Comparative Pharmacology
Head-to-head clinical analysis: SELEXIPAG versus UPTRAVI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SELEXIPAG versus UPTRAVI.
SELEXIPAG vs UPTRAVI
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective agonist of the prostacyclin (IP) receptor, causing vasodilation and inhibition of platelet aggregation via increased cAMP levels.
Uptravi (selexipag) is a prostacyclin receptor (IP receptor) agonist. Selexipag and its active metabolite, ACT-333679, selectively bind to the IP receptor, leading to vasodilation, inhibition of platelet aggregation, and antiproliferative effects on smooth muscle cells.
Oral, starting dose 200 mcg twice daily, titrated in increments of 200 mcg twice daily at weekly intervals as tolerated to a maximum of 1600 mcg twice daily.
Initial dose 200 mcg orally twice daily, titrated in increments of 200 mcg twice daily at weekly intervals to a maximum of 1600 mcg twice daily.
None Documented
None Documented
Clinical Note
moderateSelexipag + Tranilast
"Selexipag may increase the anticoagulant activities of Tranilast."
Clinical Note
moderateSelexipag + Resveratrol
"Selexipag may increase the anticoagulant activities of Resveratrol."
Clinical Note
moderateSelexipag + Teriflunomide
"The serum concentration of Teriflunomide can be increased when it is combined with Selexipag."
Clinical Note
moderateSelexipag + Nimesulide
"Selexipag may increase the anticoagulant activities of Nimesulide."
Terminal elimination half-life is approximately 6–8 hours following intravenous administration; with oral administration, the effective half-life is ~6–9 hours due to enterohepatic recirculation; clinical context: dosing every 6 hours is required to maintain therapeutic plasma concentrations.
Terminal elimination half-life is approximately 7–9 hours in healthy subjects, but prolonged in patients with hepatic impairment (Child-Pugh class A: ~11 hours; class B: ~16 hours). Steady-state is reached within 2–4 days of twice-daily dosing.
Primarily hepatic metabolism (approximately 97% of dose) via CYP2C8 and CYP3A4; biliary/fecal excretion of metabolites accounts for ~77% of total clearance; renal excretion <1% as unchanged drug.
Primarily hepatic metabolism; renal excretion of unchanged drug is <1%. Fecal excretion accounts for approximately 70% of total elimination, mainly as metabolites. Biliary excretion contributes to fecal elimination.
Category C
Category C
Prostacyclin Receptor Agonist
Prostacyclin Receptor Agonist