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Drug intelligence / Profile preview
enzalutamide + sorafenib
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Enzalutamide + sorafenib is a combination of two small molecule drugs investigated primarily for advanced cancers, including hepatocellular carcinoma (HCC) and castration-resistant prostate cancer (CRPC). Enzalutamide is an androgen receptor antagonist that blocks multiple steps in the androgen receptor signaling pathway, thereby inhibiting tumor growth driven by androgens. Sorafenib is an oral multikinase inhibitor that targets cell surface tyrosine kinase receptors and downstream kinases involved in tumor proliferation and angiogenesis, notably inhibiting the RAF/MEK/ERK pathway as well as VEGFR and PDGFR signaling. The combination has been studied for potential synergistic effects; preclinical models suggest enhanced inhibition of both AR and ERK pathways, but clinical studies have shown limited additional benefit over monotherapy in HCC. Both drugs are approved individually for other indications but not as a combination[1][2][3][4][8].
- Brand names
- Nexavar
02
Targets
AR (Adrenergic receptors)BRAF (B-Raf proto-oncogene, serine/threonine kinase)FLT3 (Fms related receptor tyrosine kinase 3)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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