TM Owner Pfizer (Seagen)
Tukysa 150mg Tablet
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Indications & Clinical Uses
- Tukysa (tucatinib) is a tyrosine kinase inhibitor (TKI) used to treat HER2-positive breast cancer in combination with trastuzumab and capecitabine.
- It is approved for advanced unresectable or metastatic HER2-positive breast cancer after prior anti-HER2 therapies.
- Tukysa was also approved for RAS wild-type HER2-positive unresectable or metastatic colorectal cancer combined with trastuzumab after disease progression on standard chemotherapy.
Side Effects
- The most common side effect of Tukysa is diarrhea (81% of patients, with 12% experiencing severe Grade 3 diarrhea).
- Other frequent side effects include palmar-plantar erythrodysesthesia (63%), nausea (58%), hepatotoxicity with liver enzyme elevation (42%), vomiting (36%), mouth sores (32%), decreased appetite (25%), and anemia (21%).
- Severe diarrhea can lead to dehydration, acute kidney injury, and rarely death.
- Serious hepatotoxicity requires monitoring.
Precautions & Warnings
- Monitor liver function tests (ALT, AST, bilirubin) before treatment and every 3 weeks during therapy to detect hepatotoxicity early.
- Tukysa can cause fetal harm and is contraindicated in pregnancy.
- Effective contraception is required during treatment.
- Manage severe diarrhea aggressively with anti-diarrheal medications and hydration.
- Monitor kidney function as the drug causes reversible increases in serum creatinine reflecting tubular transport changes, not kidney damage.
Avoid Interactions
- Strong CYP3A inducers and moderate CYP2C8 inducers reduce Tukysa effectiveness.
- Strong CYP2C8 inhibitors increase Tukysa levels, requiring dose reduction to 100 mg twice daily.
- CYP3A substrates experience 5.7-fold increase in plasma concentration, requiring dose adjustment.
- Monitor patients taking P-glycoprotein substrates for potential toxicity.
References
Frequently Asked Questions
Tukysa (tucatinib) is a tyrosine kinase inhibitor used for HER2-positive breast cancer that is advanced or has metastasized. It is taken in combination with trastuzumab and capecitabine after other HER2-targeted treatments have stopped working. It blocks a specific cancer growth protein (HER2) to slow tumor progression.
Tukysa is taken orally at 300 mg twice daily (every 12 hours) with food. Each tablet contains 150 mg of tucatinib, so you take two tablets per dose. Take doses at consistent times with meals to improve absorption and reduce gastrointestinal side effects like nausea.
Tukysa commonly causes diarrhea (occurring in 81% of patients), sometimes severe requiring intervention. Nausea, hand-foot skin redness, liver enzyme elevation, and decreased appetite are very common. Vomiting and mouth sores occur in many patients. Report persistent diarrhea immediately to your healthcare provider.
Do not take Tukysa if pregnant, as it causes fetal harm and birth defects. Use effective contraception during treatment and for one week after stopping. Tell your doctor about all medications, especially strong CYP3A inhibitors and inducers. Inform them about grapefruit, St. John's Wort, and herbal supplements.
If you miss a dose of Tukysa, take it as soon as you remember, unless it is nearly time for the next scheduled dose. Never double your dose to make up for a missed one. Set reminders at consistent times (morning and evening) to reduce missed doses and maintain steady medication levels.
Your doctor will check liver function tests (ALT, AST, bilirubin) before starting Tukysa treatment and every three weeks during your therapy. These blood tests detect serious liver injury early. Inform your healthcare provider immediately if you develop yellowing of skin or eyes, dark urine, or severe right-sided abdominal pain.
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