Apremilast
Apremilast. PDE4 inhibitor — raises cellular cAMP → reduced inflammatory cytokine release. Oral approval for psoriasis + psoriatic arthritis +… Oral half-life 8 h.
PDE4 inhibitor — raises cellular cAMP → reduced inflammatory cytokine release. Oral approval for psoriasis + psoriatic arthritis + Behçet syndrome. Modest efficacy + cleaner side-effect profile (no infection / malignancy risk) than biologics.
PK: EVERY NUMBER IS UNSOURCED AND EVERY NUMBER IS RIGHT, which is worth recording as carefully as a defect. A search for an apremilast volume of distribution returns COUNT 0, and the only published 73% sits in the introduction of a RAT formulation study restating the label, which would launder a label figure through a rodent paper and is deliberately not cited. But the stored triple reproduces real human exposure: {V 87, F 0.73, t-half 8} imply CL/F 10.33 L/h against a verbatim "Mean C(max), AUC(0-inf) and t(max) values for apremilast in plasma were 333 ng/mL, 1970 ng*h/mL and 1.5 h" after 20 mg, which is 10.15 L/h. A 1.7% agreement. The half-life is the LOWER bound of a printed "8-9 h" and no better point value exists. The analyte question closes cleanly, as predicted: "The major metabolites were at least 50-fold less pharmacologically active than apremilast", so the parent is right.
Pharmacokinetics
- Oral — t½ 8 h · F 73% · ka 0.92 h⁻¹ · Vd 87 L
Sources: PMID:33932093, PMID:24882690, PMID:21859393