Semaxanib

drugbox
IUPAC_name = (3"Z")-3- [(3,5-dimethyl-1"H"-pyrrol-2-yl)methylidene] -
1"H"-indol-2-one

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CAS_number = 194413-58-6
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PubChem = 5329098
DrugBank =
C = 15 | H = 14 | N = 2 | O = 1
molecular_weight = 238.285 g/mol
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Semaxanib (proposed INN, [cite journal | author = World Health Organization | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 85 | journal = WHO Drug Information | volume = 15 | issue = 2 | year = 2001 PDFlink| [http://www.who.int/druginformation/vol15num2_2001/list_85.pdf Full text] |244 KiB ] also semaxinib or SU5416) is a drug intended for use in the treatment of cancer. It is still at an experimental stage and as such has not yet received a licence for use on human patients (except in the setting of a clinical trial).Semaxanib is a potent and selective synthetic inhibitor of the Flk-1/KDR vascular endothelial growth factor (VEGF) receptor tyrosine kinase. It targets the VEGF pathway, and both "in vivo" and "in vitro" studies have demonstrated antiangiogenic potential.

On February 2002, Pharmacia, the developer of semaxanib, prematurely ended Phase III clinical trials it was conducting on the drug's effectiveness in the treatment of advanced colorectal cancer due to discouraging results. [cite press release | url = http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/02-08-2002/0001665238&EDATE= | title = Pharmacia Announces Closing of SU5416 (semaxanib) Clinical Trials | date = February 8, 2002 | accessdate = 2007-03-20] Other studies, at earlier phases, have since been conducted. [cite journal |author=O'Donnell A, Padhani A, Hayes C, Kakkar A, Leach M, Trigo J, Scurr M, Raynaud F, Phillips S, Aherne W, Hardcastle A, Workman P, Hannah A, Judson I |title=A Phase I study of the angiogenesis inhibitor SU5416 (semaxanib) in solid tumours, incorporating dynamic contrast MR pharmacodynamic end points |journal=Br J Cancer |volume=93 |issue=8 |pages=876–83 |year=2005 |pmid=16222321 |doi=10.1038/sj.bjc.6602797] [cite journal |author=Lockhart A, Cropp G, Berlin J, Donnelly E, Schumaker R, Schaaf L, Hande K, Fleischer A, Hannah A, Rothenberg M |title=Phase I/pilot study of SU5416 (semaxinib) in combination with irinotecan/bolus 5-FU/LV (IFL) in patients with metastatic colorectal cancer |journal=Am J Clin Oncol |volume=29 |issue=2 |pages=109–15 |year=2006 |pmid=16601426 |doi=10.1097/01.coc.0000199882.53545.ac] However, due to the prospect of next-generation tyrosine kinase inhibitors and the ineffaciousness of semaxanib in clinic trials, further development of the drug has been discontinued. [cite journal|url=http://jjco.oxfordjournals.org/cgi/content/full/36/2/100 |author= Hoff, PM, et al. |title=A Phase I Study of Escalating Doses of the Tyrosine Kinase Inhibitor Semaxanib (SU5416) in Combination with Irinotecan in Patients with Advanced Colorectal Carcinoma |journal=Japanese Journal of Clinical Oncology |volume=36 |issue=2 |pages=100–103|year=2006 |doi=10.1093/jjco/hyi229]

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