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tucatinib

Tukysa · ATC code L01EH03

Also known as: Tukatinib

Key facts
Active substance
tucatinib
ATC code
L01EH03
Authorisation
centrally authorised across the EU (EMA)
Dosage forms
TUKYSA 50 mg film-coated tablets / TUKYSA 150 mg film-coated tablets
Marketing authorisation holder
Pfizer Europe MA EEIG
Information as of
2026-10-28

Key facts

Tucatinib (Tukysa, film-coated tablets) is an oral HER2 tyrosine kinase inhibitor. It is used with trastuzumab and capecitabine for advanced HER2-positive breast cancer.

What it is used for

  • Adults with HER2-positive locally advanced or metastatic breast cancer after at least 2 prior anti-HER2 treatment regimens, in combination with trastuzumab and capecitabine.

Dosing

  • 300 mg (two 150 mg tablets) twice daily continuously, with or without a meal.
  • Capecitabine 1 000 mg/m2 twice daily on days 1 to 14 every 21 days; trastuzumab IV (initial dose 8 mg/kg, then 6 mg/kg every 21 days) or 600 mg subcutaneously every 21 days.
  • Dose reductions for adverse reactions in steps to 250 mg, 200 mg and 150 mg twice daily; permanently discontinue if 150 mg is not tolerated.
  • Do not make up a missed dose; continue until disease progression or unacceptable toxicity.

Contraindications

  • Hypersensitivity to the active substance or any of the excipients.

Important warnings

  • Increased ALT, AST and bilirubin; monitor every three weeks.
  • Serum creatinine increase (30% mean) without impaired renal function; consider alternative markers.
  • Diarrhoea, including severe cases with dehydration, acute kidney injury and death; use antidiarrhoeals and interrupt for Grade ≥ 3.
  • Tucatinib is a strong CYP3A inhibitor; avoid CYP3A substrates where small concentration changes can be dangerous.

Side effects

  • Very common: diarrhoea, nausea, vomiting, stomatitis, rash, arthralgia, epistaxis, increased AST/ALT and bilirubin, weight decrease.
  • Most common Grade 3 and 4 reactions: diarrhoea (13%), ALT increased (6%), AST increased (5%).

Interactions

  • Avoid strong CYP3A or moderate CYP2C8 inducers (e.g. rifampicin, phenytoin, St John's wort, carbamazepine).
  • Avoid strong CYP2C8 inhibitors; monitor for toxicity with moderate inhibitors.
  • Increases levels of CYP3A substrates; inhibits renal transporters of metformin and creatinine.

Pregnancy and breastfeeding

  • May harm the foetus; women and men should use effective contraception during and for at least 1 week after treatment.
  • See also the full text and the trastuzumab and capecitabine product information.

Summary of the official product information, written with AI on 2026-10-29. Every number was checked automatically against the original text. Not reviewed by a physician – the full official text is authoritative.

Full official text →

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For patients

Package leaflet, verbatim

This product has no separate US patient information.

Authorisation and brand names by country

Medicines with exactly this active-substance composition, as listed in the national registers – alphabetical and without ranking. Whether a product is currently available is not shown here.

EU – centrally authorised (all member states)

  • TukysaPfizer Europe MA EEIG · EMEA/H/C/005263

Source: European Medicines Agency (EMA), product information

Turkey

  • TukysaPFİZER PFE İLAÇLARI A.Ş. · 2 register entries

Source: TİTCK – Ruhsatlı Beşeri Tıbbi Ürünler Listesi, as of 2026-10-16

Brand names in 3 more European countries
Iceland
Tukysa
Liechtenstein
Tukysa
Norway
Tukysa

EMA – Article 57 product data (EU/EEA), 2026-10-29

Medelix receives no money from pharmaceutical companies. Brand names are listed alphabetically and without ranking.

Other substances in the same group

Another question about this substance?

Medelix answers clinical questions from guidelines, studies and product information – every claim with its source.

Sources

  1. European Medicines Agency. Tukysa – EPAR, Product Information. 2026-10-28. https://www.ema.europa.eu/en/documents/product-information/tukysa-epar-product-information_en.pdf
  2. TİTCK – Ruhsatlı Beşeri Tıbbi Ürünler Listesi, 2026-10-16. https://www.titck.gov.tr/dinamikmodul/85

Editorial: Medelix editorial team · last updated 2026-10-28 · How these pages are made · Report an error

Source: European Medicines Agency (EMA), product information. Not advertising, not a treatment recommendation. For questions about your own treatment, ask your doctor or pharmacist.