Source: FDA, National Drug Code (US) Revision Year: 2020
TUKYSA 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 in the metastatic setting.
The recommended dosage of TUKYSA is 300 mg taken orally twice daily in combination with trastuzumab and capecitabine until disease progression or unacceptable toxicity [see Clinical Studies (14)].
Advise patients to swallow TUKYSA tablets whole and not to chew, crush, or split prior to swallowing. Advise patients not to ingest tablet if it is broken, cracked, or not otherwise intact.
Advise patients to take TUKYSA approximately 12 hours apart and at the same time each day with or without a meal.
If the patient vomits or misses a dose of TUKYSA, instruct the patient to take the next dose at its usual scheduled time.
When given in combination with TUKYSA, the recommended dosage of capecitabine is 1000 mg/m² orally twice daily taken within 30 minutes after a meal. TUKYSA and capecitabine can be taken at the same time. Refer to the Full Prescribing Information for trastuzumab and capecitabine for additional information.
The recommended TUKYSA dose reductions and dosage modifications for adverse reactions are provided in Tables 1 and 2. Refer to the Full Prescribing Information for trastuzumab and capecitabine for information about dosage modifications for these drugs.
Table 1. Recommended TUKYSA Dose Reductions for Adverse Reactions:
| Dose Reduction | Recommended TUKYSA Dosage |
|---|---|
| First | 250 mg orally twice daily |
| Second | 200 mg orally twice daily |
| Third | 150 mg orally twice daily |
Permanently discontinue TUKYSA in patients unable to tolerate 150 mg orally twice daily.
Table 2. Recommended TUKYSA Dosage Modifications for Adverse Reactions:
| Adverse Reaction1 | Severity | TUKYSA Dosage Modification |
|---|---|---|
| Diarrhea [see Warnings and Precautions (5.1)] | Grade 3 without anti-diarrheal treatment | Initiate or intensify appropriate medical therapy. Hold TUKYSA until recovery to ≤ Grade 1, then resume TUKYSA at the same dose level. |
| Grade 3 with anti-diarrheal treatment | Initiate or intensify appropriate medical therapy. Hold TUKYSA until recovery to ≤ Grade 1, then resume TUKYSA at the next lower dose level. | |
| Grade 4 | Permanently discontinue TUKYSA. | |
| Hepatotoxicity2 [see Warnings and Precautions (5.2)] | Grade 2 bilirubin (>1.5 to 3 × ULN) | Hold TUKYSA until recovery to ≤ Grade 1, then resume TUKYSA at the same dose level. |
| Grade 3 ALT or AST (>5 to 20 × ULN) OR Grade 3 bilirubin (>3 to 10 × ULN) | Hold TUKYSA until recovery to ≤ Grade 1, then resume TUKYSA at the next lower dose level. | |
| Grade 4 ALT or AST (>20 × ULN) OR Grade 4 bilirubin (>10 × ULN) | Permanently discontinue TUKYSA. | |
| ALT or AST >3 × ULN AND Bilirubin > 2 × ULN | Permanently discontinue TUKYSA. | |
| Other adverse reactions [see Adverse Reactions (6.1)] | Grade 3 | Hold TUKYSA until recovery to ≤ Grade 1, then resume TUKYSA at the next lower dose level. |
| Grade 4 | Permanently discontinue TUKYSA. |
1 Grades based on National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.03
2 Abbreviations: ULN = upper limit of normal; ALT = alanine aminotransferase; AST = aspartate aminotransferase
For patients with severe hepatic impairment (Child-Pugh C), reduce the recommended dosage to 200 mg orally twice daily [see Use in Specific Populations (8.7), Clinical Pharmacology (12.3)].
Avoid concomitant use of strong CYP2C8 inhibitors with TUKYSA. If concomitant use with a strong CYP2C8 inhibitor cannot be avoided, reduce the recommended dosage to 100 mg orally twice daily. After discontinuation of the strong CYP2C8 inhibitor for 3 elimination half-lives, resume the TUKYSA dose that was taken prior to initiating the inhibitor [see Drug Interactions (7.2), Clinical Pharmacology (12.3)].
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