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Angiogenesis inhibitor
Vatalanib
Другие языки:

    Vatalanib

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    Not to be confused with Vandetanib.
    Vatalanib
    Vatalanib.svg
    Clinical data
    Pregnancy
    category
    • None assigned
    Routes of
    administration    		 Oral
    ATC code
    • none
    Legal status
    Legal status
    • Investigational
    Pharmacokinetic data
    Bioavailability High
    Metabolism Extensive hepatic metabolism (mostly CYP3A4-mediated)
    Elimination half-life 4.6 ± 1.1 h
    Excretion Fecal and renal
    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
    Formula C20H15ClN4
    Molar mass 346.82 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, that is, 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. Two large, randomized controlled Phase III trials have studied the effect of adding vatalanib to the FOLFOX chemotherapy regimen in people with metastatic colorectal cancer: CONFIRM-1, whose participants had not yet received any treatment for their cancer; and CONFIRM-2, in which participants had received first-line treatment with irinotecan and fluoropyrimidines. Vatalanib produced no significant improvement in overall survival (the primary endpoint of the studies), although it did significantly increase progression-free survival in CONFIRM-2. Both trials found that progression-free survival was improved in people with high levels of lactate dehydrogenase, an enzyme used as a marker of tissue breakdown; the reasons for and implications of this difference are still unclear.

    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.

    External links


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