Drug intelligence / Profile preview

CT-322 + irinotecan + 5-fluorouracil + leucovorin

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Recombinant Proteins and Enzymes, Small Molecules
Administration
Intravenous
01

Overview

CT-322 + irinotecan + 5-fluorouracil + leucovorin is a combination therapy under investigation, primarily for cancer, especially advanced solid tumors and recurrent glioblastoma multiforme. - **CT-322 (BMS-844203/Angiocept)** is a first-in-class engineered adnectin (a novel protein therapeutic derived from human fibronectin) that acts as a potent and specific antagonist of vascular endothelial growth factor receptor 2 (VEGFR-2), blocking its function and thus inhibiting tumor angiogenesis. CT-322 binds to the extracellular domain of VEGFR-2, blocking its activation by VEGF-A, VEGF-C, and VEGF-D, resulting in decreased tumor blood vessel formation and tumor growth[1][2][3]. - **Irinotecan** is a small molecule chemotherapy agent, a topoisomerase I inhibitor, interfering with DNA replication and transcription, causing DNA damage and cell death. - **5-Fluorouracil (5-FU)** is a classic antimetabolite chemotherapy that inhibits thymidylate synthase, disrupting DNA synthesis in rapidly dividing tumor cells. - **Leucovorin (folinic acid)** is used to potentiate the cytotoxic effects of 5-fluorouracil and rescue normal cells from certain chemotherapeutic toxicities. This specific combination is being evaluated in clinical trials, notably for recurrent glioblastoma multiforme, with CT-322 targeting the tumor vasculature and the cytotoxic agents attacking tumor cells directly[4].

Brand names
Angiocept
Other names
adnectin VEGFR-2 inhibitor + irinotecan + 5-fluorouracil + leucovorin
02

Targets

TOP1 (DNA Topoisomerase I)VEGFR2 (Vascular endothelial growth factor receptor 2)TS (Thymidylate synthase)

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