Ensartinib Dosage

Medically reviewed by Drugs.com. Last updated on Jun 30, 2025.

Usual Adult Dose for Non-Small Cell Lung Cancer

225 mg orally once a day
Duration of therapy: Until disease progression or unacceptable toxicity

Comments:

• Select patients for the treatment based on the presence of anaplastic lymphoma kinase (ALK) rearrangement(s) in tumor specimens; a US FDA-approved test to detect ALK rearrangements is not currently available.
• May administer with or without food

Use: For the treatment of ALK-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) in patients who have not previously received an ALK-inhibitor

Renal Dose Adjustments

Renal Dysfunction: Data not available

Liver Dose Adjustments

Mild liver dysfunction (total bilirubin up to 1 times the upper limit of normal [1 x ULN] and AST greater than ULN OR total bilirubin 1 to 1.5 x ULN and any AST): No adjustment recommended
Moderate liver dysfunction (total bilirubin greater than 1.5 to 3 x ULN and any AST): Caution and additional monitoring recommended; adjust dose as indicated for adverse reactions.
Severe liver dysfunction (total bilirubin greater than 3 times ULN and any AST): Not recommended

If Hepatotoxicity Develops During Therapy:
Grade 3 or 4: ALT or AST elevation (greater than 5 x ULN) with concurrent total bilirubin 2 x ULN or less:

• Withhold therapy until recovery to grade 1 or less (i.e., 3 x ULN or less) or to baseline.
• Resume therapy at a reduced dose.
• First dose reduction: 200 mg orally once a day
• Second dose reduction: 150 mg orally once a day
• If unable to tolerate 150 mg/day: Permanently discontinue therapy.

Grade 2 to 4: ALT or AST elevation (greater than 3 x ULN) with concurrent total bilirubin elevation greater than 2 x ULN in the absence of cholestasis or hemolysis: Permanently discontinue therapy.

Dose Adjustments

Stepwise Dose Reductions for Adverse Reactions:

• First dose reduction: 200 mg orally once a day
• Second dose reduction: 150 mg orally once a day
• Permanently discontinue therapy in patients unable to tolerate 150 mg orally once a day.
• Once the dose has been reduced for adverse reactions, do not subsequently increase the dose.

INTERSTITIAL LUNG DISEASE/PNEUMONITIS:
Any Grade Reaction: Permanently discontinue therapy.

DERMATOLOGIC ADVERSE REACTIONS:
Grade 1: Consider management with topical steroids.

Grade 2: Administer topical corticosteroids.

• If no improvement within 7 days of topical treatment, administer oral corticosteroids.
• If no improvement within 7 days of initiating oral corticosteroids, withhold this drug until recovery to grade 1 or less, then resume therapy at a reduced dose.

Grade 3: Withhold therapy and administer topical corticosteroids.

• If no improvement within 7 days of topical treatment, administer oral corticosteroids.
• Upon improvement to grade 1 or less, resume therapy at a reduced dose.

Grade 4: Permanently discontinue therapy.

• Administer systemic corticosteroids and consider antibiotic use.

BRADYCARDIA (Heart rate less than 60 beats per minute [bpm]):
Symptomatic Bradycardia:

• Withhold therapy until recovery to asymptomatic bradycardia or to a resting heart rate (HR) of at least 60 bpm.
• If a concomitant medication known to cause bradycardia is identified and discontinued/dose-adjusted, resume this drug at same dose upon recovery to asymptomatic bradycardia or to resting HR of at least 60 bpm.
• If there is no identified concomitant medication known to cause bradycardia, or if contributing concomitant medications are not discontinued or dose-adjusted, resume this drug at reduced dose upon recovery to asymptomatic bradycardia or to resting HR of at least 60 bpm.

