and function, and also inhibits thymidylate synthase, further impairing DNA synthesis. This combination is being explored to potentiate anticancer effects in advanced or metastatic solid tumors, and proof-of-concept for safety and preliminary efficacy was established in a Phase 1b trial. The primary indication investigated to date is advanced/metastatic cancer, with specific clinical trials in solid tumors[1][3].

Other names

prexasertib + 5-fluorouracilprexasertib + fluorouracil