Drug intelligence / Profile preview

andrographolide

Development stage
Phase 3
Lead developer
HUTCHMED
Modality
Small Molecules
Administration
Oral, Intravenous, Topical
01

Overview

Andrographolide is a labdane diterpenoid lactone and the principal bioactive compound isolated from the plant Andrographis paniculata. It is widely used in traditional medicine systems such as Traditional Chinese Medicine and Ayurveda for its anti-inflammatory and immunomodulatory properties. Mechanistically, andrographolide exhibits multiple pharmacological effects including inhibition of NF-kappaB activation (a key transcription factor in inflammation), suppression of inducible nitric oxide synthase (iNOS), inhibition of cyclooxygenase 2 (COX‑2), and non‑ATP competitive substrate‑competitive inhibition of glycogen synthase kinase 3 beta (GSK‑3β). It also blocks T-cell proliferation to allogenic stimuli and inhibits chemotactic migration of macrophages. Andrographolide has demonstrated anti-inflammatory[7][9], antiviral[5], antibacterial[5], anticancer[7][9], hepatoprotective[7][9], immunostimulant[4] activities in preclinical studies. Clinical trials have explored its use for ulcerative colitis[4], rheumatoid arthritis[4], multiple sclerosis fatigue reduction[4], upper respiratory tract infections including COVID‑19 adjunct therapy[10]. Its poor water solubility limits oral bioavailability; various formulations are under investigation to improve this property.

Brand names
ANDROGRAPHOLIDE (USP-RS)
Other names
(1R-(1-alpha(E(S)),4abeta,5alpha,6alpha,8aalpha))-3-(2-(decahydro-6-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylene-1-naphthalenyl)ethylidene)dihydro-4-hydroxy-2(3H)-furanone(3E,4S)-3-(2-((1R,4AS,5R,6R,8AS)-DECAHYDRO-6-HYDROXY-5-(HYDROXYMETHYL)-5,8A-DIMETHYL-2-METHYLENE-1-NAPHTHALENYL)ETHYLIDENE)DIHYDRO-4-HYDROXY-2(3H)-FURANONEANDROGRAPHOLIDE [USP-RS]
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)GSK3 (Glycogen synthase kinase 3 beta)NF-κBNOS2 (Nitric Oxide Synthase 2)

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