Vatalanib

Vatalanib is an oral anti-angiogenesis agent that inhibits vascular endothelial growth factor receptor tyrosine kinases, which in patients showed auto induction of metabolism and variability in pharmacokinetic (PK) disposition. At higher concentrations, other tyrosine kinases are also inhibited, including PDGFR-β (IC₅₀ = 580 nM), c-KIT (IC₅₀ = 730 nM), FLT-4 (IC₅₀ = 660 nM) and c-FMS (IC₅₀ = 1.4 µM). On the other hand, vatalanib is not active against the EGFR, c-SRC, v-ABL, and protein kinase Cα (IC₅₀ > 10 µM). Vatalanib was well tolerated as a second-line therapy and resulted in favorable 6-month survival rate in patients with metastatic pancreatic cancer, compared with historic controls. The inhibitor Vatalanib is possibly an additional option in the treatment of leiomyosarcomas.