Apremilast – Treatment for Psoriasis
Apremilast is a modern oral small-molecule compound that functions as a selective inhibitor of the phosphodiesterase-4 (PDE4) enzyme. The drug belongs to the class of non-biological anti-inflammatory agents and is used for the systemic therapy of chronic immune-mediated inflammatory diseases of the skin and joints.
The mechanism of action of apremilast involves blocking PDE4, which is the dominant enzyme in immune system cells. Inhibition of this enzyme leads to increased levels of intracellular cyclic adenosine monophosphate (cAMP). High concentrations of cAMP, in turn, suppress the production of numerous pro-inflammatory mediators (such as TNF-α, interleukin IL-17, and IL-23) while simultaneously stimulating the synthesis of the anti-inflammatory mediator IL-10. This allows for fine-tuning of the immune response, reducing inflammation without global immunosuppression.
The drug is notable for its convenient tablet form and does not require the continuous laboratory monitoring typically associated with traditional cytostatics or biological agents.
Indications
Apremilast is used in dermatology and rheumatology for the treatment of the following conditions:
- Psoriasis: treatment of adult patients with moderate to severe plaque psoriasis who are candidates for systemic therapy or phototherapy.
- Psoriatic Arthritis: use as monotherapy or in combination with other disease-modifying antirheumatic drugs (DMARDs) in adult patients with active arthritis.
- Behçet's Disease: treatment of oral mucosal ulcers in adult patients with this systemic vasculitis.
- Scalp Psoriasis: therapy for specific disease localizations that are difficult to manage with topical treatments.
Dosage and administration
The apremilast dosing regimen includes a mandatory gradual dose escalation (titration) phase to improve tolerability.
- Treatment Initiation: the dose is gradually increased from 10 mg on Day 1 to the target dose of 30 mg by Day 6.
- Maintenance Dose: 30 mg twice daily (morning and evening), approximately 12 hours apart.
- Administration Rules: tablets are taken orally with or without food and should be swallowed whole, without breaking or chewing.
- Renal Impairment Adjustment: for patients with severe renal impairment (creatinine clearance < 30 mL/min), the dose is reduced to 30 mg once daily.
- Weight Monitoring: regular weight checks are recommended during therapy, as the drug may cause a decrease in body mass.