Toceranib: Difference between revisions

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{{Drugbox
{{Drugbox
| IUPAC_name = 5-[(5''Z'')-(5-fluoro-2-oxo-1,2-dihydro-3''H''-indol-3-ylidene)methyl]-2,4-dimethyl-''N''-[2-(pyrrolidin-1-yl)ethyl]-1''H''-pyrrole-3-carboxamide
| IUPAC_name = 5-[(5''Z'')-(5-fluoro-2-oxo-1,2-dihydro-3''H''-indol-3-ylidene)methyl]-2,4-dimethyl-''N''-[2-(pyrrolidin-1-yl)ethyl]-1''H''-pyrrole-3-carboxamide
| image = Toceranib.svg
| image = Toceranib.png
| image2 = Toceranib molecule ball.png
| image2 = Toceranib_molecule_ball.png
| width2 = 260
| width2 = 260
| alt2 = Ball-and-stick model of the toceranib molecule
| alt2 = Ball-and-stick model of the toceranib molecule
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| smiles = Fc1ccc2c(c1)/C(C(=O)N2)=C/c4c(c(C(=O)NCCN3CCCC3)c(n4)C)C
| smiles = Fc1ccc2c(c1)/C(C(=O)N2)=C/c4c(c(C(=O)NCCN3CCCC3)c(n4)C)C
}}
}}
              __NOTOC__
{{SI}}
{{CMG}}
==Overview==
'''Toceranib''' is a [[receptor tyrosine kinase]] inhibitor and is used in the treatment<ref name="pmid17227978">{{cite journal |author=London CA, Malpas PB, Wood-Follis SL, ''et al.'' |title=Multi-center, Placebo-controlled, Double-blind, Randomized Study of Oral Toceranib Phosphate (SU11654), a Receptor Tyrosine Kinase Inhibitor, for the Treatment of Dogs with Recurrent (Either Local or Distant) Mast Cell Tumor Following Surgical Excision. |journal=Clin Cancer Res |volume=15 |issue=11 |pages=3856–65 |date=June 2009 |pmid=19470739 |doi= 10.1158/1078-0432.CCR-08-1860 |url=http://clincancerres.aacrjournals.org/cgi/content/abstract/15/11/3856}}</ref> of canine [[mast cell]] tumor also called [[mastocytoma]]. Together with [[masitinib]] (Kinavet (US)/Masivet (EU/ROW) by AB Science), toceranib is the only dog-specific anti-[[cancer]] drug<ref>[http://www.cbsnews.com/stories/2009/06/03/eveningnews/main5060208.shtml  CBS News FDA Approves First-Ever Dog Cancer Drug]</ref> approved by the [[Food and Drug Administration (United States)|U.S. Food and Drug Administration]].<ref>[http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm164118.htm  FDA NEWS RELEASE]</ref> It is marketed as '''Palladia''' as its phosphate salt, '''toceranib phosphate''' ([[International Nonproprietary Name|INN]]) by [[Pfizer]]. It was developed by [[SUGEN]] as SU11654,<ref>[http://www.nytimes.com/2006/11/24/business/24cancer.html In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too, New York Times]</ref> a sister compound to [[sunitinib]], which was later approved for human therapies. Toceranib is likely to act mostly through inhibition of the [[C-kit|kit]] tyrosine kinase, though it may also have an [[Angiogenesis inhibitor|anti-angiogenic]] effect.
'''Toceranib''' is a [[receptor tyrosine kinase]] inhibitor and is used in the treatment<ref name="pmid17227978">{{cite journal |author=London CA, Malpas PB, Wood-Follis SL, ''et al.'' |title=Multi-center, Placebo-controlled, Double-blind, Randomized Study of Oral Toceranib Phosphate (SU11654), a Receptor Tyrosine Kinase Inhibitor, for the Treatment of Dogs with Recurrent (Either Local or Distant) Mast Cell Tumor Following Surgical Excision. |journal=Clin Cancer Res |volume=15 |issue=11 |pages=3856–65 |date=June 2009 |pmid=19470739 |doi= 10.1158/1078-0432.CCR-08-1860 |url=http://clincancerres.aacrjournals.org/cgi/content/abstract/15/11/3856}}</ref> of canine [[mast cell]] tumor also called [[mastocytoma]]. Together with [[masitinib]] (Kinavet (US)/Masivet (EU/ROW) by AB Science), toceranib is the only dog-specific anti-[[cancer]] drug<ref>[http://www.cbsnews.com/stories/2009/06/03/eveningnews/main5060208.shtml  CBS News FDA Approves First-Ever Dog Cancer Drug]</ref> approved by the [[Food and Drug Administration (United States)|U.S. Food and Drug Administration]].<ref>[http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm164118.htm  FDA NEWS RELEASE]</ref> It is marketed as '''Palladia''' as its phosphate salt, '''toceranib phosphate''' ([[International Nonproprietary Name|INN]]) by [[Pfizer]]. It was developed by [[SUGEN]] as SU11654,<ref>[http://www.nytimes.com/2006/11/24/business/24cancer.html In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too, New York Times]</ref> a sister compound to [[sunitinib]], which was later approved for human therapies. Toceranib is likely to act mostly through inhibition of the [[C-kit|kit]] tyrosine kinase, though it may also have an [[Angiogenesis inhibitor|anti-angiogenic]] effect.


