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furafylline

Development stage: Discontinued
Modality: Small Molecules
Administration: Oral

Overview

Furafylline is a methylxanthine derivative developed as a long-acting alternative to theophylline for the treatment of asthma. It acts primarily as a potent and highly selective inhibitor of human Cytochrome P450 1A2 (CYP1A2), with an IC50 of approximately 0.07 μM. Furafylline inhibits CYP1A2 in a non-competitive, mechanism-based manner, leading to time-dependent and irreversible loss of enzyme activity. This selectivity makes it useful in research for probing CYP1A2-mediated metabolic pathways and drug interactions[3][5][6][8]. Despite its initial development for asthma, its clinical use has been limited due to concerns about drug interactions resulting from CYP1A2 inhibition[3][7].

Other names: furafilinafurafyllinum

Targets

CYP1A2 (Cytochrome P450 1A2)

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