Drug intelligence / Profile preview

plitidepsin + sorafenib

Development stage
Unknown
Lead developer
PharmaMar
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Plitidepsin + sorafenib is an investigational combination therapy composed of two distinct anticancer agents. Plitidepsin is a cyclic depsipeptide originally isolated from the sea squirt Aplidium albicans and now produced synthetically. Its primary mechanism involves inhibition of eukaryotic translation elongation factor 1 alpha 2 (eEF1A2), leading to cell cycle arrest, induction of oxidative stress, and apoptosis in tumor cells. Sorafenib is a small molecule multikinase inhibitor that targets several kinases involved in tumor cell proliferation and angiogenesis, including RAF kinases and vascular endothelial growth factor receptor (VEGFR). Sorafenib is approved for advanced renal cell carcinoma, hepatocellular carcinoma not amenable to surgery, and certain types of thyroid cancer. The combination has been studied in early-phase clinical trials for advanced solid tumors or lymphomas[3][4][5].

Brand names
Nexavar
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)VEGFR3 (Vascular endothelial growth factor receptor 3)RAF1 (c-Raf-1 (Y340D/Y341D))EEF1A2 (Eukaryotic elongation factor 1 alpha 2)VEGFR2 (Vascular endothelial growth factor receptor 2)

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