Everolimus and Lenacapavir: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Lenacapavir
Everolimus
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased everolimus exposure
Interaction Deep Dive
Coadministration of everolimus with lenacapavir (dual moderate CYP3A4 and P-gp inhibitor) may have the potential for elevated everolimus exposure. If concurrent therapy is necessary in patients with breast cancer, progressive neuroendocrine tumors of pancreatic origin, renal cell carcinoma, or renal angiomyolipoma with tuberous sclerosis complex (TSC), reduce the everolimus dosage to 2.5 mg/day. Resume dosage administered prior to inhibitor initiation, once the inhibitor is discontinued for 3 days. If the combination is tolerated, consider increasing the everolimus dosage to 5 mg/day. In patients with TSC-associated subependymal giant cell astrocytoma or partial-onset seizures, reduce the everolimus dosage by 50%; for patients already receiving the lowest available strength, administer everolimus every other day. Assess the everolimus trough concentrations 2 weeks after initiating or discontinuing the inhibitor. When the inhibitor is discontinued, resume the everolimus dosage used prior to initiating the inhibitor after a washout period of 3 days1. Lenacapavir may increase the exposure of drugs primarily metabolized by CYP3A, initiated within 9 months after the last dose of lenacapavir, which may also increase the potential risk of adverse reactions 3. If concurrent therapy is necessary in transplant recipients, closely monitor everolimus levels 2.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of everolimus; inhibition of P-gp mediated efflux transport of everolimus
Literature reports
3 reports — tap to read
a) Coadministration of everolimus with verapamil in healthy subjects (N=16) increased everolimus Cmax by 1.3-fold and AUC by 2.5-fold, as compared with everolimus administered alone 4.
b) Multiple-dose administration of 500 mg erythromycin 3 times daily for 5 days to 16 healthy volunteers significantly increased everolimus Cmax, AUC, and half-life by 2-fold, 4.4-fold, and 39%, respectively, when coadministered with 2 mg everolimus 2.
c) Multiple-dose administration of 80 mg verapamil (CYP3A4 inhibitor and a P-gp substrate) 3 times daily for 5 days to 16 healthy volunteers significantly increased everolimus Cmax and AUC by 2.3-fold and 3.5-fold, respectively, when coadministered with 2 mg everolimus. Everolimus half-life was not changed 2.
Common questions
Can I take Everolimus and Lenacapavir together?
Increased everolimus exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Everolimus and Lenacapavir interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Everolimus or Lenacapavir need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (4)
- Product Information: AFINITOR® oral tablets, everolimus oral tablets. Novartis Pharmaceuticals Corporation, East Hanover, NJ, 2026. DailyMed
- Product Information: ZORTRESS(R) oral tablets, everolimus oral tablets. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2023. DailyMed
- Product Information: YEZTUGO(R) oral tablets, subcutaneous injection, lenacapavir oral tablets, subcutaneous injection. Gilead Sciences Inc (per manufacturer), Foster City, CA, 2025. DailyMed
- Product Information: COVERA-HS(R) oral extended release tablets, verapamil HCl oral extended release tablets. G.D. Searle LLC (per FDA), New York, NY, 2017. DailyMed
Keep reading about Lenacapavir
Keep reading about Everolimus
These medications also interact with supplements
Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
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