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Drug Interactions between brincidofovir and saquinavir

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

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Interactions between your drugs

Major

saquinavir brincidofovir

Applies to: saquinavir and brincidofovir

GENERALLY AVOID: Coadministration with inhibitors of the hepatic influx transporters organic anion transporting polypeptides (OATP) 1B1 and 1B3 may increase the plasma concentrations and adverse effects of brincidofovir. In clinical studies, coadministration with a single 600 mg oral dose of the OATP1B1 and 1B3 inhibitor cyclosporine increased the mean systemic exposure (AUC) and peak plasma concentration (Cmax) of brincidofovir by 374% and 269%, respectively.

MANAGEMENT: The manufacturer advises that, where possible, coadministration of brincidofovir with OATP1B1 or 1B3 inhibitors should be avoided and alternative medicines considered. However, if concomitant use is necessary, administration of the OATP1B1 or 1B3 inhibitor should be postponed by at least 3 hours after the administration of brincidofovir. Patients should also be closely monitored for brincidofovir-related adverse reactions such as elevations in hepatic transaminases and bilirubin, diarrhea, nausea, vomiting, and abdominal pain.

References (1)
  1. (2022) "Product Information. Tembexa (brincidofovir)." Chimerix, Inc.

Drug and food interactions

Moderate

saquinavir food

Applies to: saquinavir

ADJUST DOSING INTERVAL: Food significantly increases the absorption of saquinavir.

MONITOR: Coadministration with grapefruit juice may increase the plasma concentrations of saquinavir. The primary mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. In eight healthy volunteers, ingestion of 400 mL of grapefruit juice prior to administration of a 600 mg dose of saquinavir mesylate increased the area under the plasma concentration-time curve and oral bioavailability of saquinavir by 50% and 100%, respectively, compared to water; however, the increase is not considered clinically relevant. A high degree of intersubject variability in the grapefruit juice effect was also observed. The extent to which this interaction may occur with the saquinavir free base soft gelatin capsule is unknown. However, the saquinavir soft gelatin capsule formulation is no longer commercially available.

MANAGEMENT: Saquinavir mesylate should be taken with meals or within 2 hours after eating to enhance bioavailability. Patients should be advised to avoid the consumption of large amounts of grapefruit and grapefruit juice during saquinavir therapy unless otherwise directed by their doctor, as the interaction is unreliable and subject to a high degree of interpatient variation.

References (6)
  1. (2001) "Product Information. Invirase (saquinavir)." Roche Laboratories
  2. Kupferschmidt HHT, Fattinger KE, Ha HR, Follath F, Krahenbuhl S (1998) "Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man." Br J Clin Pharmacol, 45, p. 355-9
  3. Bailey DG, Malcolm J, Arnold O, Spence JD (1998) "Grapefruit juice-drug interactions." Br J Clin Pharmacol, 46, p. 101-10
  4. Eagling VA, Profit L, Back DJ (1999) "Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-I protease inhibitor saquinavir by grapefruit juice components." Br J Clin Pharmacol, 48, p. 543-52
  5. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  6. Cerner Multum, Inc. "Australian Product Information."
Moderate

brincidofovir food

Applies to: brincidofovir

ADJUST DOSING INTERVAL: Administration with food decreases the oral bioavailability of brincidofovir. According to the product labeling, administration of brincidofovir tablets with a low-fat meal (approximately 400 calories, 25% of calories from fat) was associated with a reduction in the systemic exposure (AUC) and peak plasma concentration (Cmax) of brincidofovir by 31% and 49%, respectively, compared to administration under fasting. However, no clinically meaningful changes in intracellular concentrations of cidofovir diphosphate were observed. The effect of food on the oral suspension formulation has not been evaluated.

MANAGEMENT: Brincidofovir oral tablets and suspension should be taken on an empty stomach. If necessary, the oral tablets may be taken with a low-fat meal.

References (1)
  1. (2022) "Product Information. Tembexa (brincidofovir)." Chimerix, Inc.

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.


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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.