Drugs (Pharma Research)

Erdafitinib Erdafitinib (also known as JNJ-42756493) is an orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, Erdafitinib binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumour cell proliferation and tumour cell death in FGFR-overexpressing tumour cells. FGFR, upregulated in many tumour cell types, is a receptor tyrosine kinase essential to tumour cell proliferation, differentiation and survival. Astex Pharmaceuticals discovered this drug and licensed it to Janssen Pharmaceuticals for further development. Erdafitinib has been used in trials studying the basic science and treatment of Tumour or Lymphoma . Common Name:   Erdafitinib Synonyms :    JNJ-42756493; JNJ42756493; JNJ 42756493; G-024; JNJ-493 IUPAC Name :   N...

Drugs in Clinical Pipeline: Vatalanib Vatalanib [ N-(4-chlorophenyl)-4-(pyridine-4-ylmethyl)phthalazin-1-amine ] is an orally bioavailable anilinophthalazine compound that has potent antineoplastic activity. Vatalanib binds to and inhibits the protein kinase domain of vascular endothelial growth factor receptors 1 and 2 (VEGFR 1 and VEGFR2); both receptor tyrosine kinases are involved in angiogenesis. This agent also binds to and inhibits related receptor tyrosine kinases, including platelet-derived growth factor (PDGF) receptor, c-Kit, and c-Fms [1]. Preclinical studies demonstrated antitumor activity against a broad range of cancer types, including colorectal, prostate, renal, hepatocellular, myeloma, recurrent glioblastoma multiform and ovarian. The compound has been investigated in phase I/II studies, alone and in combination with chemotherapy. The activity of Vatalanib is as follows: IC 50  (VEGFR2/KDR, cell-free assay) = 37 nM IC 50  (VEGFR1/F...