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erlotinib + sorafenib
- Development stage
- Unknown
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Erlotinib + sorafenib is a combination of two oral small molecule kinase inhibitors used in clinical trials for the treatment of various solid tumors, including recurrent glioblastoma and advanced pancreatic cancer. Erlotinib acts as an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, blocking EGFR-mediated signaling pathways involved in tumor cell proliferation. Sorafenib inhibits multiple kinases, including RAF kinases in the Ras/Raf/MEK/ERK pathway and receptor tyrosine kinases such as VEGFR and PDGFR, thereby inhibiting both tumor cell proliferation and angiogenesis. The combination has been studied to target complementary pathways involved in cancer progression but has shown limited efficacy with notable toxicity risks[1][2][5][6].
- Brand names
- Tarceva (for erlotinib)Nexavar (for sorafenib)
- Other names
- erlotinib + sorafenib
02
Targets
RAF1 (c-Raf-1 (Y340D/Y341D))CYP1A1 (Cytochrome P450 1A1)BRAF (B-Raf proto-oncogene, serine/threonine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)VEGFR3 (Vascular endothelial growth factor receptor 3)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)DDR1 (Discoidin domain receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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