Crisaborole

CBNumber： CB42518350
Name： Crisaborole
MF： C14H10BNO3
MW： 251.05
CAS： 906673-24-3

Introduction:

Criborole (AN2728) is a non-steroidal phosphodiesterase 4 (PDE-4) inhibitor. It was first developed by Anacor Pharmaceuticals. In May 2016, Pfizer acquired Anacor. In December of the same year, the US FDA approved Criborone (AN2728) ointment (2% or 5%) for the topical treatment of patients over 2 years old. Severe to moderate atopic dermatitis, marketed under the trade name Eucrisa.

Product advantages:

The biggest advantage of criborole is that it is a small-molecule non-hormonal drug, which can achieve a combination of therapeutic effect and comfort, and even has almost no side effects for some patients. It is the first topical dermatology drug to enter the list of urgently needed new drugs in clinical practice. It can be said that the launch of criborole has filled the treatment needs of Chinese children and adults with atopic dermatitis, breaking the current situation of no new products in the field of topical non-hormonal anti-inflammatory for more than 10 years, which is of epoch-making significance.

Market outlook:

Criborole was developed by Anacor, and Pfizer acquired Anacor at a high price. In December 2016, Criborole was approved by the US FDA, becoming the first new drug approved by the US FDA for the treatment of atopic dermatitis (AD) in the past 15 years. molecular entities. In July 2020, Criborone ointment was approved by Chemicalbook in China, becoming the first and only hormone-free PDE-4 inhibitor suitable for the treatment of mild to moderate atopic dermatitis in children and adults aged 2 years and above in China Topical prescription drugs. Criborone is a phosphodiesterase 4 (PDE4) inhibitor. PDE4 is an enzyme involved in controlling the activity of inflammatory cells. PDE4 participates in IL-4/5 in inflammatory cells by controlling the degradation of cyclic adenosine monophosphate. The production of inflammatory factors such as /10/13 and prostaglandin PGE2 plays a role by inhibiting the activity of PDE4 and improves the body's inflammatory response. Clinical studies have shown that 28-day treatment with criborole resulted in significant remission, complete or almost complete resolution of the rash compared with placebo in patients 2-79 years of age with mild to moderate atopic dermatitis. In 2017, the sales of criborole were US$67 million; in 2018, the global sales of criborole were US$147 million, with a growth rate of 119.40%, which brought new hope to many patients with atopic dermatitis.

Use:

AN2728 has shown potent activity in vivo and in vitro, and the anti-inflammatory properties of AN2728 are being investigated. Also used as pharmaceutical intermediates. Biologically active Crisaborole (AN2728) is a selective small molecule PDE4 inhibitor with broad-spectrum anti-inflammatory activity.