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CT-2106 + 5-fluorouracil + folinic acid

Development stage
Unknown
Lead developer
Sobi
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

This is a **combination chemotherapy regimen** comprising CT-2106 (a polymer-drug conjugate of camptothecin), **5-fluorouracil** (an antimetabolite), and **folinic acid** (leucovorin). CT-2106 is a macromolecular conjugate where camptothecin, a potent topoisomerase I inhibitor, is bound to a biodegradable α-poly-L-glutamic acid-glycine polymer, increasing water solubility, tumor targeting, and stability versus camptothecin alone. 5-fluorouracil inhibits thymidylate synthase and RNA functions, hampering tumor cell DNA synthesis. Folinic acid potentiates 5-fluorouracil’s cytotoxic effect by stabilizing its binding to thymidylate synthase. This triple regimen is used in metastatic colorectal cancer that has failed prior oxaliplatin-containing therapy and has been studied for dose limiting toxicities, safety, and antitumor activity in phase I/II trials[4][1].

Other names
PG-Gly-CPT + 5-fluorouracil + folinic acid
02

Targets

TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)

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