Drug intelligence / Profile preview

MK-0731

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

MK‑0731 is a synthetic small molecule that acts as a potent and selective inhibitor of kinesin spindle protein (KSP; also known as KIF11 or Eg5), an essential mitotic kinesin required for the separation of spindle poles during cell division. By inhibiting KSP, MK‑0731 disrupts mitotic spindle assembly, leading to cell cycle arrest in the mitotic phase and apoptosis in proliferating tumor cells. This mechanism offers potential antineoplastic activity with reduced risk of peripheral neuropathy compared to microtubule-targeted agents. Developed by Merck Sharp & Dohme Corp., it was investigated primarily for advanced solid tumors and taxane-resistant cancers but did not progress beyond early clinical trials due to limited efficacy and development discontinuation[1][2][5][6][7].

Other names
(2S)-4-(2,5-difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamideUNII-8HIJ5G3O02UNII8HIJ5G3O02UNII 8HIJ5G3O02
02

Targets

KCNH2 (Voltage-gated potassium channel subfamily H member 2)KIF11 (Kinesin Spindle Protein)

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