Crisaborole (CAS 906673-24-3) is a boron-containing, non-steroidal topical phosphodiesterase 4 (PDE4) inhibitor. The molecule features a benzoxaborole core—a boron atom incorporated into a five-membered oxaborole ring fused to a benzene ring—substituted with a 4-cyanophenoxy group.
Crisaborole is a topical active pharmaceutical ingredient and reference standard for quality control of this first-in-class boron-based PDE4 inhibitor. The synthesis of Crisaborole involves reaction of 4-halogenated benzonitrile with benzo[c][1,2]oxaborole-1,5(3H)-diol under basic conditions in an organic solvent, yielding the product in high purity . In quality control contexts, Crisaborole and its related impurities are essential analytical reference standards for impurity profiling and method development. As a topical ointment, Crisaborole is indicated for mild-to-moderate atopic dermatitis in patients 2 years of age and older .
Product Parameters
Parameter
Specification
Product Name
Crisaborole
CAS Number
906673-24-3
Molecular Formula
C₁₄H₁₀BNO₃
Molecular Weight
251.05 g/mol
Appearance
Solid
Storage Condition
Room temperature (20–25°C) per FDA label for ointment
Application
Crisaborole (AN2728) shows potent activity both in vivo and in vitro. The anti-inflammatory properties of AN2728 are under research. It is also used as a pharmaceutical intermediate.
Product Advantage
The biggest advantage of Crisaborole is that it is a small-molecule non-hormonal drug that can combine both therapeutic effect and comfort. For some patients, it even has almost no side effects. It is the first topical dermatological drug to be included in the list of new drugs urgently needed in clinical practice. The launch of Crisaborole has filled the treatment demand for atopic dermatitis in children and adults in China, breaking the status quo that there had been no new products in the field of topical non-hormonal anti-inflammatory therapy for more than 10 years, which is of epoch-making significance.
Bioactivity
Crisaborole (AN2728) is a selective small-molecule PDE4 inhibitor with broad-spectrum anti-inflammatory activity.
Contact Us
Contact Cosperpharm for Crisaborole inquiries related to your topical PDE4 inhibitor program.
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