Drug intelligence / Profile preview

ispinesib + capecitabine

Development stage
Unknown
Lead developer
Cytokinetics
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This combination consists of **ispinesib**, a small molecule inhibitor of kinesin spindle protein (KSP, also known as Eg5), and **capecitabine**, an oral prodrug of 5-fluorouracil. Ispinesib disrupts mitosis by inhibiting KSP, an ATPase essential for mitotic spindle formation and cell division, leading to cell cycle arrest and apoptosis. Capecitabine is metabolized to 5-fluorouracil, which inhibits thymidylate synthase, hampering DNA synthesis and repair. Together, they aim to enhance antitumor activity in cancers, particularly in advanced or metastatic solid tumors such as breast cancer. Preclinical and early clinical studies showed ispinesib + capecitabine to be active and reasonably well tolerated, with enhanced tumor growth inhibition compared to either agent alone, particularly in breast cancer models[1][3][5][7].

02

Targets

KIF11 (Kinesin Spindle Protein)TS (Thymidylate synthase)

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