Breast cancer:
Indications for: TUKYSA
In combination with trastuzumab and capecitabine, for the treatment of patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received 1 or more prior anti-HER2-based regimens in the metastatic setting.
Adult Dosage:
Swallow whole. Take approx. 12hrs apart and at the same time each day. 300mg twice daily (in combination with trastuzumab and capecitabine; refer to the respective full product labeling for additional information) until disease progression or unacceptable toxicity. Concomitant strong CYP2C8 inhibitors (if unavoidable): 100mg twice daily. Severe hepatic impairment (Child-Pugh C): 200mg twice daily. Dose modifications for adverse reactions: see full labeling.
Children Dosage:
Not established.
TUKYSA Warnings/Precautions:
Risk of severe diarrhea (including dehydration, hypotension, acute kidney injury, death); give antidiarrheal if occurs. Perform diagnostic tests as needed to exclude other causes of diarrhea. Risk of severe hepatotoxicity. Monitor liver function tests prior to initiation, every 3 weeks during, then as clinically indicated. Severe renal impairment (CrCl <30mL/min): not recommended. Severe hepatic impairment: see Adults. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for at least 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for at least 1 week after the last dose).
TUKYSA Classification:
Tyrosine kinase inhibitor.
TUKYSA Interactions:
Potentiated by strong CYP2C8 inhibitors (eg, gemfibrozil); avoid concomitant use; reduce dose if unavoidable (see Adults); monitor frequently for moderate CYP2C8 inhibitors. Antagonized by strong CYP3A or moderate CYP2C8 inducers (eg, rifampin); avoid. Potentiates CYP3A substrates (eg, midazolam); avoid concomitant use; decrease CYP3A substrate dose if unavoidable. Potentiates P-gp substrates (eg, digoxin); consider dose reduction of P-gp substrate.
Adverse Reactions:
Diarrhea, palmar-plantar erythrodysesthesia, nausea, fatigue, hepatotoxicity, vomiting, stomatitis, decreased appetite, abdominal pain, headache, anemia, rash, infusion-related reactions, pyrexia.
Drug Elimination:
Fecal (86%), renal (4.1%). Half-life: ~8.5 hours
Generic Drug Availability:
NO
How Supplied:
Tabs 50mg—60; 150mg—60, 120
Colorectal and other GI cancers:
Indications for: TUKYSA
In combination with trastuzumab, for the treatment of adults with RAS wild-type HER2-positive unresectable or metastatic colorectal cancer that has progressed following treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy.
Adult Dosage:
Select patients based on the presence of HER2 overexpression or gene amplification, or RAS wild-type. Swallow whole. Take approx. 12hrs apart and at the same time each day. 300mg twice daily (in combination with trastuzumab; refer to the respective full product labeling for additional information) until disease progression or unacceptable toxicity. Concomitant strong CYP2C8 inhibitors (if unavoidable): 100mg twice daily. Severe hepatic impairment (Child-Pugh C): 200mg twice daily. Dose modifications for adverse reactions: see full labeling.
Children Dosage:
Not established.
TUKYSA Warnings/Precautions:
Risk of severe diarrhea (including dehydration, hypotension, acute kidney injury, death); give antidiarrheal if occurs. Perform diagnostic tests as needed to exclude other causes of diarrhea. Risk of severe hepatotoxicity. Monitor liver function tests prior to initiation, every 3 weeks during, then as clinically indicated. Severe renal impairment (CrCl <30mL/min): not recommended. Severe hepatic impairment: see Adults. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for at least 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for at least 1 week after the last dose).
TUKYSA Classification:
Tyrosine kinase inhibitor.
TUKYSA Interactions:
Potentiated by strong CYP2C8 inhibitors (eg, gemfibrozil); avoid concomitant use; reduce dose if unavoidable (see Adults); monitor frequently for moderate CYP2C8 inhibitors. Antagonized by strong CYP3A or moderate CYP2C8 inducers (eg, rifampin); avoid. Potentiates CYP3A substrates (eg, midazolam); avoid concomitant use; decrease CYP3A substrate dose if unavoidable. Potentiates P-gp substrates (eg, digoxin); consider dose reduction of P-gp substrate.
Adverse Reactions:
Diarrhea, palmar-plantar erythrodysesthesia, nausea, fatigue, hepatotoxicity, vomiting, stomatitis, decreased appetite, abdominal pain, headache, anemia, rash, infusion-related reactions, pyrexia.
Drug Elimination:
Fecal (86%), renal (4.1%). Half-life: ~8.5 hours
Generic Drug Availability:
NO
How Supplied:
Tabs 50mg—60; 150mg—60, 120
