Apremilast is a small-molecule immunomodulator that acts as a selective phosphodiesterase 4 (PDE4) inhibitor. It is used for the treatment of inflammatory conditions such as psoriatic arthritis, plaque psoriasis, and oral ulcers in Behçet’s disease. By inhibiting PDE4, apremilast increases intracellular cyclic AMP (cAMP) levels, thereby downregulating pro-inflammatory mediators like TNF-α, IL-17, IL-23, and increasing anti-inflammatory cytokines such as IL-10.
It is administered orally, offering a non-biologic, systemic treatment option for chronic inflammatory diseases.
Indications include:
∙ Psoriatic arthritis
∙ Moderate to severe plaque psoriasis
∙ Oral ulcers associated with Behçet’s disease
Parent: Apremilast
Parent: Apremilast
Parent: Apremilast
Parent: Apremilast
Parent: Gefitinib / Apremilast
Parent: Apremilast
Impurities in apremilast arise from its multi-step chemical synthesis, which involves amide bond formation, aryl nitration, and chiral resolution, and from degradation under light, oxidative, or hydrolytic conditions. Given its long-term use in chronic inflammatory diseases, impurity limits must comply with ICH Q3A/B, USP, and EMA standards.
Process-Related Impurities
Degradation Impurities
Elemental Impurities
Analytical Techniques for Impurity Detection
Apremilast is used to treat psoriatic arthritis, moderate-to-severe plaque psoriasis, and oral ulcers from Behçet’s disease, by modulating the body’s inflammatory response.
It inhibits PDE4, increasing cAMP levels, which suppresses production of pro-inflammatory cytokines and promotes anti-inflammatory pathways.
No. Apremilast is a small-molecule oral drug, offering an alternative to injectable biologic therapies.
Yes, but it is sensitive to light and humidity. It should be stored in a cool, dry place in its original packaging, away from direct sunlight and moisture.
