Skip to content

Drug interactions

Regorafenib + Tucatinib

Severity: Major

Regorafenib and Tucatinib: major interaction.

Last updated

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

Tucatinib is a strong CYP3A inhibitor and may increase regorafenib parent exposure while lowering active metabolite levels. Toxicity such as liver injury and hypertension may increase, and both drugs can cause hepatotoxicity.

What this interaction means in plain words

Regorafenib and Tucatinib 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.

Regorafenib belongs to Oncology; Tucatinib belongs to Oncology.

Evidence level: Moderate

Why it happens

CYP3A4 inhibition by tucatinib reduces regorafenib metabolism.

What to do

Avoid the combination if possible. If unavoidable, monitor liver tests and blood pressure closely and modify regorafenib dose for toxicity.

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.

Pro+ members

Unlock the full page

Create an account and start a Pro+ trial to unlock the full management advice for Regorafenib and Tucatinib, the additional notes, the evidence detail and the whole-prescription interaction checker.

  • Full clinical management advice
  • Additional notes
  • Evidence detail
  • Interaction checker for a whole prescription

Try Pro+ free for 14 days on the web. No card needed.

Frequently asked questions

Can I take Regorafenib with Tucatinib?

MediHelp rates the interaction as major. Regorafenib and Tucatinib 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. Tucatinib is a strong CYP3A inhibitor and may increase regorafenib parent exposure while lowering active metabolite levels. Toxicity such as liver injury and hypertension may increase, and both drugs can cause hepatotoxicity.

How serious is the interaction between Regorafenib and Tucatinib?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid the combination if possible. If unavoidable, monitor liver tests and blood pressure closely and modify regorafenib dose for toxicity.

What other medicines interact with Regorafenib?

MediHelp also lists interactions of Regorafenib with, for example, Apalutamide, Atazanavir, Carbamazepine. The full list is on the Regorafenib page.

Full monographs, dosing and an interaction checker in the MediHelp app

Open the complete reference, check multi-drug interactions and use dosing tools in the MediHelp app.

Browse A–Z · Drug interactions

Get the app Sign in