Drug intelligence / Profile preview

sinomenine

Development stage
Phase 3
Lead developer
Zhengqing Pharmaceutical Group
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Sinomenine is a bioactive alkaloid extracted from the Chinese medicinal plant Sinomenium acutum. It exhibits significant pharmacological effects, including anti-inflammatory, analgesic (pain-relieving), immunosuppressive, antihypertensive, and anti-arrhythmic activities[2][5][8]. Its primary mechanism involves inhibition of cyclooxygenase-2 (COX-2) expression and modulation of inflammatory cytokines such as TNF-α and IL-1β[5][6]. Sinomenine also potently releases histamine by degranulating tissue mast cells, leading to vasodilation and increased vascular permeability in skin and joint capsules[3]. Clinically, it is used for the treatment of rheumatoid arthritis (RA), osteoarthritis, neuralgia, and gouty arthritis in China under various formulations including tablets (e.g., Zhengqing Fengtongning), injections, sustained-release agents, and transdermal preparations[1][2][4][6]. It has demonstrated efficacy in reducing joint pain/swelling/stiffness in RA patients while lowering inflammatory markers such as CRP and ESR. Side effects are generally mild but may include fatigue or allergic reactions at higher doses.

Brand names
正清风痛宁 Zhengqing Fengtongning ZQFTN
Other names
青藤碱 Sinomenine hydrochloride SIN
02

Targets

IL1B (Interleukin-1 beta)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)HRH1 (Histamine H1 Receptor)

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