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.
Clin PharmacokinetAug 29, 2026 (epub)
David Nguyen, Xiaohui Tracey Wei, Xianzhang Meng et al.
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In 30 seconds
This Phase I trial assessed the impact of rivoceranib 200 mg once daily on the pharmacokinetics of various cytochrome P450 substrates in 18 healthy volunteers. The study found that rivoceranib significantly increased the AUC for dextromethorphan by 2.67-fold, indicating substantial inhibition of CYP2D6 metabolism, while also affecting other CYP substrates.
Key findings
- Rivoceranib decreased caffeine AUC 0-inf by 20% and C max by 7%.
- S-warfarin AUC 0-inf increased by 1.35-fold and C max by 1.05-fold.
- Omeprazole AUC 0-inf increased by 2.06-fold and C max by 1.64-fold.
- Dextromethorphan AUC 0-inf increased by 2.67-fold and C max by 1.9-fold.
Why it matters
Understanding the drug-drug interactions involving rivoceranib is crucial for clinicians, as it may necessitate dose adjustments for CYP substrate medications to avoid adverse effects and ensure patient safety.