Drug intelligence / Profile preview

irinotecan + pemetrexed

Development stage
Unknown
Lead developer
Pfizer
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Irinotecan + pemetrexed is a combination of two chemotherapeutic agents used primarily in the treatment of advanced or metastatic colorectal cancer and has also been studied in pancreatic and other solid tumors. Irinotecan is a topoisomerase I inhibitor that prevents DNA replication by stabilizing the cleavable complex between topoisomerase I and DNA, leading to double-strand breaks and cell death. Pemetrexed is an antifolate antimetabolite that inhibits several folate-dependent enzymes involved in purine and pyrimidine synthesis (including thymidylate synthase), thereby disrupting DNA and RNA synthesis. The combination leverages their distinct mechanisms for potential synergistic cytotoxicity against tumor cells[2][3][6].

Other names
CPT-11 + PMXirinotecan hydrochloride + pemetrexed disodium
02

Targets

TOP1 (DNA Topoisomerase I)GART (GAR transformylase)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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