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**CT900** is a novel small molecule thymidylate synthase (TS) inhibitor that specifically binds to the α-folate receptor (α-FR), leading to selective uptake and cytotoxic action in α-FR-overexpressing tumor cells. Its cyclopentaquinazoline scaffold enables entry into cancer cells via α-FR rather than the reduced folate carrier, distinguishing it from other TS inhibitors. CT900 has shown single-agent antitumor responses in high-grade serous ovarian cancer and is being developed as a targeted therapy for tumors with elevated α-FR expression. The primary mechanism involves inhibition of thymidylate synthase, resulting in disruption of DNA synthesis and tumor cell proliferation. It is distinct from antibody-drug conjugates targeting α-FR, functioning as a standalone targeted small molecule[1][2].
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