Mechanism of Action

  • Mechanism of Action Video
  • Mechanism of Action Diagram
  • Moa Quiz

Learn more about the intracellular mechanism of action of Otezla® (apremilast) in the video below.

Otezla is an oral, non-biologic inhibitor of PDE41

Phosphodiesterase 4 (PDE4) has been shown to be present within inflammatory cells2-7

The role of PDE4 and cAMP in controlling inflammation

learn about the role of PDE4 and cAMP in controlling inflammation

Inflammatory cell

Visual representation based on preclinical evidence

  • Cyclic adenosine monophosphate (cAMP) is a second messenger for a variety of inflammatory mediators2,4-6
  • PDE4 is a cAMP-specific PDE that has been shown to degrade cAMP to AMP in inflammatory cells2-5,7
  • The balance between cAMP and AMP within a cell may modulate the expression of pro-inflammatory and anti-inflammatory mediators7

Otezla® (apremilast) inhibits PDE4 intracellularly and has anti-inflammatory properties1,3,5,7

Otezla has a different MOA3

Inflammatory cell

Visual representation based on preclinical evidence

  • By elevating cAMP levels, Otezla is thought to indirectly modulate production of inflammatory mediators3
  • In a phase 2 open-label study, patients with plaque psoriasis treated with Otezla (n = 19) showed decreased2,8:
    • Lesional skin epidermal thickness
    • Expression of pro-inflammatory genes
    • Inflammatory cell infiltration
  • The specific mechanism(s) by which apremilast exerts its therapeutic action in patients with psoriasis is not well defined1

References: 1. Otezla [package insert]. Summit, NJ: Celgene Corporation. 2. Gottlieb AB, Matheson RT, Menter A, et al. J Drugs Dermatol. 2013;12(8):888-897. 3. Schafer PH, Parton A, Capone L, et al. Cell Signal. 2014;26(9):2016-2029. 4. Schett G, Sloan VS, Stevens RM, Schafer P. Ther Adv Musculoskelet Dis. 2010;2(5):271-278. 5. Schafer PH, Parton A, Gandhi AK, et al. Br J Pharm. 2010;159(4):842-855. 6. Moore AR, Willoughby DA. Clin Exp Immunol. 1995;101(3):387-389. 7. Schafer P. Biochem Pharmacol. 2012;83(12):1583-1590. 8. Data on file, Celgene Corporation.

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Indications & Important Safety Information

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