vatalanib vatalanib 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. not to be confused with vandetanib. vatalanibclinical datapregnancycategory none assigned routes ofadministrationoralatc codenonelegal statuslegal status investigational pharmacokinetic databioavailabilityhighmetabolismextensive hepatic metabolism (mostly cyp3a4-mediated)elimination half-life4.6 ± 1.1 hexcretionfecal and renalidentifiers iupac name n-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin- 1-amine cas number212141-54-3pubchem cid151194iuphar/bps5705drugbankdb04879chemspider133257unii5dx9u76296chebichebi:90620chemblchembl101253comptox dashboard (epa)dtxsid2046919 chemical and physical dataformulac20h15cln4molar mass346.82 g·mol−13d model (jsmol)interactive image smiles clc1ccc(cc1)nc3nnc(c2c3cccc2)cc4ccncc4 inchi 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) nkey:ycoydoiwsshvck-uhfffaoysa-n n 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.