克立硼罗的药理作用与临床评价

Introduction: Crisaborole is a new non-steroidal topical ointment that exerts anti-inflammatory effects by inhibiting phosphodiesterase 4 (PDE4). The increased PDE4 activity in inflammatory cells in atopic dermatitis can lead to lower intracellular cyclic adenosine monophosphate (CAMP) levels than normal people and the production of inflammatory cytokines.

Criborole R&D Company

It is an ointment developed by Anacor Pharmaceuticals in the United States. It can treat allergic dermatitis. It was approved by the FDA on December 14, 2016. Criborole, sold under the trade name Eucrisa and others, is a nonsteroidal topical drug used to treat mild to moderate atopic dermatitis in adults and children. The most common side effect of criborole is local reaction at the administration site. Criborole is a phosphodiesterase 4 inhibitor, and its specific mechanism of action in atopic dermatitis is unknown.

Pharmacological effects

Criborole is a phosphodiesterase 4 inhibitor. PDE-4 exists in a variety of immune cells and can reduce intracellular cyclic adenosine monophosphate levels, while cAMP is an important second messenger involved in regulating immune responses and inflammatory processes. By inhibiting PDE-4, criborole can increase the concentration of intracellular cAMP, thereby downregulating the inflammatory response and reducing the production and release of pro-inflammatory cytokines. These cytokines are closely related to the inflammatory response in atopic dermatitis.

In addition, through PDE-4 inhibition, criborole can reduce skin inflammation, including anti-inflammatory and analgesic effects. It can relieve symptoms such as skin redness, swelling and itching caused by an overactive immune system, and help control acute attacks of dermatitis.

Clinical Evaluation

Clinical studies have shown that criborole has a significant effect in treating allergic dermatitis. The average cure rate of 29 days for treating initial, moderate and severe atopic dermatitis is 32%, and it is highly safe. No adverse reactions have been seen in children aged 2 years and above and pregnant women. Criborole is the first new drug approved by the US FDA to treat atopic dermatitis in the past 15 years, providing an important non-steroid alternative therapy for patients with atopic dermatitis.

Precautions

If eczema worsens or skin infection occurs during the use of criborole, or the skin condition does not improve after four weeks of medication, it is recommended that the patient consult a doctor in time and adjust the treatment plan under the guidance of the doctor.