Taletrectinib

Taletrectinib is an inhibitor of tyrosine kinase ROS1, including ROS1 resistance mutations. Taletrectinib also showed inhibitory effects on tropomyosin receptor kinases (TRKs) TRKA, TRKB, and TRKC.

• IBTROZI ® (taletrectinib) is indicated for the treatment of adult patients with locally advanced or metastatic ROS1 -positive non-small cell lung cancer (NSCLC) [see Dosage and Administration ( 2.1 )] . 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).ICD-10: C34.90

• None.contraindicated

Select patients for the treatment of locally advanced or metastatic NSCLC based on the presence of ROS1 rearrangement(s). ( 2.1 ) 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). ( 2.3 ) Continue treatment until disease progression or unacceptable toxicity. ( 2.3 ) 2.1 Patient Selection Select patients for the treatment of locally advanced or metastatic NSCLC with IBTROZI based on the presence of ROS1 rearrangement(s) in tumor specimens [see Clinical Studies ( 14.1 )] . An FDA-approved test to detect ROS1 rearrangement(s) for selecting patients for treatment with IBTROZI is not currently available. 2.2 Recommended Testing and Evaluation Before Initiating IBTROZI Before initiating IBTROZI, evaluate liver function tests (including ALT, AST, and bilirubin), electrolytes, ECG, and uric acid [see Warnings and Precautions ( 5.1 , 5.3 , 5.4 )]. 2.3 Recommended Dosage and Administration The recommended dosage of IBTROZI is 600 mg orally once daily on an empty stomach (no food intake at least 2 hours before and 2 hours after taking IBTROZI) [see Clinical Pharmacology ( 12.2 , 12.3 )] until disease progression or unacceptable toxicity. Take IBTROZI at approximately the same time each day. Swallow IBTROZI capsules whole. Do not open, chew, crush, or dissolve the capsule prior to swallowing. Avoid food or drink containing grapefruit during treatment with IBTROZI.

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. Immediately withhold in patients with suspected ILD/pneumonitis. Based on severity and resolution, resume at the same or reduced dose, or permanently discontinue. ( 2.4 , 5.2 ) 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. ( 2.4 , 5.3 ) 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. ( 2.4 , 5.4 ) 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. ( 2.4 , 5.5 ) Skeletal Fractures: Promptly evaluate patients with signs or symptoms (e.g., pain, changes in mobility, deformity) of fractures.

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 most frequently reported adverse reactions (≥20%) were: diarrhea, nausea, vomiting, dizziness, rash, constipation, and fatigue. ( 6.1 ) The most frequently reported Grade 3 or 4 laboratory abnormalities (≥5%) were: increased ALT, increased AST, decreased neutrophils, and increased creatine phosphokinase. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Nuvation Bio Inc. at 1-844-688-4550 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The pooled safety population described in the WARNINGS AND PRECAUTIONS section and below reflects exposure to IBTROZI as a single agent at 600 mg orally once daily until disease progression or unacceptable toxicity in 352 patients with ROS1 -positive NSCLC (N=337) and other solid tumors (N=15).

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on literature reports in humans with congenital mutations leading to changes in TRK signaling, findings from animal studies, and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , IBTROZI can cause fetal harm when administered to a pregnant woman. Limited data from case reports with IBTROZI used in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes. In animal reproduction studies, oral administration of taletrectinib to pregnant rats and rabbits during the period of organogenesis resulted in embryo-fetal mortalities and structural abnormalities at exposures that were below or equal to the human exposure based on AUC at the recommended dose ( see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Human Data Published reports of individuals with congenital mutations in TRK pathway proteins suggest that decreases in TRK-mediated signaling are correlated with obesity, developmental delays, cognitive impairment, insensitivity to pain, and anhidrosis.

Metabolism

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.

• Jun 11, 2025NDANDA219713Nuvation

1. 1Diarrhoea1430%
2. 2Nausea1226%
3. 3Fatigue613%
4. 4Vomiting613%
5. 5Decreased Appetite48.5%
6. 6Dysphagia48.5%
7. 7Pyrexia48.5%
8. 8Rash48.5%
9. 9Death36.4%
10. 10Disease Progression36.4%
11. 11Dizziness36.4%
12. 12Dyspepsia36.4%
13. 13Headache36.4%
14. 14Insomnia36.4%
15. 15Constipation24.3%

The 7 most recently updated of 7 ClinicalTrials.gov registrations naming Taletrectinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC)
  Suspended · Phase 2 · Interventional · 61 enrolled · Megan Kruse, MD
  NCT06214793updated 2026-06-05
• Phase 3 Study of Taletrectinib vs Placebo as an Adjuvant Therapy in ROS1 Positive NSCLC (TRUST-IV)
  Recruiting · Phase 3 · Interventional · 180 enrolled · Nuvation Bio Inc.
  NCT07154706updated 2026-05-19
• A Phase III Study Comparing Taletrectinib With Standard Therapy in ROS1 Positive Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients
  Recruiting · Phase 3 · Interventional · 194 enrolled · Nuvation Bio Inc.
  NCT06564324updated 2026-04-13
• Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC
  Active not recruiting · Phase 2 · Interventional · 217 enrolled · Nuvation Bio Inc.
  NCT04919811updated 2026-01-07
• Expanded Access Program of Taletrectinib in Patients With Advanced or Metastatic ROS1-Positive NSCLC
  No longer available · Expanded access · Nuvation Bio Inc.
  NCT06841874updated 2025-12-24
• Real-world Study of Taletrectinib in Advanced ROS1+ NSCLC Following Entrectinib Progression
  Not yet recruiting · Observational · 50 enrolled · Innovent Biologics (Suzhou) Co. Ltd.
  NCT07199010updated 2025-09-30
• Real-world Study of Taletrectinib for Advanced ROS1+ NSCLC With Brain Metastases
  Recruiting · Observational · 100 enrolled · Innovent Biologics (Suzhou) Co. Ltd.
  NCT07008287updated 2025-07-22

Frequently asked questions

How does Taletrectinib work?

Taletrectinib is an inhibitor of tyrosine kinase ROS1, including ROS1 resistance mutations. Taletrectinib also showed inhibitory effects on tropomyosin receptor kinases (TRKs) TRKA, TRKB, and TRKC.

What is Taletrectinib used for?

According to FDA labeling, Taletrectinib carries indications including: IBTROZI ® (taletrectinib) is indicated for the treatment of adult patients with locally advanced or metastatic ROS1 -positive non-small cell lung cancer (NSCLC) [see Dosage and Administration ( 2.1 )] . 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).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Taletrectinib?

Taletrectinib is classified as Kinase Inhibitor, Proto-Oncogene Tyrosine-Protein Kinase ROS1 Inhibitors, Tropomyosin Receptor Tyrosine Kinase A Inhibitors, Tropomyosin Receptor Tyrosine Kinase B Inhibitors, Tropomyosin Receptor Tyrosine Kinase C Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Taletrectinib?

Taletrectinib is marketed under brand names including Ibtrozi.

What are the contraindications for Taletrectinib?

Taletrectinib labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.