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Drug interactions

Apalutamide + Mestranol

Severity: Major

Apalutamide and Mestranol: major interaction.

Last updated Sources: US FDA label

For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.

Summary

Apalutamide may lower estrogen exposure from mestranol, which is converted to ethinylestradiol and cleared by CYP3A4. This may reduce contraceptive effectiveness and cause breakthrough bleeding.

What this interaction means in plain words

Apalutamide and Mestranol can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.

Evidence level: Moderate

Why it happens

CYP3A4 induction by apalutamide increases clearance of mestranol and its active metabolite.

What to do

Advise an additional non-hormonal contraceptive method or switch to a non-hormonal method during and after apalutamide use.

What to ask your pharmacist

  • Does the benefit of taking both outweigh the risk in my case?
  • Do I need any blood test, ECG or other check while on both?
  • What early warning signs should I watch for, and what should I do if they appear?

Bring a full list of your medicines, including over-the-counter products, supplements and herbal remedies, to every pharmacy visit.

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References

Frequently asked questions

Can I take Apalutamide with Mestranol?

MediHelp rates the interaction as major. Apalutamide and Mestranol can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Apalutamide may lower estrogen exposure from mestranol, which is converted to ethinylestradiol and cleared by CYP3A4. This may reduce contraceptive effectiveness and cause breakthrough bleeding.

How serious is the interaction between Apalutamide and Mestranol?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Advise an additional non-hormonal contraceptive method or switch to a non-hormonal method during and after apalutamide use.

What other medicines interact with Apalutamide?

MediHelp also lists interactions of Apalutamide with, for example, Cabotegravir, Cobicistat, Doravirine. The full list is on the Apalutamide page.

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