Initial US Approval:
2025
Key Clinical Studies:
TRUST-I (NCT04395677) and TRUST-II (NCT04919811)
Drug Class/Description:
Kinase inhibitor
Indications and Usage:
IBTROZI is a kinase inhibitor indicated for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).
Dosage and Administration:
- Select patients for the treatment of locally advanced or metastatic NSCLC based on the presence of ROS1 rearrangement(s).
- Recommended Dosage: 600 mg orally once daily on an empty stomach (no food intake at least 2 hours before and 2 hours after taking IBTROZI).
- Continue treatment until disease progression or unacceptable toxicity.
Dosage Forms and Strengths:
Capsules: 200 mg of taletrectinib
Contraindications:
None
Warnings and Precautions:
- Hepatotoxicity: Monitor liver function tests prior to initiating, every 2 weeks during the first 2 months of treatment, then monthly thereafter as clinically indicated, with more frequent testing in patients who develop transaminase elevations. Based on severity and resolution, withhold and then resume at reduced dose, or permanently discontinue.
- Interstitial Lung Disease (ILD)/Pneumonitis: Monitor patients for new or worsening pulmonary symptoms indicative of ILD/pneumonitis. Immediately withhold in patients with suspected ILD/pneumonitis. Based on severity and resolution, resume at the same or reduced dose, or permanently discontinue.
- QTc Interval Prolongation: Monitor ECG and electrolytes prior to initiating and periodically during treatment. Based on severity and resolution, withhold and then resume at same or reduced dose, or permanently discontinue.
- Hyperuricemia: Monitor serum uric acid levels prior to initiating and periodically during treatment. Initiate treatment with urate-lowering medications as clinically indicated. Withhold and resume at same or reduced dose or permanently discontinue based on severity.
- Myalgia with Creatine Phosphokinase (CPK) Elevation: Monitor serum CPK levels during treatment in patients reporting unexplained muscle pain, tenderness, or weakness. Based on severity, withhold and resume at same or reduced dose upon improvement.
- Skeletal Fractures: Promptly evaluate patients with signs or symptoms (e.g., pain, changes in mobility, deformity) of fractures.
- Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception.
Adverse Reactions:
The most frequently reported adverse reactions (≥20%) were: diarrhea, nausea, vomiting, dizziness, rash, constipation, and fatigue.
The most frequently reported Grade 3 or 4 laboratory abnormalities (≥5%) were: increased ALT, increased AST, decreased neutrophils, and increased creatine phosphokinase.
Drug Interactions:
- Strong and Moderate CYP3A inhibitors: Avoid concomitant use.
- Strong and Moderate CYP3A inducers: Avoid concomitant use.
- Gastric Acid Reducing Agents: Avoid concomitant use with proton pump inhibitors (PPIs) and H2 receptor antagonists. If an acid-reducing agent cannot be avoided, administer IBTROZI 2 hours before or 2 hours after taking a locally acting antacid.
- Drugs That Prolong the QTc Interval: Avoid concomitant use.
Use in Specific Populations:
- Lactation: Advise not to breastfeed.
Adapted From:
https://www.ibtrozi-pi.com/IBTROZI_taletrectinib-prescribing-information.pdf
Every health-care provider should make their own determination regarding specific safe and appropriate patient care practices, including drug dosages and indications. The provider should always consult the most recent prescribing/product information. FDA Focus information is not guaranteed to be accurate, complete, or current. JADPRO and its editors, authors, reviewers, and commentators cannot be held responsible for any liability incurred as a consequence of the application of any of the information listed within.
