Drug intelligence / Profile preview

mivobulin isethionate

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

Mivobulin isethionate (CI-980) is a small molecule chemotherapeutic and mitotic inhibitor that acts by binding to the colchicine site on tubulin, thereby inhibiting tubulin polymerization and preventing microtubule assembly. This arrests cells in the M (mitotic) phase, ultimately leading to cell death. It is structurally and functionally similar to colchicine, exhibits a broad spectrum of preclinical activity (including multi-drug resistant tumors), and was noted for its ability to cross the blood-brain barrier. Clinical trials focused on advanced melanoma, prostate cancer, small cell lung cancer, colorectal cancer, and ovarian cancer. Toxicities included myelosuppression and neurotoxicity, particularly reversible memory impairment. CI-980 showed limited efficacy in late-phase trials, resulting in discontinued development as an antineoplastic agent[1][2][4][5][6][9].

Other names
ethyl (S)-(5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazine-7-yl) carbamate 2-hydroxyethansulfonate
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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