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Drug Interactions between riociguat and Rukobia

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

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Interactions between your drugs

Moderate

riociguat fostemsavir

Applies to: riociguat and Rukobia (fostemsavir)

MONITOR: Coadministration with fostemsavir may increase the plasma concentrations of drugs that are substrates of the transporters, organic anion transporting polypeptides (OATP) 1B1/1B3 and breast cancer resistance protein (BCRP). Temsavir, the active moiety of fostemsavir, is an inhibitor of OATP 1B1 and 1B3. Additionally, temsavir and two metabolites are inhibitors of BCRP. When a single 10 mg dose of rosuvastatin, an OATP 1B1/1B3 and BCRP substrate, was administered with fostemsavir 600 mg twice daily in 18 study subjects, mean rosuvastatin peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 78% and 69%, respectively, compared to rosuvastatin administered alone.

MANAGEMENT: Caution is advised when fostemsavir is used concurrently with medications that are substrates of OATP 1B1/1B3 and/or BCRP, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever fostemsavir is added to or withdrawn from therapy.

References (3)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2020) "Product Information. Rukobia (fostemsavir)." ViiV Healthcare

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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