HER2+ Metastatic Breast Cancer: In combination with trastuzumab and capecitabine for adult patients with HER2-positive unresectable locally advanced or metastatic breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.
HER2+ Metastatic Colorectal Cancer: In combination with trastuzumab for adult patients with RAS wild-type, HER2-positive unresectable or metastatic colorectal cancer that has progressed after fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy.
Recommended dose: 300 mg orally twice daily, approximately 12 hours apart, in combination with trastuzumab and capecitabine (breast) or trastuzumab alone (CRC)
Administration: With or without food. Swallow tablets whole.
Dose reductions: First: 250 mg twice daily; Second: 200 mg twice daily; Third: 150 mg twice daily. Discontinue if unable to tolerate 150 mg.
Tablets (film-coated): 50 mg, 150 mg
None listed in the prescribing information.
Diarrhea (81%), PPE Syndrome (63%), Nausea (58%), Fatigue (45%), Vomiting (36%), Stomatitis (32%), Decreased Appetite (24%), Abdominal Pain (20%), Headache (16%), Anemia (15%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Strong CYP3A Inducers: Avoid concurrent use as they decrease tucatinib exposure.
Strong CYP3A Inhibitors: Avoid concurrent use as they increase tucatinib exposure.
CYP3A Substrates: Tucatinib is a strong CYP3A inhibitor. The dose of sensitive CYP3A substrates with narrow therapeutic index may need to be reduced.
CYP2C8 Substrates: Tucatinib is a moderate CYP2C8 inhibitor. Monitor for increased adverse reactions of CYP2C8 substrates.
P-gp Substrates: Tucatinib is a P-gp inhibitor. Consider reducing the dose of P-gp substrates with narrow therapeutic index.
Consult the full prescribing information for pregnancy-related considerations.
Refer to prescribing information for lactation guidance.
Pediatric safety and efficacy information is detailed in the full label.
Dose modifications for organ impairment are specified in the complete prescribing information.
Tucatinib is a tyrosine kinase inhibitor that is highly selective for the kinase domain of HER2 with minimal inhibition of EGFR. In combination with trastuzumab, tucatinib demonstrated enhanced anti-tumor activity compared with either agent alone. Tucatinib has demonstrated activity in the CNS, supporting its use in patients with brain metastases.
Tmax: 2 hours. Bioavailability not characterized. Vd: 1670 L. Protein binding: 97%. Metabolized by CYP2C8 and CYP3A. Half-life: 8.5 hours. Steady state within 4 days. Elimination: feces 86%, urine 5%.
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
Tukysa has FDA-approved indications across the following cancer types covered on CancerDrugEvidence:
Tukysa (tucatinib) is an FDA-approved oncology agent. Refer to the full prescribing information for complete indication details.
Refer to the full prescribing information for dosing schedules, administration instructions, and dose modifications.
Tucatinib is a tyrosine kinase inhibitor that is highly selective for the kinase domain of HER2 with minimal inhibition of EGFR. In combination with trastuzumab, tucatinib demonstrated enhanced anti-tumor activity compared with either agent alone. Tucatinib has demonstrated activity in the CNS, supporting its use in patients with brain metastases.
Diarrhea (81%), PPE Syndrome (63%), Nausea (58%), Fatigue (45%), Vomiting (36%), Stomatitis (32%), Decreased Appetite (24%), Abdominal Pain (20%), Headache (16%), Anemia (15%) Diarrhea 81% PPE Syndrome 63% Nausea 58% Fatigue 45% Vomiting 36% Stomatitis 32% Decreased Appetite 24% Abdominal Pain 20% H