Chemistry:Taletrectinib
Taletrectinib, sold under the brand name Ibtrozi, is an anti-cancer medication used for the treatment of non-small cell lung cancer.[1][2] It is used as the salt, taletrectinib adipate.[1] Taletrectinib is a kinase inhibitor.[1] It is taken by mouth.[1]
Taletrectinib was approved for medical use in the United States in June 2025.[3][4]
Medical uses
Taletrectinib is indicated for the treatment of adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer.[1][4]
Adverse effects
The US Food and Drug Administration (FDA) prescribing information for taletrectinib includes warnings and precautions for hepatotoxicity, interstitial lung disease/pneumonitis, QTc interval prolongation, hyperuricemia, myalgia with creatine phosphokinase elevation, skeletal fractures, and embryo-fetal toxicity.[1][3]
History
The US Food and Drug Administration (FDA) approved taletrectinib based on evidence from 270 participants with ROS1-positive NSCLC that had spread beyond the lungs who received taletrectinib 600 mg orally once daily, enrolled in two clinical trials: TRUST-I (NCT04395677) or TRUST-II (NCT04919811).[4] The TRUST-I trial was conducted exclusively in China and the TRUST-II trial was conducted globally in North America (United States and Canada), Europe (France, Italy, Spain, and Poland), and Asia (China, Japan, and South Korea).[4]
The efficacy of taletrectinib to treat ROS1-positive non-small cell lung cancer was evaluated in participants with locally advanced or metastatic, ROS1-positive non-small cell lung cancer enrolled in two multi-center, single-arm, open-label clinical trials, TRUST-I (NCT04395677) and TRUST-II (NCT04919811).[3] The efficacy population included 157 participants (103 in TRUST-I; 54 in TRUST-II) who were naïve to treatment with a ROS1 tyrosine kinase inhibitor (TKI) and 113 participants (66 in TRUST-I; 47 in TRUST-II) who had received one prior ROS1 tyrosine kinase inhibitor.[3] Participants may have received prior chemotherapy for advanced disease.[3]
The safety of taletrectinib was evaluated in 352 participants (337 with non-small cell lung cancer and 15 with other solid tumors) who received at least one 600 mg dose of taletrectinib.[4] In the 337 participants with non-small cell lung cancer, the median age was 56 years (range: 26 to 83); 56% female; 76% Asian, 15% White, 0.6% Black or African American, 8% unknown or other races; and 1.8% were of Hispanic or Latino ethnicity.[4] The number of participants representing efficacy findings differs from the number of participants representing safety findings due to different groups of study participants analyzed for efficacy and safety.[4]
The FDA granted the application for taletrectinib priority review, breakthrough therapy, and orphan drug designations.[3]
Society and culture
Legal status
Taletrectinib was approved for medical use in the United States in June 2025.[3][5]
Names
Taletrectinib is the international nonproprietary name.[6]
Taletrectinib is sold under the brand name Ibtrozi.[3][5]
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 Cite error: Invalid
<ref>tag; no text was provided for refs namedIbtrozi FDA label - ↑ "Efficacy and safety of taletrectinib for treatment of ROS1-positive non-small cell lung cancer: A systematic review". Expert Opinion on Pharmacotherapy 26 (6): 765–772. April 2025. doi:10.1080/14656566.2025.2487150. PMID 40170301.
- ↑ 3.0 3.1 3.2 3.3 3.4 3.5 3.6 3.7 "FDA approves taletrectinib for ROS1-positive non-small cell lung cancer". 11 June 2025. https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-taletrectinib-ros1-positive-non-small-cell-lung-cancer.
This article incorporates text from this source, which is in the public domain.
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 "Drug Trials Snapshots: Ibtrozi". 11 June 2025. https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trials-snapshots-ibtrozi. This article incorporates text from this source, which is in the public domain.
- ↑ 5.0 5.1 "U.S. Food and Drug Administration Approves Nuvation Bio's Ibtrozi (taletrectinib), a Next-Generation Oral Treatment for Advanced ROS1-Positive Non-Small Cell Lung Cancer". Nuvation Bio (Press release). 12 June 2025. Retrieved 13 June 2025.
- ↑ "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 85". WHO Drug Information 35 (1). 2021.
External links
- Clinical trial number NCT04395677 for "A Study of AB-106 in Subjects With Advanced NSCLC Harboring ROS1 Fusion Gene" at ClinicalTrials.gov
- Clinical trial number NCT04919811 for "Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC (TRUST-II)" at ClinicalTrials.gov
 |  |
