Comparative Pharmacology
Head-to-head clinical analysis: ASCLERA versus MACITENTAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASCLERA versus MACITENTAN.
ASCLERA vs MACITENTAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
ASCLERA (corticotropin) is a proopiomelanocortin (POMC) analog that stimulates the adrenal cortex to release cortisol, corticosterone, and aldosterone, increasing corticosteroid levels. It also has immunomodulatory and anti-inflammatory effects mediated through melanocortin receptors.
Endothelin receptor antagonist (ERA) that blocks the binding of endothelin-1 (ET-1) to ETA and ETB receptors, thereby inhibiting vasoconstriction and smooth muscle proliferation.
Adults: 240 mg/m2 intravenously over 2 hours on day 1 of each 21-day cycle.
10 mg orally once daily.
None Documented
None Documented
Terminal elimination half-life is 12-15 hours. In patients with moderate-to-severe renal impairment (CrCl < 30 mL/min), half-life may increase to 30-40 hours, requiring dose adjustment.
Clinical Note
moderateMacitentan + Methylphenidate
"Macitentan may decrease the antihypertensive activities of Methylphenidate."
Clinical Note
moderateMacitentan + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Macitentan."
Clinical Note
moderateMacitentan + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Macitentan."
Clinical Note
moderateMacitentan + Cyclosporine
Terminal elimination half-life is 11–22 hours in healthy subjects; in pulmonary arterial hypertension patients, mean half-life is approximately 13 hours.
Renal excretion of unchanged drug accounts for 60-70% of administered dose; fecal/biliary elimination contributes 20-30%.
Biliary/fecal (major, 93% as metabolites) and renal (3% unchanged, <5% of dose in urine).
Category C
Category D/X
Endothelin Receptor Antagonist
Endothelin Receptor Antagonist
"The metabolism of Cyclosporine can be decreased when combined with Macitentan."