Vatalanib

Not to be confused with Vandetanib.
Vatalanib
Clinical data
Pregnancy
category
  • None assigned
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Pharmacokinetic data
BioavailabilityHigh
MetabolismExtensive hepatic metabolism (mostly CYP3A4-mediated)[1]
Elimination half-life4.6 ± 1.1 h[1]
ExcretionFecal and renal[1]
Identifiers
  • N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin- 1-amine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC20H15ClN4
Molar mass346.82 g·mol−1
3D model (JSmol)
  • Clc1ccc(cc1)Nc3nnc(c2c3cccc2)Cc4ccncc4
  • InChI=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) ☒N
  • Key:YCOYDOIWSSHVCK-UHFFFAOYSA-N ☒N

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.[1][2][3][4]

  1. ^ a b c d Jost LM, Gschwind HP, Jalava T, et al. (November 2006). "Metabolism and disposition of vatalanib (PTK787/ZK-222584) in cancer patients". Drug Metabolism and Disposition. 34 (11): 1817–28. doi:10.1124/dmd.106.009944. PMID 16882767. S2CID 9545358.
  2. ^ Cite error: The named reference Mariani was invoked but never defined (see the help page).
  3. ^ Wood JM, Bold G, Buchdunger E, et al. (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. 60 (8): 2178–89. PMID 10786682.
  4. ^ Los M, Roodhart JM, Voest EE (April 2007). "Target practice: lessons from phase III trials with bevacizumab and vatalanib in the treatment of advanced colorectal cancer". The Oncologist. 12 (4): 443–50. doi:10.1634/theoncologist.12-4-443. PMID 17470687.