Effect of Rivoceranib 200 mg Once Daily on the Pharmacokinetics of a Cocktail Probe Substrate of Cytochrome P450 Enzymes: A Phase I Trial in Healthy Volunteers
Aug 2026· Clinical Pharmacokinetics· Vol 65, pp. 1565 - 1574· 0 citations· 32 references
Medicine
TL;DR
Rivoceranib 200 mg QD may substantially inhibit the metabolism of CYP2D6 substrates, and concomitant use of CYP2D6 substrate drugs with rivoceranib should be approached with caution, and dose adjustment of substrates of CYP2D6 may be necessary when co-administration cannot be avoided.
Savolitinib is an oral, potent, selective CNS‐penetrant MET‐tyrosine kinase inhibitor that in vitro studies indicate is metabolized by cytochrome P450 (CYP) enzymes, including CYP1A2, and by non‐CYP enzymes, such as aldehyde oxidase (AO). Savolitinib primary metabolites, M2 and M3, are formed mainly by CYP1A2 and AO, r...
Kowser Miah, Jitendar Reddy, Pradeep Sharma et al.· Pharmacology Research & Pers...· 0 citations
Cendakimab had no clinically meaningful effects on cytochrome P450 enzyme activities and was generally safe and well tolerated with or without probe substrates in adults with active eosinophilic esophagitis.
Pei-Jin Zhang, C. Charriez, Bindu Murthy et al.· Clinical and Translational S...· 0 citations
BV100 is a mild/weak CYP3A enzyme inducer and a mild substrate for CYP3A inhibitors, however, co-administration with strong CYP3A inhibitors resulted in a disproportionate increase in exposure to the active metabolite 25-O-desacetyl rifabutin, leading to an ∼2-fold increase in total active-moiety exposure.
Pierre Delique, C. Kemmer, Lisa Husband et al.· Journal of Antimicrobial Che...· 0 citations
AIMS
Aildenafil citrate, an orally bioavailable phosphodiesterase type 5 (PDE5) inhibitor, is primarily metabolized by cytochrome P450 3A4 (CYP3A4). This study aimed to assess potential pharmacokinetic interactions between aildenafil citrate tablets and cytochrome P450 (CYP)3A modulators.
METHODS
This study involved...
Ran Xie, Nan Zhao, B. Jia et al.· British Journal of Clinical...· 0 citations
The authors' model predicts that ceritinib co-administration substantially elevates rivaroxaban exposure and exploratory major bleeding risk, and predicts model-predicted dosing strategies comparable to standard monotherapy.
Jian-Wei Ren, Yi-Yao Li, Xin Zheng et al.· European Journal of Pharmaco...· 0 citations
BACKGROUND
Direct oral anticoagulants such as rivaroxaban are a feasible and convenient option for anticoagulation in people living with HIV. Here, we assess the effect of cobicistat or darunavir/cobicistat on the pharmacokinetics (PK), pharmacodynamics (PD), and safety of rivaroxaban.
METHODS
This open-label, fixed...
Lilian W. Adeojo, Cheryl Pauls, Doris Z. Swaim et al.· Journal of Acquired Immune D...· 0 citations
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