simmitecan + 5-fluorouracil + leucovorin calcium

A combination regimen consisting of the small molecule **simmitecan** (a camptothecin analog and prodrug), **5-fluorouracil** (5-FU, a pyrimidine analog antimetabolite), and **leucovorin calcium** (a reduced folate/folic acid analog) that is being investigated primarily for the treatment of **advanced solid tumors**, especially metastatic colorectal cancer. - **Simmitecan** acts as a **topoisomerase I inhibitor**, similar to irinotecan but with improved anti-tumor potency in preclinical models. It is a prodrug that is converted to the active metabolite chimmitecan. - **5-fluorouracil** interferes with DNA synthesis by inhibiting thymidylate synthase. - **Leucovorin calcium** stabilizes the binding of 5-FU's active metabolite (5-FdUMP) to thymidylate synthase, enhancing 5-FU's cytotoxic effects. The combination is designed to maximize antineoplastic activity by synergistically targeting DNA replication and repair in rapidly proliferating tumor cells. This regimen has demonstrated a manageable safety profile and disease control in heavily pretreated advanced solid tumor populations, notably metastatic colorectal cancer.

Other names

simmitecan + 5-FU/LV