Crisaborole

CAS 906673-24-3

About the API

Systematic name 4-[(1-hydroxy-3H-2,1-benzoxaborol-5-yl)oxy]benzonitrile
Molecular Formula C14H10BNO3
Molecular Weight 251.05 g/mol
Therapeutic category Dermatology
Available formulations Topical / Dermatological
Regulations US DMF Flag US DMF

General Information

Crisaborole is a small-molecule compound, non-steroidal and anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor used for the treatment of mild-to-moderate atopic dermatitis (eczema) in adults and children (at the age of 2 and older). PDE4 is an enzyme that converts the intracellular second messenger 3’5′-cyclic adenosine monophosphate (cAMP) into the active metabolite adenosine monophosphate (AMP). By inhibiting PDE4 and thus increasing levels of cAMP, crisaborole controls inflammation. The use of boron chemistry enabled synthesis of a low-molecular-weight compound (251 daltons), thereby facilitating effective penetration of crisaborole through human skin.

Crisaborole is approved for the topical treatment of atopic dermatitis and preliminary studies in children and adults demonstrated favorable efficacy and safety profiles. Crisaborole may represent an anti-inflammatory option that safely minimizes the symptoms and severity of atopic dermatitis and that can be used for both acute and long-term management.