Drug intelligence / Profile preview

excavatolide B

Development stage
Preclinical
Modality
Small Molecules
Administration
Topical, Not Established For Human Systemic Use (investigational Routes In Animal Models, Including Systemic Administration)
01

Overview

Excavatolide B is a **briarane-type diterpenoid** isolated from marine soft corals, primarily *Briareum excavatum* and *Briareum stechei*. It exhibits **anti-inflammatory, analgesic, immunomodulatory, anti-angiogenic, and anti-proliferative (anti-tumor)** activities. Mechanistic studies indicate that excavatolide B inhibits the expression of inflammatory mediators, including **inducible nitric oxide synthase (iNOS)** and **cyclooxygenase-2 (COX-2)**, and reduces the production of cytokines such as IL-1β, IL-6, IL-17A, and TNF. It also downregulates angiogenesis marker VEGF and modulates STING (stimulator of interferon genes) signaling through covalent inhibition, as well as inhibiting osteoclast differentiation, and exerts effects via suppression of NF-κB activity and upregulation of PTEN. The compound is being investigated for inflammatory diseases (such as rheumatoid arthritis and atopic dermatitis) and various cancers in preclinical settings[1][3][4][7][9][11][12][13].

Other names
excavatolide BExc-BBrD1BrD-1BrD 1((1S,2R,3S,4R,5S,7S,8R,9S,10S,12Z,14S,17R)-2,7,9-triacetyloxy-5-hydroxy-4,8,12,17-tetramethyl-16-oxo-15,18-dioxatetracyclo(12.4.0.01,17.03...
02

Targets

STING (Stimulator of interferon genes protein)NOS2 (Nitric Oxide Synthase 2)NF-κBPPARG (Peroxisome proliferator-activated receptor gamma)

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