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Drug Interactions between Pomalyst and saquinavir

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

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Interactions between your drugs

Moderate

saquinavir pomalidomide

Applies to: saquinavir and Pomalyst (pomalidomide)

GENERALLY AVOID: Coadministration with potent inhibitors of CYP450 1A2, CYP450 3A4, and P-glycoprotein may increase the plasma concentrations of pomalidomide, which has been shown to be primarily metabolized by these isoenzymes and also a substrate of the efflux transporter. Pomalidomide exposure is increased when given with a strong CYP450 1A2 inhibitor (e.g., fluvoxamine) in the presence of a strong CYP450 3A4 and P-gp inhibitor (e.g., ketoconazole). Coadministration with ketoconazole alone did not have a clinically significant effect on exposure to pomalidomide. However, the combination of pomalidomide and fluvoxamine in the presence of ketoconazole increased exposure to pomalidomide by 104% compared to pomalidomide plus ketoconazole.

MANAGEMENT: The use of pomalidomide with potent inhibitors of CYP450 1A2 (e.g., ciprofloxacin, fluvoxamine, tiabendazole) in the presence of strong CYP450 3A4 and P-gp inhibitors should generally be avoided. If coadministration is considered clinically necessary, the pomalidomide dose should be reduced by 50%. Dose reduction may also be required if pomalidomide is given with a strong inhibitor of CYP450 1A2 in the absence of a coadministered CYP450 3A4 and P-gp inhibitor. Patients should be monitored for occurrence of pomalidomide-related side effects, including nausea, diarrhea, and neutropenia.

References (3)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2013) "Product Information. Pomalyst (pomalidomide)." QLT Phototherapeutics 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

pomalidomide food

Applies to: Pomalyst (pomalidomide)

MONITOR: Cigarette smoking may reduce pomalidomide exposure due to induction of CYP450 1A2, the isoenzyme that is responsible for the metabolic clearance of pomalidomide along with CYP450 3A4.

MANAGEMENT: Patients should be advised that smoking may reduce the efficacy of pomalidomide therapy. Pomalidomide should be taken on an empty stomach, at least 2 hours before or 2 hours after a meal.

References (1)
  1. (2013) "Product Information. Pomalyst (pomalidomide)." QLT Phototherapeutics 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

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