Last reviewed 2026-04-20 · How we verify

Ibtrozi (TALETRECTINIB)

Ibtrozi works by blocking the ROS1 protein, which is a genetic mutation found in some lung cancer cells.

Ibtrozi (taletrectinib) is a small molecule drug developed by Nuvation, currently owned by the same company. It is approved by the FDA for the treatment of locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC). Ibtrozi works by targeting a specific genetic mutation in cancer cells, ROS1, to inhibit tumor growth. The drug has a half-life of 66 hours and is patented, with no generic manufacturers available. Key safety considerations include the need for regular monitoring of liver function and potential side effects such as fatigue and nausea.

At a glance

Mechanism of action

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. Fusion proteins that include ROS1 domains can drive tumorigenic potential through hyperactivation of downstream signaling pathways leading to unconstrained cell proliferation. Taletrectinib inhibited growth of cancer cells expressing ROS1 fusion genes and mutations. In mice subcutaneously implanted with tumors harboring ROS1 fusions, including the G2032R mutation, administration of taletrectinib resulted in tumor growth inhibition. Taletrectinib had anticancer activity in an intracranial NSCLC xenograft model harboring a ROS1 fusion.

Approved indications

• locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC)

Common side effects

• Diarrhea
• Nausea
• Vomiting
• Constipation
• Dizziness
• Rash
• Fatigue
• Peripheral neuropathy
• Dysgeusia
• Decreased appetite
• Cough
• Hemoglobin decreased

Drug interactions

• Strong and Moderate CYP3A inhibitors
• Strong and Moderate CYP3A inducers
• Proton pump inhibitors (PPIs)
• H2 receptor antagonists
• Locally acting antacids
• Drugs That Prolong the QTc Interval
• Antiarrhythmic drugs

Key clinical trials

• A Study of AB-106 in Subjects With Advanced NSCLC Harboring ROS1 Fusion Gene (PHASE2)
• Phase 3 Study of Taletrectinib vs Placebo as an Adjuvant Therapy in ROS1 Positive NSCLC (TRUST-IV) (PHASE3)
• Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC (PHASE2)
• Expanded Access Program of Taletrectinib in Patients With Advanced or Metastatic ROS1-Positive NSCLC
• A Phase III Study Comparing Taletrectinib With Standard Therapy in ROS1 Positive Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients (PHASE3)
• Real-world Study of Taletrectinib in Advanced ROS1+ NSCLC Following Entrectinib Progression
• Real-world Study of Taletrectinib for Advanced ROS1+ NSCLC With Brain Metastases
• Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC) (PHASE2)

Patents

Primary sources

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