Usual Adult Dose for Gastrointestinal Stromal Tumor

150 mg orally once daily until disease progression or unacceptable toxicity

Use: For adults with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors, including imatinib

Renal Dose Adjustments

Data not available

Liver Dose Adjustments

Mild hepatic impairment (total bilirubin upper limit of normal or less and AST greater than ULN or total bilirubin 1 to 1.5 x ULN and any AST): No adjustment recommended.
Moderate or severe hepatic impairment: Dose adjustment(s) may be required; however, no specific guidelines have been suggested. Caution recommended.

Dose Adjustments

The recommended dose reduction for adverse reactions is 100 mg orally once daily.
Permanently discontinue this drug in patients who are unable to tolerate 100 mg orally once daily.

DOSE MODIFICATIONS FOR ADVERSE REACTIONS:
PALMAR-PLANTAR ERYTHRODYSESTHESIA SYNDROME (PPES):

• Grade 2: Withhold this drug until Grade 1 or less or baseline; if recovered within 7 days, resume at same dose; otherwise resume at reduced dose; consider re-escalating this drug if maintained at Grade 1 or less or baseline for at least 28 days; if PPES recurs, withhold this drug until Grade 1 or less or baseline and then resume at a reduced dose regardless of time to improvement.
• Grade 3: Withhold this drug for at least 7 days or until Grade 1 or less or baseline (maximum 28 days); resume at a reduced dose; consider re-escalating this drug if maintained at Grade 1 or less or baseline for at least 28 days.

• Grade 3: If symptomatic, withhold this drug until symptoms have resolved and blood pressure is controlled; if blood pressure is controlled to Grade 1 or less or baseline, resume at the same dose; otherwise, resume at reduced dose; if Grade 3 hypertension recurs, withhold this drug until symptoms have resolved and blood pressure is controlled; resume at reduced dose.
• Grade 4: Permanently discontinue this drug.

• Grade 3 or 4: Permanently discontinue this drug.

• Grade 2: Withhold this drug until Grade 1 or less or baseline; if recovered within 7 days, resume at same dose; otherwise resume at reduced dose; consider re-escalating this drug if maintained at Grade 1 or less or baseline for at least 28 day; if arthralgia or myalgia recurs, withhold this drug until Grade 1 or less or baseline and then resume at reduced dose regardless of time to improvement.
• Grade 3: Withhold this drug for at least 7 days or until Grade 1 or less or baseline (maximum of 28 days); resume at reduced dose; consider re-escalating this drug if maintained at Grade 1 or less or baseline for at least 28 days.

• Grade 3 or 4: Withhold this drug until Grade 1 or less or baseline (maximum 28 days), and then resume at reduced dose; otherwise permanently discontinue this drug; consider re-escalating this drug if no recurrence of the adverse reaction for at least 28 days; if Grade 3 or 4 recurs, permanently discontinue this drug.

Precautions

CONTRAINDICATIONS:

• None

Dialysis

Data not available

Other Comments

Administration advice:

• This drug may be taken with or without food.
• Swallow tablets whole; do not crush, chew, or dissolve.
• Take this drug at the same time each day.
• Take a missed dose if less than 8 hours have passed since the missed scheduled dose.
• Do not take an additional dose if vomiting occurs after taking and to continue with the next scheduled dose.

• Store at 20C to 25C (68F to 77F); excursion permitted between 15C to 30C (59F to 86F).

• Take this drug with or without food at the same time each day.
• This drug can harm a developing fetus.
• This tablet contains lactose.