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Drug Interactions between lenacapavir and riociguat

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

riociguat lenacapavir

Applies to: riociguat and lenacapavir

MONITOR: Coadministration with lenacapavir may increase the plasma concentrations of drugs that are substrates of the efflux transporters P-glycoprotein (P-gp) and/or breast cancer resistance protein (BCRP). Lenacapavir is an inhibitor of P-gp and BCRP. In pharmacokinetic studies in subjects without HIV, coadministration of oral lenacapavir (600 mg twice daily for 2 days, then single 600 mg dose) with the P-gp substrate tenofovir alafenamide increased the peak plasma concentration (Cmax) and systemic exposure (AUC) of tenofovir alafenamide by 24% and 32%, respectively. In addition, under similar conditions, coadministration of lenacapavir with the BCRP substrate rosuvastatin (single 5 mg dose) led to an increase in rosuvastatin Cmax and AUC by 57% and 31%, respectively. However, these changes for tenofovir alafenamide and rosuvastatin are not reported to be clinically significant.

MANAGEMENT: Caution and monitoring are advised if lenacapavir is used concomitantly with drugs that are substrates of the transporters P-gp and/or BCRP, particularly sensitive substrates, or those with a narrow therapeutic range. Dose adjustments or alternative therapy may be necessary if an interaction is suspected.

References (1)
  1. (2022) "Product Information. Sunlenca (lenacapavir)." Gilead Sciences

Drug and food interactions

Moderate

riociguat food

Applies to: riociguat

ADJUST DOSE: Smoking may decrease the plasma concentrations of riociguat. The proposed mechanism is induction of the CYP450 1A1-mediated metabolism of riociguat by polycyclic aromatic hydrocarbons present in cigarette smoke. CYP450 1A1 is responsible for the formation of the major active metabolite, M1, which has just 1/3 to 1/10 the pharmacologic activity of riociguat. According to the product labeling, plasma concentrations of riociguat are reduced by 50% to 60% in smokers compared to nonsmokers.

MANAGEMENT: Patients should be advised to stop smoking. Riociguat dosages higher than 2.5 mg three times a day may be considered in cigarette smokers, if tolerated, to match the exposure seen in nonsmoking patients. However, safety and effectiveness of higher dosages have not been established. A dosage reduction should be considered in patients who stop smoking during treatment with riociguat. The tablet form of riociguat can generally be taken with or without food. Some authorities recommend not to switch between fed and fasted riociguat intake because of increased peak plasma levels of riociguat in the fasting compared to the fed state.

References (3)
  1. (2013) "Product Information. Adempas (riociguat)." Bayer Pharmaceutical Inc
  2. (2023) "Product Information. Adempas (riociguat)." Merck Sharp & Dohme (UK) Ltd
  3. (2014) "Product Information. Adempas (riociguat)." Bayer Australia Limited

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

See also

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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