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At a glance

Tucatinib is indicated in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens.

Indications
  • HER2-positive metastatic breast cancer
  • HER2-positive breast cancer with brain metastases
Pharmacology

Tucatinib is a tyrosine kinase inhibitor of HER2. In vitro, tucatinib inhibits phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell proliferation. In vivo, tucatinib inhibited the growth of HER2 expressing tumors. The combination of tucatinib and trastuzumab showed increased anti-tumor activity compared to either drug alone.

Dosage

Adult Dose (Oral):

  • 300 mg twice daily in combination with trastuzumab and capecitabine until disease progression or unacceptable toxicity
  • Swallow tablets whole; do not chew, crush, or split
  • Take approximately 12 hours apart at the same time each day with or without a meal
  • If patient vomits or misses a dose, take the next dose at its usual scheduled time
  • Severe hepatic impairment (Child-Pugh C): 200 mg twice daily
  • Avoid concomitant use with strong CYP2C8 inhibitors; if unavoidable, reduce dose to 100 mg twice daily
Side effects

Common Side Effects:

  • Diarrhea
  • Palmar-plantar erythrodysesthesia
  • Nausea
  • Fatigue
  • Hepatotoxicity
  • Vomiting
  • Stomatitis
  • Decreased appetite
  • Abdominal pain
  • Headache
  • Anemia
  • Rash
Use in pregnancy

Use in Pregnancy: Animal studies show embryo-fetal mortality, reduced fetal weight, and fetal abnormalities; advise pregnant women of potential risk.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Precautions & warnings
  • Can cause severe diarrhea; administer antidiarrheal treatment as clinically indicated
  • Monitor ALT, AST, and bilirubin prior to starting, every 3 weeks during treatment, and as clinically indicated
  • May cause fetal harm; use effective contraception during treatment and for at least 1 week after last dose
  • Advise male patients with female partners of reproductive potential to use effective contraception
Overdose effects

No specific antidote; benefit of hemodialysis unknown.

Treatment: Withhold tucatinib and apply general supportive measures.

Storage conditions

Store below 25°C in a cool and dry place. Keep away from light. Keep out of reach of children.

Tucatinib — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.