Midazolam and Lenacapavir Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Midazolam
No brand names on recordLenacapavir Injection
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 midazolam exposure
Interaction Deep Dive
Use caution when midazolam is administered concomitantly with lenacapavir (SUNLENCA®)2. Coadministration of lenacapavir (a moderate CYP3A inhibitor) together with midazolam (a sensitive CYP3A substrate) may increase midazolam exposure. 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 21.
Why it happens (mechanism)
Inhibition of CYP3A-mediated metabolism of midazolam
Literature reports
2 reports — tap to read
a) In the interaction studies conducted in subjects without HIV-1, lenacapavir 600 mg twice daily for 2 days and single 600 mg doses were administered with a 2.5 mg single dose of midazolam, a substrate of CYP3A (simultaneous administration, fed). The mean ratio for AUC and Cmax of lenacapavir with and without midazolam were 3.59 (90% CI, 3.3 to 3.91) and 1.94 (90% CI, 1.81 to 2.08) respectively 21.
b) In the interaction studies conducted in subjects without HIV-1, lenacapavir 600 mg twice daily for 2 days and single 600 mg doses were administered with a 2.5 mg single dose of midazolam, a substrate of CYP3A (1 day after lenacapavir, fed) The mean ratio for AUC and Cmax of lenacapavir with and without midazolam were 4.08 (90% CI, 3.77 to 4.41) and 2.16 (90% CI, 2.02 to 2.3) respectively 21.
Common questions
Can I take Midazolam and Lenacapavir Injection together?
Increased midazolam exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Midazolam and Lenacapavir Injection 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 "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Midazolam or Lenacapavir Injection 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 (2)
- 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: SUNLENCA(R) oral tablets, subcutaneous injection, lenacapavir oral tablets, subcutaneous injection. Gilead Sciences Inc (per FDA), Foster City, CA, 2024. DailyMed
Keep reading about Midazolam
Keep reading about Lenacapavir Injection
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.
Check another combination
Our instant two-drug interaction checker is almost here.
Still have questions about this combination?
Every question gets a real answer from a licensed pharmacist — free, and usually within a day.
Ask the pharmacist