IBTROZI

Taletrectinib pharmacokinetics (PK) were characterized at steady state for the approved recommended dosage and the PK parameters presented below are as mean (CV%), unless otherwise specified. Taletrectinib maximum concentration (C max ) is 476 (36%) ng/mL and systemic exposure (AUC) is 9,649 (36%) ng

• h/mL. Taletrectinib C max and AUC increase in a dose proportional manner over the dose range of 50 mg to 1200 mg (0.08 to 2 times the approved recommended dosage). Taletrectinib accumulation is appr...

14.1 Locally Advanced or Metastatic ROS1 -Positive NSCLC The efficacy of IBTROZI was evaluated in 270 patients with ROS1 -positive locally advanced or metastatic NSCLC who received IBTROZI at a dose of 600 mg orally once daily, enrolled in two multicenter, single-arm, open-label clinical trials: TRUST-I (NCT04395677) or TRUST-II (NCT04919811). In both trials, patients were required to have histologically confirmed, locally advanced or metastatic, ROS1 -positive NSCLC, ECOG performance status of 0 or 1, and measurable disease per Response Evaluation Criteria in Solid Tumors (RECIST) v1.1. Ident...

The following adverse reactions are discussed in greater detail in the WARNINGS AND PRECAUTIONS section: Hepatotoxicity [see Warnings and Precautions ( 5.1 )] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions ( 5.2 )] QTc Interval Prolongation [see Warnings and Precautions ( 5.3 )] Hyperuricemia [see Warnings and Precautions ( 5.4 )] Myalgia with Creatine Phosphokinase Elevation [see Warnings and Precautions ( 5.5 )] Skeletal fractures [see Warnings and Precautions ( 5.6 )] The...

None. None ( 4 )

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. ( 2.4 , 5.1 ) Interstitial Lung Disease (ILD)/Pneumonitis: Monitor patients for new or worsening pulmonary symptoms indicative of ILD/pneumonitis. Imme...

7 DRUG INTERACTIONS Strong and Moderate CYP3A inhibitors : Avoid concomitant use. ( 7.1 ) Strong and Moderate CYP3A inducers: Avoid concomitant use. ( 7.1 ) 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...