==References==
==References==
{{Reflist}}
{{Reflist|2}}


==External links==
==External links==
*[http://www.palladia-pi.com/ Official Site for Palladia]
*[http://www.palladia-pi.com/ Official Site for Palladia]


{{Extracellular chemotherapeutic agents}}


[[Category:Receptor tyrosine kinase inhibitors]]
 
 
[[Category:Organofluorides]]
[[Category:Organofluorides]]
[[Category:Indoles]]
[[Category:Indoles]]
[[Category:Pyrroles]]
[[Category:Drug]]
[[Category:Amides]]
[[Category:Amides]]
[[Category:Pyrrolidines]]
[[Category:Pyrrolidines]]
[[Category:Dog health]]
[[Category:Dog health]]
{{antineoplastic-drug-stub}}

Latest revision as of 17:18, 20 August 2015

Toceranib
Ball-and-stick model of the toceranib molecule
Clinical data
Trade namesPalladia
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATCvet code
Legal status
Legal status
Pharmacokinetic data
Bioavailability77%
Protein binding91%-93%
Elimination half-life16 h
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC22H25FN4O2
Molar mass396.46 g/mol
494.46 g/mol (phosphate)
3D model (JSmol)

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Toceranib is a receptor tyrosine kinase inhibitor and is used in the treatment[1] of canine mast cell tumor also called mastocytoma. Together with masitinib (Kinavet (US)/Masivet (EU/ROW) by AB Science), toceranib is the only dog-specific anti-cancer drug[2] approved by the U.S. Food and Drug Administration.[3] It is marketed as Palladia as its phosphate salt, toceranib phosphate (INN) by Pfizer. It was developed by SUGEN as SU11654,[4] a sister compound to sunitinib, which was later approved for human therapies. Toceranib is likely to act mostly through inhibition of the kit tyrosine kinase, though it may also have an anti-angiogenic effect.

References

  1. ↑ London CA, Malpas PB, Wood-Follis SL; et al. (June 2009). "Multi-center, Placebo-controlled, Double-blind, Randomized Study of Oral Toceranib Phosphate (SU11654), a Receptor Tyrosine Kinase Inhibitor, for the Treatment of Dogs with Recurrent (Either Local or Distant) Mast Cell Tumor Following Surgical Excision". Clin Cancer Res. 15 (11): 3856–65. doi:10.1158/1078-0432.CCR-08-1860. PMID 19470739.
  2. ↑ CBS News FDA Approves First-Ever Dog Cancer Drug
  3. ↑ FDA NEWS RELEASE
  4. ↑ In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too, New York Times

External links

Retrieved from "https://www.wikidoc.org/index.php?title=Toceranib&oldid=1137715"