Bradycardia With Life-Threatening Consequences Requiring Urgent Intervention:

• Permanently discontinue therapy if no contributing concomitant medication is identified.
• If contributing concomitant medication is identified and discontinued or dose-adjusted, resume this drug at reduced dose upon recovery to asymptomatic bradycardia or to a resting HR of at least 60 bpm, with frequent monitoring as clinically indicated.
• For recurrence, permanently discontinue this drug.

HYPERGLYCEMIA:
Grade 3 (blood glucose greater than 250 mg/dL despite optimal management) OR Grade 4:

• Withhold therapy until hyperglycemia is adequately controlled, then resume at a reduced dose.
• Permanently discontinue therapy if adequate hyperglycemic control cannot be achieved with optimal medical management.

VISUAL DISTURBANCE:
Grade 2 or 3: Withhold therapy until recovery to grade 1 or baseline, then consider resuming at a reduced dose.

Grade 4: Permanently discontinue therapy.

INCREASED CREATINE PHOSPHOKINASE (CPK):
Elevated CPK greater than 5 x ULN: Temporarily withhold therapy until recovery to baseline or 2.5 x ULN or less, then resume therapy at same dose.

Elevated CPK greater than 10 x ULN, OR second occurrence greater than 5 x ULN: Temporarily withhold therapy until recovery to baseline or 2.5 x ULN or less, then resume therapy at reduced dose.

HYPERURICEMIA:
Grade 4 or Symptomatic: Initiate urate-lowering medication and withhold this drug.

• Once signs or symptoms have improved, resume therapy at the same or reduced dose.

OTHER ADVERSE REACTIONS:
Grade 3 or 4: Withhold therapy until recovery to grade 1 or baseline, then resume at reduced dose.

Grade 4 Recurrent: Permanently discontinue therapy.

Precautions

CONTRAINDICATIONS:

• Known severe hypersensitivity reaction to the active component, FD&C yellow no. 5 (tartrazine), or any of the ingredients

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:

• Before initiating therapy, evaluate liver function tests and fasting blood glucose.
• Administer therapy orally with or without food and at the same time each day.
• Capsules should be swallowed whole; do not crush, chew, or open/dissolve the capsule contents.
• If a dose is missed, administer as soon as possible unless the next dose is due within 12 hours; do not administer 2 doses on the same day.
• If vomiting occurs after taking a dose, do not administer an additional dose and give the next dose at its scheduled time.

Storage requirements:

• Store at room temperature 20C to 25C (68F to 77F); excursions permitted to 15C to 30C (59F to 86F).
• Store and dispense in the original bottle with desiccant to protect from moisture.

General:

• This drug contains tartrazine (FD&C yellow no. 5) which may cause allergic reactions in susceptible patients.

Monitoring:

• Cardiovascular: Heart rate (during therapy)
• Dermatologic: For adverse skin reactions (during therapy)
• Hepatic: Liver function tests including AST, ALT, and bilirubin (at baseline, every 2 weeks during first treatment cycle, then monthly and as clinically indicated during therapy)
• Metabolic: Fasting blood glucose and serum uric acid (at baseline and periodically during therapy)
• Other: CPK levels (periodically during therapy)
• Respiratory: For new/worsening interstitial lung disease/pneumonitis (during therapy)

Patient advice:

• Read the US FDA-approved patient labeling (Patient Information).
• Inform your health care provider immediately of any new or worsening respiratory, liver, cardiac, or vision signs/symptoms.
• Treatment may increase uric acid, glucose, and creatine phosphokinase levels; report any related new or worsening symptoms to your health care provider.
• Limit sun exposure during treatment and for at least 1 week after the final dose.
• Seek urgent medical care if symptoms of an allergic reaction to tartrazine (FD&C yellow no. 5) occur.
• Breastfeeding is not recommended during treatment.
• Patients of childbearing potential: This drug may cause potential harm to a fetus.
• Notify your health care provider of a known/suspected pregnancy.
• Females: Use effective contraception during treatment and for 1 week after the last dose.
• Males (with female partners of reproductive potential): Use effective contraception during treatment and for 1 week after the last dose.

See also:

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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