Drug Interaction Report

Nateglinide and Apalutamide: Interaction Details

A pharmacist-reviewed analysis of the Nateglinide and Apalutamide interaction: the documented clinical effects, severity rating, onset, mechanism, and management considerations, with cited references throughout.

AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature

Apalutamide

Erleada
+

Nateglinide

Starlix®
Dr. Brian Staiger, PharmD, BCPS
Medically reviewed by
Dr. Brian Staiger, PharmD, BCPS
Updated Aug 8, 2026
Editorial policy · Data sources
LinkedIn
Interaction severity
Major
Potentially serious — often needs a change or close monitoring.
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.

Of 209 documented Nateglinide interactions, 95 are rated major — including this one.
Worried about symptoms right now? Contact your pharmacist or prescriber, or call Poison Control at 1-800-222-1222 (US). Call 911 for an emergency.
Onset
unspecified
Evidence
theoretical
Severity
Major

What happens

Reduced nateglinide exposure

Interaction Deep Dive

Use caution with concomitant use of apalutamide with nateglinide (CYP3A4/CYP2C9 substrate and OATP1B1 substrate) may result in reduced nateglinide exposure. Coadministration of apalutamide with single oral doses of transporter substrates resulted in a 41% decrease in the AUC of rosuvastatin (a OATP1B1 substrate). Coadministration of a single dose of apalutamide with midazolam, CYP3A4 substrate, resulted in a 92% decrease in the midazolam AUC. Also, coadministration of a single dose of apalutamide with S-warfarin, CYP2C9 substrate, resulted in a 46% decrease in the S-warfarin AUC. Substitution of the medication primarily metabolized by CYP3A4/CYP2C9 is recommended during apalutamide therapy. Evaluate for loss of activity if medication is continued1.

Why it happens (mechanism)

Induction of OATP1B1-mediated efflux transport of nateglinide; induction of CYP3A4-mediated efflux transport of nateglinide; induction of CYP2C9-mediated metabolism of nateglinide

Literature reports

3 reports — tap to read

a) Coadministration of apalutamide with single oral doses of transporter substrates resulted in 41% decrease in the AUC of rosuvastatin (a OATP1B1 substrate) 1.

b) Coadministration of a single dose of apalutamide with midazolam, CYP3A4 substrate, resulted in a 92% decrease in the midazolam AUC 1.

c) Coadministration of a single dose of apalutamide with S-warfarin, CYP2C9 substrate, resulted in a 46% decrease in the S-warfarin AUC 1.

Common questions

Can I take Nateglinide and Apalutamide together?

Reduced nateglinide exposure Always confirm with your pharmacist or prescriber before making any change.

How serious is the Nateglinide and Apalutamide 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 Nateglinide or Apalutamide 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 (1)

  1. Product Information: ERLEADA(R) oral tablets, apalutamide oral tablets. Janssen Products LP (per FDA), Horsham, PA, 2024. DailyMed
Was this write-up helpful?
Apalutamide

Keep reading about Apalutamide

All Apalutamide interactions (162)
Also serious with: Lurasidone Lenacapavir Oral Doravirine Lenacapavir Injection
Nateglinide

Keep reading about Nateglinide

All Nateglinide interactions (209) Nateglinide drug information
Also serious with: Ensitrelvir Insulin Glulisine (Rdna Origin) Injection Levofloxacin Chloroquine
Beyond drug–drug

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:

Apalutamide + Activated Charcoal Grapefruit St. John's Wort Acacia Rigidula Adrafinil African Wild Potato Alkanna Alpine Ragwort + 147 more
Nateglinide + Activated Charcoal Siberian Cocklebur Acai Adrafinil African Wild Potato Agaricus Mushroom Agmatine Agrimony + 282 more

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.

Coming soon

The instant two-drug checker is on its way.

In the meantime, browse the directory below to look up any drug and see its documented interactions.

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
This information is for education, not a substitute for professional medical advice. Do not start, stop, or change any medication without talking to your pharmacist or prescriber.