Taletrectinib

Taletrectinib
Clinical data
Trade names	Ibtrozi
License data	US DailyMed: Taletrectinib;
Routes of; administration	By mouth
Drug class	Antineoplastic
ATC code	None;
Legal status
Legal status	US: ℞-only;
Identifiers
CAS Number	1505514-27-1; as salt: 1505515-69-4;
PubChem CID	72202474; as salt: 72694302;
DrugBank	DB18711;
UNII	W4141180YD; as salt: 6KLL51GNBG;
KEGG	D12363; as salt: D12364;
ChEMBL	ChEMBL4650989; as salt: ChEMBL4650361;
Chemical and physical data
Formula	C23H24FN5O
Molar mass	405.477 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H](N)COc1ccc(-c2cnc3ccc(N[C@H](C)c4cccc(F)c4)nn23)cc1;
	InChI 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] 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.^[2]

Medical uses

Taletrectinib is indicated for the treatment of adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer.^[1]

Adverse effects

The 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]^[2]

History

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).^[2] 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.^[2] Participants may have received prior chemotherapy for advanced disease.^[2] The US Food and Drug Administration (FDA) granted the application for taletrectinib priority review, breakthrough therapy, and orphan drug designations.^[2]

Society and culture

Legal status

Taletrectinib was approved for medical use in the United States in June 2025.^[2]^[3]

Names

Taletrectinib is the international nonproprietary name.^[4]

Taletrectinib is sold under the brand name Ibtrozi.^[2]^[3]

References

^ ^a ^b ^c ^d ^e ^f ^g https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/219713s000lbl.pdf
^ ^a ^b ^c ^d ^e ^f ^g ^h "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. This article incorporates text from this source, which is in the public domain.
^ ^a ^b "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.
^ World Health Organization (2021). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 85". WHO Drug Information. 35 (1). hdl:10665/340684.

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

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[Ibtrozi_FDA_label-1] ^ ^a ^b ^c ^d ^e ^f ^g https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/219713s000lbl.pdf

[FDA_Ibtrozi-2] ^ ^a ^b ^c ^d ^e ^f ^g ^h "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. This article incorporates text from this source, which is in the public domain.

[Nuvation_Bio_PR-3] "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.

[4] 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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