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Ispinesib

Ispinesib is a synthetic small molecule, derived from quinazolinone, with antineoplastic properties. Ispinesib selectively inhibits the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and cell death in tumor cells that are actively dividing. Because KSP is not involved in nonmitotic processes, such as neuronal transport, ispinesib may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

According to Cytokinestics, Ispinesib, a novel small molecule inhibitor of kinesin spindle protein (KSP) has been the subject of nine Phase II clinical trials and eight Phase I or Ib clinical trials evaluating ispinesib in a variety of both solid and hematologic cancers. To date, Cytokinestics believes clinical activity for ispinesib has been observed in non-small cell lung, ovarian and breast cancers, with the most clinical activity observed in a Phase II clinical trial evaluating ispinesib in the treatment of patients with locally advanced or metastatic breast cancer that had failed treatment with taxanes and anthracyclines. Cytokinestics, are conducting a Phase I/II clinical trial for ispinesib to further define its clinical activity profile in chemotherapy-naïve locally advanced or metastatic breast cancer patients on a more dose-dense schedule than that previously evaluated to determine if the overall response to ispinesib can be increased while maintaining its existing safety profile. 

Current developer:   GlaxoSmithKline and Cytokinetics

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21. Knox, Jennifer J.; Gill, Sharlene; Synold, Timothy W.; Biagi, James J.; Major, Pierre; Feld, Ron; Cripps, Christine; Wainman, Nancy; Eisenhauer, Elizabeth; Seymour, Lesley. A phase II and pharmacokinetic study of SB-715992, in patients with metastatic hepatocellular carcinoma: a study of the National Cancer Institute of Canada Clinical Trials Group (NCIC CTG IND.168). Investigational New Drugs (2008), 26(3), 265-272. CODEN: INNDDK ISSN:0167-6997. CAN 149:439556 AN 2008:498027

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