Drug intelligence / Profile preview

apafant

Development stage: Discontinued
Lead developer: Boehringer Ingelheim
Modality: Small Molecules
Administration: Inhalation, Intravenous, Ophthalmic, Oral

Overview

Apafant (WEB 2086) is a potent and selective antagonist of the platelet-activating factor (PAF) receptor. It is a thieno-triazolodiazepine compound developed by structural modification of brotizolam, demonstrating that PAF inhibitory actions can be separated from activity at the benzodiazepine receptor. Apafant inhibits PAF-induced platelet and neutrophil aggregation in vitro and in vivo, with anti-inflammatory, antiangiogenic, and anticancer activities reported. It has been investigated for applications involving inflammatory responses such as asthma and conjunctivitis but was never adopted for medical use; it continues to be used in pharmacology research[2][3][1].

Other names: WEB-2086WEB2086WEB 2086

Targets

PTAFR (Platelet-activating factor receptor)

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