Taletrectinib

Last updated

Taletrectinib
Taletrectinib.svg
Clinical data
Trade names Ibtrozi
AHFS/Drugs.com Monograph
MedlinePlus a625089
License data
Routes of
administration 		By mouth
Drug class Antineoplastic
ATC code
  • None
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C23H24FN5O
Molar mass 405.477 g·mol−1
3D model (JSmol)
  • C[C@@H](N)COc1ccc(-c2cnc3ccc(N[C@H](C)c4cccc(F)c4)nn23)cc1
  • InChI=1S/C23H24FN5O/c1-15(25)14-30-20-8-6-17(7-9-20)21-13-26-23-11-10-22(28-29(21)23)27-16(2)18-4-3-5-19(24)12-18/h3-13,15-16H,14,25H2,1-2H3,(H,27,28)/t15-,16-/m1/s1
  • Key:HEVHTYMYEMEBPX-HZPDHXFCSA-N

  • as salt: InChI=1S/C23H24FN5O.C6H10O4/c1-15(25)14-30-20-8-6-17(7-9-20)21-13-26-23-11-10-22(28-29(21)23)27-16(2)18-4-3-5-19(24)12-18;7-5(8)3-1-2-4-6(9)10/h3-13,15-16H,14,25H2,1-2H3,(H,27,28);1-4H2,(H,7,8)(H,9,10)/t15-,16-;/m1./s1
  • Key:DORJQZDOULKINH-QNBGGDODSA-N

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]

Contents

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

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. 1 2 3 4 5 6 7 "Ibtrozi- taletrectinib capsule". DailyMed. 11 June 2025. Retrieved 6 July 2025.
  2. ↑ Khan I, Sahar A, Numra S, Saha N, Nidhi, Parveen R (April 2025). "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. doi:10.1080/14656566.2025.2487150. PMID   40170301.
  3. 1 2 3 4 5 6 7 8 "FDA approves taletrectinib for ROS1-positive non-small cell lung cancer". U.S. Food and Drug Administration (FDA). 11 June 2025. Retrieved 13 June 2025.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  4. 1 2 3 4 5 6 7 "Drug Trials Snapshots: Ibtrozi". U.S. Food and Drug Administration. 11 June 2025. Retrieved 5 September 2025.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  5. 1 2 "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.
  6. ↑ World Health Organization (2021). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 85". WHO Drug Information. 35 (1). hdl: 10665/340684 .


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