Taletrectinib Dosage

Medically reviewed by Drugs.com. Last updated on Jul 8, 2025.

Usual Adult Dose for Non-Small Cell Lung Cancer

600 mg orally once a day on an empty stomach
Duration of therapy: Until disease progression or unacceptable toxicity

Comments:

• Select patients for the treatment based on the presence of ROS1 rearrangement(s) in tumor specimens; a US FDA-approved test to detect ROS1 rearrangements is not currently available.
• Administer at least 2 hours before and 2 hours after food intake.

Use: For the treatment of locally advanced or metastatic ROS1-positive non-small cell lung cancer

Renal Dose Adjustments

Renal dysfunction: Data not available

Liver Dose Adjustments

LIVER DYSFUNCTION: Data not available

HEPATOTOXICITY:
Stepwise Dose Reductions for Hepatotoxicity:

• First dose reduction: 400 mg orally once a day
• Second dose reduction: 200 mg orally once a day
• If unable to tolerate 200 mg/day: Permanently discontinue therapy.

Grade 3 ALT or AST elevation greater than 5 to 20 times the upper limit of normal (5 to 20 x ULN): Withhold therapy until recovery to grade 1 or less, or baseline.

• If resolved within 6 weeks, resume at a reduced dose level.
• If not resolved after 6 weeks, permanently discontinue therapy.
• For recurrence: If resolved within 6 weeks, resume at a reduced dose level.
• For recurrence: If not resolved after 6 weeks, permanently discontinue therapy.

Grade 4 ALT or AST elevation greater than 20 x ULN: Withhold therapy until recovery to grade 1 or less, or baseline.

• If resolved within 6 weeks, resume at a reduced dose level.
• If not resolved after 6 weeks, permanently discontinue therapy.
• For recurrence: Permanently discontinue therapy.

For ALT or AST at least 3 x ULN with concurrent total bilirubin at least 2 x ULN (in the absence of cholestasis or hemolysis): Permanently discontinue therapy.

Dose Adjustments

Stepwise Dose Reductions for Adverse Reactions:

• First dose reduction: 400 mg orally once a day
• Second dose reduction: 200 mg orally once a day
• Permanently discontinue therapy in patients unable to tolerate 200 mg orally once a day.

INTERSTITIAL LUNG DISEASE (ILD)/PNEUMONITIS:
Grade 1: If ILD/pneumonitis occurs or is suspected, withhold therapy until recovery to grade 0 or baseline.

• If resolved within 6 weeks, resume at the same dose level.
• If not resolved after 6 weeks, permanently discontinue therapy.
• For recurrence: Permanently discontinue therapy.

Grade 2: If ILD/pneumonitis occurs or is suspected, withhold therapy until recovery to grade 0 or baseline.

• If resolved within 6 weeks, resume at a reduced dose level.
• If not resolved after 6 weeks, permanently discontinue therapy.
• For recurrence: Permanently discontinue therapy.

Grade 3 or 4: Permanently discontinue therapy.

QTc INTERVAL PROLONGATION
Grade 2 QTc interval 481 to 500 milliseconds (msec): Withhold therapy until recovery to at least grade 1 or baseline.

• Correct electrolytes and/or change concomitant medications.
• Resume therapy at the same dose.

Grade 3 QTc interval 501 msec or greater, OR QTc interval increase of more than 60 msec from baseline: Withhold therapy until recovery to at least grade 1 or baseline.

• Correct electrolytes and/or change concomitant medications.
• Resume therapy at a reduced dose level.

Grade 4 (e.g., Torsade de pointes, polymorphic ventricular tachycardia, signs/symptoms of serious arrhythmia): Permanently discontinue therapy.

HYPERURICEMIA:
Grade 3 or 4: Withhold therapy until improvement in signs or symptoms.

• Resume therapy at the same or reduced dose level or permanently discontinue treatment.

CREATINE PHOSPHOKINASE (CPK) ELEVATION:
CPK greater than 5 x ULN: Withhold therapy until recovery to baseline or at least 2.5 x ULN, then resume therapy at the same dose.

• For recurrence: Withhold until recovery to baseline or at least 2.5 x ULN, then resume at a reduced dose.

CPK greater than 10 x ULN: Withhold until recovery to baseline or at least 2.5 x ULN, then resume at a reduced dose.

OTHER ADVERSE REACTIONS:
Grade 3: Withhold therapy until recovery to at least grade 1 or baseline.

• If resolved within 6 weeks, resume therapy at a reduced dose level.
• If not resolved after 6 weeks, permanently discontinue therapy.
• For recurrence: Resume therapy at a reduced dose, or permanently discontinue

Grade 4: Withhold therapy until recovery to at least grade 1 or baseline.

• Once resolved, resume therapy at a reduced dose level or permanently discontinue as clinically indicated.
• For recurrence: Permanently discontinue therapy.

Precautions

CONTRAINDICATIONS: None

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 treatment, evaluate liver function tests (including ALT, AST, and bilirubin), electrolytes, electrocardiogram (ECG), and uric acid.
• Administer therapy orally at the same time each day on an empty stomach (with no food intake at least 2 hours before and 2 hours after administration); avoid grapefruit during therapy.
• Capsules should be swallowed whole; do not crush, chew, or open/dissolve the capsule contents.
• If a dose is missed or vomiting occurs anytime after dosing, administer the next dose at its scheduled time on the following day.

Storage requirements:

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

General:

• This drug may cause photosensitivity; sun protection is recommended during treatment and at least 5 days after discontinuation.

Monitoring:

• Cardiovascular: ECG (at baseline, then periodically as indicated during therapy; more often with risk factors)
• Hepatic: Liver function tests, including AST, ALT, and bilirubin (at baseline, every 2 weeks during the first two months, then monthly as indicated during therapy; more often if transaminase elevations occur)
• Metabolic: Electrolytes and serum uric acid (at baseline, then periodically as indicated during therapy)
• Musculoskeletal: Serum creatinine phosphokinase (every 2 weeks during the first month of therapy, then as indicated for muscle symptoms)
• Pulmonary: For new or worsening pulmonary symptoms (during therapy)

Patient advice:

• Read the US FDA-approved patient labeling (Patient Information).
• Avoid food or drink containing grapefruit during treatment.
• Minimize sun exposure and use sun protection, including broad-spectrum sunscreen, during treatment and for at least 5 days after discontinuation.
• Understand that laboratory testing is needed before and periodically (or as indicated) during treatment.
• Report any signs or symptoms of hepatotoxicity, worsening pulmonary function, QT prolongation, hyperuricemia, unexplained muscle pain, tenderness, or weakness, and/or bone fractures to your health care provider.
• 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 3 weeks after the last dose.
• Males (with female partners of reproductive potential): Use effective contraception during treatment and for 3 weeks 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.

Medical Disclaimer