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Drug Interactions between saquinavir and Scemblix

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

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Interactions between your drugs

Moderate

saquinavir asciminib

Applies to: saquinavir and Scemblix (asciminib)

MONITOR: Coadministration with potent inhibitors of CYP450 3A4 may increase the plasma concentrations of asciminib. According to the prescribing information, asciminib is metabolized by CYP450 3A4-mediated oxidation and uridine diphosphate glucuronosyl transferase (UGT) 2B7- and 2B17-mediated glucuronidation. When a single 40 mg dose of asciminib was coadministered with clarithromycin, a potent CYP450 3A4 inhibitor, asciminib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 19% and 36%, respectively. Coadministration of asciminib 200 mg twice daily and clarithromycin is predicted to increase asciminib Cmax and AUC by 49% and 77%, respectively, per physiologically-based pharmacokinetic (PBPK) models. However, no clinically significant differences in the pharmacokinetics of asciminib were observed when coadministered with itraconazole, another potent CYP450 3A4 inhibitor.

MANAGEMENT: Caution is advised when asciminib is prescribed with potent CYP450 3A4 inhibitors, particularly at higher dosages. The manufacturer recommends that patients treated with asciminib at 200 mg twice daily be monitored closely for adverse reactions, such as nausea, diarrhea, rash, myelosuppression, pancreatitis, hypertension, and cardiovascular toxicity including ischemic cardiac conditions, arterial thrombotic and embolic conditions, cardiac failure, QT prolongation, and arrhythmia.

References (1)
  1. (2021) "Product Information. Scemblix (asciminib)." Novartis Pharmaceuticals

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

asciminib food

Applies to: Scemblix (asciminib)

ADJUST DOSING INTERVAL: Food may reduce the oral bioavailability of asciminib. When a single 40 mg dose of asciminib was administered with a low-fat meal (400 calories; 25% fat) in healthy volunteers, asciminib peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 35% and 30%, respectively, compared to asciminib administered in the fasted state. Administration with a high-fat meal (1000 calories; 50% fat) decreased the Cmax and AUC of asciminib by 68% and 62%, respectively.

MANAGEMENT: To ensure adequate asciminib exposures, food consumption should be avoided for at least 2 hours before and 1 hour after taking asciminib.

References (2)
  1. (2021) "Product Information. Scemblix (asciminib)." Novartis Pharmaceuticals
  2. (2022) "Product Information. Scemblix (asciminib)." Novartis Pharmaceuticals UK Ltd, Scemblix 20 mg film-

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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