Piclamilast

Piclamilast (also known as RP-73,401) is a selective PDE4 inhibitor developed by Rhône-Poulenc Rorer, a French pharmaceutical company. It is a second-generation PDE4 inhibitor, which means it is more selective and has fewer side effects than first-generation PDE4 inhibitors. Piclamilast has been studied for its potential use in the treatment of conditions such as COPD, Asthma, and IBD.

Pharmacology

Piclamilast works by inhibiting the action of the enzyme PDE4. This enzyme is involved in the breakdown of cAMP, a molecule that plays a key role in many biological processes, including inflammation. By inhibiting PDE4, Piclamilast increases the levels of cAMP, which in turn reduces inflammation.

Clinical Trials

Several clinical trials have been conducted to evaluate the efficacy and safety of Piclamilast in various conditions. In a Phase II trial for COPD, Piclamilast showed a significant improvement in lung function and a reduction in symptoms. However, in a Phase III trial for asthma, the drug did not meet the primary endpoint.

Side Effects

The most common side effects of Piclamilast are gastrointestinal, including nausea, vomiting, and diarrhea. These side effects are generally mild and tend to decrease over time. Other side effects may include headache, dizziness, and fatigue.

Development and Market

Piclamilast was developed by Rhône-Poulenc Rorer in the 1990s. Despite showing promise in early clinical trials, the development of the drug was discontinued due to lack of efficacy in later trials. As of now, Piclamilast is not marketed in any country.

See Also

• Phosphodiesterase-4 inhibitor
• Chronic obstructive pulmonary disease
• Asthma
• Inflammatory bowel disease