Semaxanib

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Semaxanib
Systematic (IUPAC) name
(3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]- 1H-indol-2-one
Identifiers
CAS number	194413-58-6
ATC code	?
PubChem	5329098
Chemical data
Formula	C₁₅H₁₄N₂O
Mol. mass	238.285 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Semaxanib (proposed INN,^[1] 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.^[2] Other studies, at earlier phases, have since been conducted.^[3]^[4]

[edit] Notes

^ World Health Organization (2001). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 85". WHO Drug Information 15 (2). Full textPDF (244 KiB)
^ (February 8, 2002). Pharmacia Announces Closing of SU5416 (semaxanib) Clinical Trials. Press release. Retrieved on 2007-03-20.
^ 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 (2005). "A Phase I study of the angiogenesis inhibitor SU5416 (semaxanib) in solid tumours, incorporating dynamic contrast MR pharmacodynamic end points". Br J Cancer 93 (8): 876–83. PMID 16222321.
^ Lockhart A, Cropp G, Berlin J, Donnelly E, Schumaker R, Schaaf L, Hande K, Fleischer A, Hannah A, Rothenberg M (2006). "Phase I/pilot study of SU5416 (semaxinib) in combination with irinotecan/bolus 5-FU/LV (IFL) in patients with metastatic colorectal cancer". Am J Clin Oncol 29 (2): 109–15. PMID 16601426.

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