Apalutamide with Lopinavir Interaction Details
Brand Names Associated with Apalutamide
- Apalutamide
- Erleada®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Decreased efficacy of lopinavir; increased exposure of apalutamide
Interaction Summary
Concomitant use of apalutamide and a strong CYP3A4 inhibitor such as lopinavir/ritonavir may increase the exposure of apalutamide[1]. Coadministration of lopinavir (a CYP3A substrate) with apalutamide (a strong CYP3A inducer) is contraindicated; significantly reduced lopinavir plasma concentrations may be associated with the potential for loss of virologic response and possible resistance and cross-resistance [2].
Severity
Contraindicated
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of apalutamide and a strong CYP3A4 inhibitor such as lopinavir/ritonavir may increase the exposure of apalutamide[1]. Coadministration of lopinavir (a CYP3A substrate) with apalutamide (a strong CYP3A inducer) is contraindicated; significantly reduced lopinavir plasma concentrations may be associated with the potential for loss of virologic response and possible resistance and cross-resistance [2].
Mechanism Of Interaction
Induction of CYP3A-mediated lopinavir metabolism by apalutamide; inhibition of CYP3A4-mediated metabolism of apalutamide by lopinavir/ritonavir
Literature Reports
A) Coadministration of a single dose of apalutamide 240 mg with itraconazole (strong CYP3A4 inhibitor) resulted in a decreased of 22% in the apalutamide Cmax of while the AUC did not change [1]. Lopinavir/ritonavir is a strong CYP3A4 inhibitor [2].
B) Coadministration of a single dose of apalutamide with ketoconazole (strong CYP3A4 inhibitor) is predicted to increase the apalutamide AUC by 24% but have no affect on Cmax. At steady state, ketoconazole is expected to increase the apalutamide Cmax by 38% and AUC by 51%. For the active moieties, the predicted apalutamide steady-state Cmax increased by 23% and AUC by 28% [1]. Lopinavir/ritonavir is a strong CYP3A4 inhibitor [2].
References
1 ) Product Information: Erleada(TM) oral tablets, apalutamide oral tablets. Janssen Products, LP (per FDA), Horsham, PA, 2018.
2 ) Product Information: KALETRA(R) oral tablets, oral solution, lopinavir ritonavir oral tablets, oral solution. AbbVie Inc (per FDA), North Chicago, IL, 2019.
Apalutamide Overview
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Apalutamide is used to treat certain types of prostate cancer (cancer in men that begins in the prostate [a male reproductive gland]) and has spread to other parts of the body or that has not spread to other parts of the body but has not been helped by other medical treatments. Apalutamide is in a class of medications called androgen receptor inhibitors. It works by blocking the effects of androgen (a male reproductive hormone) to stop the growth and spread of cancer cells.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.