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sorafenib + leuprolide + bicalutamide
- Development stage
- Discontinued
- Lead developer
- Mount Sinai Beth Israel
- Modality
- Small Molecules, Peptides
- Administration
- Oral, Intramuscular, Subcutaneous
01
Overview
This combination therapy regimen consists of the multi-kinase inhibitor sorafenib, the GnRH agonist leuprolide acetate, and the androgen receptor antagonist bicalutamide. It was specifically evaluated in a Phase I/II clinical trial (NCT00924807) led by Beth Israel Medical Center for the treatment of intermediate- and high-risk localized prostate cancer. In this therapeutic setting, sorafenib was investigated as a potential radiosensitizer to be administered concurrently with standard external beam radiotherapy and androgen deprivation therapy (ADT). Sorafenib targets multiple tyrosine kinases including VEGFR and PDGFR, as well as Raf kinases, to inhibit angiogenesis and tumor cell proliferation. Leuprolide and bicalutamide work together to achieve profound androgen suppression, which is the standard of care for hormone-sensitive prostate cancer.
- Brand names
- Nexavar
- Other names
- Sorafenib with ADT and Radiotherapy in Localized Prostate Cancer
02
Targets
AR (Adrenergic receptors)BRAF (B-Raf proto-oncogene, serine/threonine kinase)FLT3 (Fms related receptor tyrosine kinase 3)GnRHR (Gonadotropin-releasing hormone receptor)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))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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