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Vatalanib

Chemical compound

Field	Value
IUPAC_name	N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin- 1-amine
image	Vatalanib.svg
image_class	skin-invert-image
width	180px
pregnancy_AU
pregnancy_US
pregnancy_category	None assigned
legal_AU
legal_CA
legal_UK
legal_US
legal_status	Investigational
routes_of_administration	Oral
bioavailability	High
metabolism	Extensive hepatic metabolism (mostly CYP3A4-mediated)
elimination_half-life	4.6 ± 1.1 h
excretion	Fecal and renal
IUPHAR_ligand	5705
CAS_number	212141-54-3
ATC_prefix	none
PubChem	151194
DrugBank	DB04879
ChEBI	90620
ChEMBL	101253
ChemSpiderID	133257
UNII_Ref
UNII	5DX9U76296
C	20	H=15	Cl=1	N=4
smiles	Clc1ccc(cc1)Nc3nnc(c2c3cccc2)Cc4ccncc4
StdInChI_Ref
StdInChI	1S/C20H15ClN4/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14/h1-12H,13H2,(H,23,25)
StdInChIKey_Ref
StdInChIKey	YCOYDOIWSSHVCK-UHFFFAOYSA-N

| elimination_half-life = 4.6 ± 1.1 h

Vatalanib (INN, codenamed PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis. It is being studied as a possible treatment for several types of cancer, particularly cancer that is at an advanced stage or has not responded to chemotherapy. Vatalanib is orally active, which is to say it is effective when taken by mouth.

Vatalanib is being developed by Bayer Schering and Novartis. It inhibits all known VEGF receptors, as well as platelet-derived growth factor receptor-beta and c-kit, but is most selective for VEGFR-2.

Development

Vatalanib was discovered through high-throughput screening. It has been extensively investigated in Phase I, II and III clinical trials.

Adverse effects

The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.

Notable users

Patrick Swayze, a popular actor in the 1980s who starred in such films as Dirty Dancing and Road House was given this drug when he was diagnosed with Stage IV Pancreatic Cancer in 2008. Doctors hoped the drug would cut off blood supply to the tumor. Despite this, Swayze died on September 14, 2009, 20 months after being diagnosed.

References

(November 2006). "Metabolism and disposition of vatalanib (PTK787/ZK-222584) in cancer patients". Drug Metabolism and Disposition.
(April 2000). "PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration". Cancer Research.
(April 2007). "Target practice: lessons from phase III trials with bevacizumab and vatalanib in the treatment of advanced colorectal cancer". The Oncologist.
Mariani SM. (2004). "Antiangiogenesis Cocktails -- Stirred or Shaken?: Highlights of the 9th Annual Drug Discovery Technology World Congress; August 8-13, 2004; Boston, Massachusetts". Medscape General Medicine.
"Patrick Swayze Dies of Pancreatic Cancer".

Info: Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

angiogenesis-inhibitors tyrosine-kinase-inhibitors experimental-cancer-drugs

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