Clopidogrel, a CYP2C8 inhibitor, causes a clinically relevant increase in the systemic exposure to the active metabolite of selexipag in healthy subjects

LN Axelsen, I Poggesi, F Rasschaert… - British Journal of …, 2021 - Wiley Online Library
Selexipag is a prostacyclin … in the metabolism of selexipag and its active metabolite,
ACT-333679. This study evaluated the interaction of selexipag and clopidogrel, a CYP2C8 inhibitor. …

The metabolism and drug–drug interaction potential of the selective prostacyclin receptor agonist selexipag

C Gnerre, J Segrestaa, S Seeland, P Äänismaa… - Xenobiotica, 2018 - Taylor & Francis
… the active metabolite ACT-333679 is catalysed by carboxylesterases, while the oxidation and
dealkylation reactions are metabolized by CYP2C8 … The potential of selexipag to inhibit or …

Clinical evaluation of drug–drug interactions between the cytochrome P450 substrates selexipag and clopidogrel in Japanese volunteers

N Katayama, K Odagiri, A Hakamata… - British Journal of …, 2021 - Wiley Online Library
… on the pharmacokinetics of selexipag and its active metabolite and suggested that … the effect
of clopidogrel, an inhibitor of CYP2C8, on the PK of selexipag and ACT-33367 in Japanese …

Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects

S Bruderer, M Petersen‐Sylla… - British Journal of …, 2017 - Wiley Online Library
… (CYP) 2C8 is involved in the metabolism of selexipag and its active metabolite, ACT-333679.
The … of selexipag with gemfibrozil, a strong CYP2C8 inhibitor, and rifampicin, an inducer of …

Effect of quercetin on the pharmacokinetics of selexipag and its active metabolite in beagles

S Luo, E Gu, Y Chen, S Zhou, C Fan… - Pharmaceutical Biology, 2022 - Taylor & Francis
CYP2C8, selexipag is a strong inhibitor of CYP2C8 at the same time. Meanwhile, CYP2C8
is an extent inhibited … primarily by CYP2C8 and may compete with selexipag for CYP2C8. In …

Effect of lopinavir/ritonavir on the pharmacokinetics of selexipag an oral prostacyclin receptor agonist and its active metabolite in healthy subjects

P Kaufmann, S Niglis, S Bruderer… - British Journal of …, 2015 - Wiley Online Library
… that CYP2C8 and CYP3A4 are involved in the metabolism of … of selexipag and its metabolites
in animals and humans 24, subjects administered selexipag concomitantly with inhibitors

[HTML][HTML] Drug-drug interactions in the management of patients with pulmonary arterial hypertension

S Wu, HB Hoang, JZ Yang, DG Papamatheakis… - Chest, 2022 - Elsevier
… pathway bypass significant liver metabolism and avoid drug interactions, selexipag and
oral treprostinil may exhibit interactions with CYP2C8 inhibitors such as gemfibrozil and …

Pharmacokinetic drug evaluation of selexipag for the treatment of pulmonary arterial hypertension

M Sardana, M Moll, HW Farber - … Opinion on Drug Metabolism & …, 2016 - Taylor & Francis
Selexipag and its active metabolite do not activate or inhibit the P450 enzyme system, but
concomitant use of CYP2C8 inhibitors (eg gemfibrozil) with selexipag … high levels of selexipag […

Contribution of human liver and intestinal carboxylesterases to the hydrolysis of selexipag in vitro

S Imai, T Ichikawa, C Sugiyama, K Nonaka… - Journal of …, 2019 - Elsevier
… PGI 2 and its analogs act as potent vasodilators and inhibit platelet aggregation via the PGI
… and MRE-269 are converted into several metabolites by recombinant CYP2C8 and CYP3A4, …

Simultaneous quantification and pharmacokinetic investigation of selexipag and its main metabolite ACT-333679 in rat plasma by UPLC-MS/MS method

S Xie, L Shi, J Chen, R Xu, X Ye - Journal of Pharmaceutical and …, 2020 - Elsevier
… study between a strong CYP2C8 inhibitor gemfibrozil and selexipag with ACT-333679 has …
for the simultaneous detection of selexipag as well as its metabolite ACT-333679 in biological …