Drug intelligence / Profile preview

bilobalide

Development stage
Phase 4
Lead developer
HWI pharma services
Modality
Small Molecules
Administration
Oral
01

Overview

**Bilobalide** is a natural sesquiterpene trilactone isolated from the leaves of *Ginkgo biloba*. It is a primary terpenoid component of Ginkgo extracts and possesses extensive pharmacological actions. Bilobalide exhibits **neuroprotective**, **antioxidant**, **anti-inflammatory**, **anti-ischemic**, and **cardiovascular protective** activities. Mechanistically, bilobalide acts as a **negative allosteric modulator of GABA-A and GABA-A-rho receptors**, potentially influencing cognitive and memory functions, with selectivity for certain receptor subunits. It also acts as a glycine receptor antagonist and an enzyme modulator (induces CYP3A1, CYP1A2, and activates constitutive androstane receptor). Additional mechanisms include inhibition of neuronal apoptosis, protection against hypoxia-induced cellular damage, upregulation of mitochondrial respiratory chain proteins, and promotion of amyloid-beta degrading enzymes in astrocytes. Bilobalide has demonstrated protection against neuronal injury in models of Alzheimer's disease and vascular dementia[1][3][4][5][7].

Other names
Bilobalide AGinkgolactone(-)-bilobalideVitexicarpim
02

Targets

GABRR (GABA-A receptor subunit rho)CXADR (Coxsackievirus and adenovirus receptor)CYP1A2 (Cytochrome P450 1A2)CYP3A1 (Cytochrome P450 3A1)Glycine receptorSTAT3 (Signal Transducer and Activator of Transcription 3)

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