Repotrectinib
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| Trade names | Augtyro |
| Other names | TPX-0005 |
| AHFS/Drugs.com | Augtyro |
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| Routes of administration | By mouth |
| Drug class | Tyrosine kinase inhibitor |
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| PDB ligand | |
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| Formula | C18H18FN5O2 |
| Molar mass | 355.373 g·mol−1 |
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Repotrectinib, sold under the brand name Augtyro, is an anti-cancer medication used for the treatment of non-small cell lung cancer.[1][2] It is taken by mouth.[1] Repotrectinib is an inhibitor of proto-oncogene tyrosine-protein kinase ROS1 (ROS1) and of the tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC.[1]
The most common adverse reactions include dizziness, dysgeusia, peripheral neuropathy, constipation, dyspnea, ataxia, fatigue, cognitive disorders, and muscular weakness.[2]
Repotrectinib was approved for medical use in the United States in November 2023.[2][3]
Medical uses[edit]
Repotrectinib is indicated for the treatment of adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer.[1][2]
History[edit]
Approval by the US Food and Drug Administration (FDA) was based on TRIDENT-1, a global, multicenter, single-arm, open-label, multi-cohort clinical trial (NCT03093116) which included participants with ROS1-positive locally advanced or metastatic non-small cell lung cancer.[2] Efficacy was evaluated in 71 ROS1 tyrosine kinase inhibitor-naïve participants who received up to one prior line of platinum-based chemotherapy and/or immunotherapy and 56 participants who received one prior ROS1 tyrosine kinase inhibitor with no prior platinum-based chemotherapy or immunotherapy.[2]
The FDA granted the application for repotrectinib priority review, breakthrough therapy, and fast track designations.[2]
References[edit]
- ^ a b c d e "Augtyro- repotrectinib capsule". DailyMed. 15 November 2023. Archived from the original on 12 December 2023. Retrieved 12 December 2023.
- ^ a b c d e f g This article incorporates text from this source, which is in the public domain.
- ^ "U.S. Food and Drug Administration Approves Augtyro (repotrectinib), a Next-Generation Tyrosine Kinase Inhibitor (TKI), for the Treatment of Locally Advanced or Metastatic ROS1-Positive Non-Small Cell Lung Cancer (NSCLC)" (Press release). Bristol Myers Squibb. 16 November 2023. Archived from the original on 16 November 2023. Retrieved 17 November 2023 – via Business Wire.
Further reading[edit]
- Drilon A, Ou SI, Cho BC, Kim DW, Lee J, Lin JJ, et al. (October 2018). "Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations". Cancer Discovery. 8 (10): 1227–1236. doi:10.1158/2159-8290.CD-18-0484. PMID 30093503.
External links[edit]
- "Repotrectinib (Code C133821)". NCI Thesaurus. 25 September 2023. Retrieved 17 November 2023.
- Clinical trial number NCT03093116 for "A Study of Repotrectinib (TPX-0005) in Patients With Advanced Solid Tumors Harboring ALK, ROS1, or NTRK1-3 Rearrangements (TRIDENT-1)" at ClinicalTrials.gov
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