Drug intelligence / Profile preview

cepharanthine

Development stage
Phase 2
Lead developer
PharmaDrug
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Cepharanthine is a natural bisbenzylisoquinoline alkaloid extracted from the plant Stephania cepharantha Hayata. It has been used in Japan since the 1950s to treat a variety of acute and chronic diseases, including radiation-induced leukopenia, alopecia areata, idiopathic thrombocytopenic purpura, venomous snakebites, xerostomia, sarcoidosis, refractory anemia, and various cancer-related conditions. Cepharanthine exhibits anti-inflammatory, immunomodulatory, antineoplastic (anticancer), antiviral (including activity against HSV and HIV in vitro), anti-parasitic and antioxidative properties[1][5][7][8]. Its mechanism of action is multifactorial: it modulates membrane efflux pumps and rigidifies membranes; intracellularly it activates AMP-activated protein kinase (AMPK) and inhibits NFκB signaling pathways—leading to reduced inflammation—and can also inhibit PI3K/Akt and p38 MAPK signaling pathways involved in cell proliferation and survival[1][6][8]. Cepharanthine can induce cell cycle arrest at G2/M phase and promote apoptosis in infected or malignant cells. It is approved for use primarily in Japan.

Brand names
Cepharanthin (Japan)
Other names
bisbenzylisoquinoline alkaloidcycleanine
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)AKT (RAC-alpha serine/threonine-protein kinase)NF-κBMAPK14 (p38 mitogen-activated protein kinase alpha)PIK3CA (Phosphoinositide 3-kinase alpha)

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