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.

?

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Routes ?

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Overview

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] 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.[5]

Notes

  1. World Health Organization (2001). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 85". WHO Drug Information. 15 (2).  Full textPDF (244 KiB)
  2. "Pharmacia Announces Closing of SU5416 (semaxanib) Clinical Trials" (Press release). February 8, 2002. Retrieved 2007-03-20. 
  3. 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. 
  4. 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. 
  5. Hoff, PM; et al. (2006). "A Phase I Study of Escalating Doses of the Tyrosine Kinase Inhibitor Semaxanib (SU5416) in Combination with Irinotecan in Patients with Advanced Colorectal Carcinoma". Japanese Journal of Clinical Oncology. 36 (2): 100–103. 




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