TUKYSA® Highlights

(tucatinib)

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use TUKYSA safely and effectively. See full prescribing information for TUKYSA.

TUKYSA (tucatinib) tablets, for oral use
Initial U.S. Approval: 2020

RECENT MAJOR CHANGES

Indications and Usage (1.2)

1/2023

Patient Selection (2.1)

1/2023

Warnings and Precautions (5.1), (5.2)

1/2023

INDICATIONS AND USAGE

TUKYSA is a kinase inhibitor 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 in the metastatic setting. (1.1)
•
in combination with trastuzumab for the treatment of adult patients with RAS wild-type HER2-positive unresectable or metastatic colorectal cancer that has progressed following treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy. (1.2)

This indication is approved under accelerated approval based on tumor response rate and durability of response [see Clinical Studies (14.2)]. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.

DOSAGE AND ADMINISTRATION

•
In patients with unresectable or metastatic colorectal cancer, confirm the presence of HER2 protein overexpression and RAS wild-type in tumor specimens prior to the initiation of TUKYSA (2.1)
•
Recommended dosage: 300 mg taken orally twice daily with or without food. (2.1)
•
For patients with severe hepatic impairment, the recommended dosage is 200 mg orally twice daily. (2.3, 8.7)

DOSAGE FORMS AND STRENGTHS

Tablets: 50 mg and 150 mg. (3)

CONTRAINDICATIONS

None. (4)

WARNINGS AND PRECAUTIONS

•
Diarrhea: Severe diarrhea, including dehydration, acute kidney injury, and death, has been reported. Administer antidiarrheal treatment as clinically indicated. Interrupt dose, then dose reduce, or permanently discontinue TUKYSA based on severity. (2.2, 5.1)
•
Hepatotoxicity: Severe hepatotoxicity has been reported on TUKYSA. Monitor ALT, AST and bilirubin prior to starting TUKYSA, every 3 weeks during treatment and as clinically indicated. Interrupt dose, then dose reduce, or permanently discontinue TUKYSA based on severity. (2.2, 5.2)
•
Embryo-Fetal Toxicity: TUKYSA can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception. (5.3, 8.1, 8.3)
Also, refer to the Full Prescribing Information of trastuzumab and capecitabine for pregnancy and contraception information.

ADVERSE REACTIONS

•
The most common adverse reactions (≥20%) with TUKYSA in combination with trastuzumab and capecitabine in patients with metastatic breast cancer are diarrhea, palmar-plantar erythrodysesthesia, nausea, hepatotoxicity, vomiting, stomatitis, decreased appetite, anemia, and rash. (6.1)
•
The most common adverse reactions (≥20%) with TUKYSA in combination with trastuzumab in patients with unresectable or metastatic colorectal cancer are diarrhea, fatigue, rash, nausea, abdominal pain, infusion related reactions, and pyrexia.

To report SUSPECTED ADVERSE REACTIONS, contact Seagen at 1-855-4SEAGEN or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

•
Strong CYP3A Inducers or Moderate CYP2C8 Inducers: Avoid concomitant use. (7.1)
•
Strong CYP2C8 Inhibitors: Avoid concomitant use; reduce TUKYSA dose if concomitant use cannot be avoided. (2.4, 7.1)
•
CYP3A Substrates: Avoid concomitant use with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. (7.2)
•
P-gp Substrates: Consider reducing the dose of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. (7.2)

USE IN SPECIFIC POPULATIONS

Lactation: Advise not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 1/2023

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Highlights

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use TUKYSA safely and effectively. See full prescribing information for TUKYSA.

TUKYSA (tucatinib) tablets, for oral use
Initial U.S. Approval: 2020

RECENT MAJOR CHANGES

Indications and Usage (1.2)

1/2023

Patient Selection (2.1)

1/2023

Warnings and Precautions (5.1), (5.2)

1/2023

INDICATIONS AND USAGE

TUKYSA is a kinase inhibitor 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 in the metastatic setting. (1.1)
•
in combination with trastuzumab for the treatment of adult patients with RAS wild-type HER2-positive unresectable or metastatic colorectal cancer that has progressed following treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy. (1.2)

This indication is approved under accelerated approval based on tumor response rate and durability of response [see Clinical Studies (14.2)]. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.

DOSAGE AND ADMINISTRATION

•
In patients with unresectable or metastatic colorectal cancer, confirm the presence of HER2 protein overexpression and RAS wild-type in tumor specimens prior to the initiation of TUKYSA (2.1)
•
Recommended dosage: 300 mg taken orally twice daily with or without food. (2.1)
•
For patients with severe hepatic impairment, the recommended dosage is 200 mg orally twice daily. (2.3, 8.7)

DOSAGE FORMS AND STRENGTHS

Tablets: 50 mg and 150 mg. (3)

CONTRAINDICATIONS

None. (4)

WARNINGS AND PRECAUTIONS

•
Diarrhea: Severe diarrhea, including dehydration, acute kidney injury, and death, has been reported. Administer antidiarrheal treatment as clinically indicated. Interrupt dose, then dose reduce, or permanently discontinue TUKYSA based on severity. (2.2, 5.1)
•
Hepatotoxicity: Severe hepatotoxicity has been reported on TUKYSA. Monitor ALT, AST and bilirubin prior to starting TUKYSA, every 3 weeks during treatment and as clinically indicated. Interrupt dose, then dose reduce, or permanently discontinue TUKYSA based on severity. (2.2, 5.2)
•
Embryo-Fetal Toxicity: TUKYSA can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception. (5.3, 8.1, 8.3)
Also, refer to the Full Prescribing Information of trastuzumab and capecitabine for pregnancy and contraception information.

ADVERSE REACTIONS

•
The most common adverse reactions (≥20%) with TUKYSA in combination with trastuzumab and capecitabine in patients with metastatic breast cancer are diarrhea, palmar-plantar erythrodysesthesia, nausea, hepatotoxicity, vomiting, stomatitis, decreased appetite, anemia, and rash. (6.1)
•
The most common adverse reactions (≥20%) with TUKYSA in combination with trastuzumab in patients with unresectable or metastatic colorectal cancer are diarrhea, fatigue, rash, nausea, abdominal pain, infusion related reactions, and pyrexia.

To report SUSPECTED ADVERSE REACTIONS, contact Seagen at 1-855-4SEAGEN or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

•
Strong CYP3A Inducers or Moderate CYP2C8 Inducers: Avoid concomitant use. (7.1)
•
Strong CYP2C8 Inhibitors: Avoid concomitant use; reduce TUKYSA dose if concomitant use cannot be avoided. (2.4, 7.1)
•
CYP3A Substrates: Avoid concomitant use with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. (7.2)
•
P-gp Substrates: Consider reducing the dose of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. (7.2)

USE IN SPECIFIC POPULATIONS

Lactation: Advise not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 1/2023
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