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m Remove redundant parameters InChI, InChIKey (StdInChI, StdInChIKey are used). See Talk (via AWB script)
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| StdInChIKey = WUWDLXZGHZSWQZ-WQLSENKSSA-N
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{{Distinguish|Semax]]
'''Semaxanib'''<ref>{{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&nbsp;[[Kibibyte|KiB]]<!-- application/pdf, 250247 bytes -->}}</ref> ('''SU5416''') is a [[tyrosine-kinase inhibitor]] drug designed by [[SUGEN]] as a cancer therapeutic. It is an [[investigational product|experimental stage]] drug, not [[Regulation of therapeutic goods|licensed]] for use on human patients outside of [[clinical trial]]s.
'''Semaxanib'''<ref>{{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&nbsp;[[Kibibyte|KiB]]<!-- application/pdf, 250247 bytes -->}}</ref> ('''SU5416''') is a [[tyrosine-kinase inhibitor]] drug designed by [[SUGEN]] as a cancer therapeutic. It is an [[investigational product|experimental stage]] drug, not [[Regulation of therapeutic goods|licensed]] for use on human patients outside of [[clinical trial]]s.
Semaxanib is a potent and selective synthetic [[kinase inhibitor|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.
Semaxanib is a potent and selective synthetic [[kinase inhibitor|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.

Revision as of 00:43, 9 May 2016

Semaxanib
Clinical data
ATC code
  • none
Identifiers
  • (3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1,3-dihydro-2H-indol-2-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H14N2O
Molar mass238.285 g/mol g·mol−1
3D model (JSmol)
  • O=C2C(\c1ccccc1N2)=C/c3c(cc(n3)C)C
  • InChI=1S/C15H14N2O/c1-9-7-10(2)16-14(9)8-12-11-5-3-4-6-13(11)17-15(12)18/h3-8,16H,1-2H3,(H,17,18)/b12-8- checkY
  • Key:WUWDLXZGHZSWQZ-WQLSENKSSA-N checkY
 ☒NcheckY (what is this?)  (verify)

{{Distinguish|Semax]] Semaxanib[1] (SU5416) is a tyrosine-kinase inhibitor drug designed by SUGEN as a cancer therapeutic. It is an experimental stage drug, not licensed for use on human patients outside of clinical trials. 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 then-parent of Sugen, prematurely ended Phase III clinical trials of semaxinib 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] A related compound, SU11248 was further developed by Sugen, and then by Pfizer and was FDA-approved as sunitinib (Sutent) for treatment of renal carcinoma in January 2006.

References

  1. ^ World Health Organization (2001). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 85". WHO Drug Information. 15 (2). Template:PDFlink
  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. doi:10.1038/sj.bjc.6602797. PMC 2361651. PMID 16222321.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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. doi:10.1097/01.coc.0000199882.53545.ac. PMID 16601426.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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. doi:10.1093/jjco/hyi229. PMID 16449240.


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