Related Experiment Video
Updated: Jul 19, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Cilomilast: orally active selective phosphodiesterase-4 inhibitor for treatment of chronic obstructive pulmonary
Shaunta' D Martina1, Maha S Ismail, Kimi S Vesta
1College of Pharmacy, University of Oklahoma, Oklahoma City, OK 73190-5040, USA.
Objective:
To review available literature evaluating the pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of cilomilast, a selective phosphodiesterase-4 (PDE4) inhibitor.
Data Sources:
Literature was accessed through MEDLINE (1966-May 2006), Current Contents Clinical Medicine (1998-May 2006), and The Cochrane Library Database (1st quarter 2006) using the terms cilomilast, Ariflo, and SB 207 499. Reference lists from retrieved articles and information from the manufacturer were manually reviewed.
Study Selection And Data Extraction:
All clinical trials evaluating cilomilast and published in English were included in this review. In addition, articles evaluating the pharmacology, pharmacokinetics, and safety of cilomilast in humans were reviewed.
Data Synthesis:
Cilomilast is a second-generation PDE4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with chronic obstructive pulmonary disease (COPD). Selective PDE4 inhibition is proposed to maximize the antiinflammatory effects of PDE inhibition while minimizing the adverse effects of nonselective agents. To date, 4 clinical trials have evaluated the efficacy of cilomilast and demonstrated improvement in lung function (forced expiratory volume in 1 second) and quality of life and reduction in the occurrence of COPD exacerbations compared with placebo. Cilomilast is generally well tolerated, with adverse effects being overall mild and self-limiting.
Conclusions:
COPD is a progressive disease, and available treatment options provide limited efficacy. Given its unique mechanism of action and improved adverse effect profile compared with previous agents, cilomilast may have a promising role for the management of COPD.
Related Concept Videos
Antiasthma Drugs: Leukotriene Modifiers
Leukotriene modifiers work through two distinct mechanisms:
COPD: Management Using Bronchodilators and Corticosteroids
Chronic Obstructive Pulmonary Disease-V: Management
Smoking Cessation
Antiasthma Drugs: Muscarinic Receptor Antagonists
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
Antiasthma Drugs: Methylxanthines
Theophylline is thought to inhibit phosphodiesterase enzymes, increasing intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). This rise in cAMP and cGMP concentrations stimulates cardiac function,...
Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs
Mast cell stabilizers, such as cromolyn (also known as sodium cromoglycate) and nedocromil (Tilade), are effective drugs in asthma management. These stabilizers hinder histamine release by skillfully obstructing the activation of mast cells and other cellular entities. Notably, they navigate this task without...