Pharmacodynamic assessment of apremilast for the treatment of moderate-to-severe plaque psoriasis

Expert Opin Drug Metab Toxicol. 2016 Sep;12(9):1121-8. doi: 10.1080/17425255.2016.1206886. Epub 2016 Jul 14.

Abstract

Introduction: Psoriasis is a chronic inflammatory skin disease affecting 2-3% of the population. Certain systemic drugs currently available for its treatment could be associated, in the long term, with organ toxicity and adverse events, thus, clinical monitoring throughout treatment is required. Moreover, tolerability issues, parenteral administration, and barriers to patient access, such as high cost and specialist management lead to treatment failure.

Areas covered: Apremilast is an oral small molecule inhibitor of phosphodiesterase 4 (PDE4i). PDE is the major enzyme class responsible for the hydrolysis of cyclic adenosine monophosphate in immune cells (cAMP). With PDE4 inhibition, apremilast works intracellularly to modulate pro-inflammatory and anti-inflammatory mediator production critically involved in psoriasis. The aim of this paper is to focus the attention on apremilast pharmacodynamics effects, its efficacy and safety in treating moderate-to-severe plaque psoriasis.

Expert opinion: Apremilast is an effective and well-tolerated option in treating moderate-to-severe plaque psoriasis. Its safety profile and the oral administration offer significant advantages in prescribing apremilast for the treatment of psoriasis, particularly in some subsets of patients.

Keywords: Apremilast; oral therapy; phosphodiesterase-4-inhibitor; psoriasis; small molecule.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / adverse effects
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
  • Humans
  • Inflammation / drug therapy
  • Inflammation / pathology
  • Inflammation Mediators / metabolism
  • Phosphodiesterase 4 Inhibitors / adverse effects
  • Phosphodiesterase 4 Inhibitors / pharmacology
  • Phosphodiesterase 4 Inhibitors / therapeutic use*
  • Psoriasis / drug therapy*
  • Psoriasis / pathology
  • Severity of Illness Index
  • Thalidomide / adverse effects
  • Thalidomide / analogs & derivatives*
  • Thalidomide / pharmacology
  • Thalidomide / therapeutic use

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Inflammation Mediators
  • Phosphodiesterase 4 Inhibitors
  • Thalidomide
  • apremilast