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Wikipedia

Repotrectinib

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]

Repotrectinib
Clinical data
Trade namesAugtyro
Other namesTPX-0005
AHFS/Drugs.comAugtyro
License data
Routes of
administration
By mouth
Drug classTyrosine kinase inhibitor
ATC code
  • None
Legal status
Legal status
Identifiers
CAS Number
  • 1802220-02-5
PubChem CID
  • 135565923
DrugBank
  • DB16826
ChemSpider
  • 64853849
UNII
  • 08O3FQ4UNP
KEGG
  • D11454
ChEBI
  • CHEBI:229220
ChEMBL
  • ChEMBL4298138
PDB ligand
  • 7GI (PDBe, RCSB PDB)
Chemical and physical data
FormulaC18H18FN5O2
Molar mass355.373 g·mol−1
3D model (JSmol)
  • Interactive image
  • C[C@H]1CNC(=O)C2=C3N=C(N[C@H](C)C4=CC(F)=CC=C4O1)C=CN3N=C2
  • InChI=1S/C18H18FN5O2/c1-10-8-20-18(25)14-9-21-24-6-5-16(23-17(14)24)22-11(2)13-7-12(19)3-4-15(13)26-10/h3-7,9-11H,8H2,1-2H3,(H,20,25)(H,22,23)/t10-,11+/m0/s1
  • Key:FIKPXCOQUIZNHB-WDEREUQCSA-N

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

  1. ^ a b c d e "Augtyro- repotrectinib capsule". DailyMed. 15 November 2023. from the original on 12 December 2023. Retrieved 12 December 2023.
  2. ^ a b c d e f g "FDA approves repotrectinib for ROS1-positive non-small cell lung cancer". U.S. Food and Drug Administration (FDA). 15 November 2023. from the original on 16 November 2023. Retrieved 17 November 2023.   This article incorporates text from this source, which is in the public domain.
  3. ^ "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. 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


repotrectinib, sold, under, brand, name, augtyro, anti, cancer, medication, used, treatment, small, cell, lung, cancer, taken, mouth, inhibitor, proto, oncogene, tyrosine, protein, kinase, ros1, ros1, tropomyosin, receptor, tyrosine, kinases, trks, trka, trkb,. 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 RepotrectinibClinical dataTrade namesAugtyroOther namesTPX 0005AHFS Drugs comAugtyroLicense dataUS DailyMed RepotrectinibRoutes ofadministrationBy mouthDrug classTyrosine kinase inhibitorATC codeNoneLegal statusLegal statusUS only 1 IdentifiersCAS Number1802220 02 5PubChem CID135565923DrugBankDB16826ChemSpider64853849UNII08O3FQ4UNPKEGGD11454ChEBICHEBI 229220ChEMBLChEMBL4298138PDB ligand7GI PDBe RCSB PDB Chemical and physical dataFormulaC 18H 18F N 5O 2Molar mass355 373 g mol 13D model JSmol Interactive imageSMILES C C H 1CNC O C2 C3N C N C H C C4 CC F CC C4O1 C CN3N C2InChI InChI 1S C18H18FN5O2 c1 10 8 20 18 25 14 9 21 24 6 5 16 23 17 14 24 22 11 2 13 7 12 19 3 4 15 13 26 10 h3 7 9 11H 8H2 1 2H3 H 20 25 H 22 23 t10 11 m0 s1Key FIKPXCOQUIZNHB WDEREUQCSA NThe 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 Contents 1 Medical uses 2 History 3 References 4 Further reading 5 External linksMedical uses editRepotrectinib is indicated for the treatment of adults with locally advanced or metastatic ROS1 positive non small cell lung cancer 1 2 History editApproval 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 naive 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 FDA approves repotrectinib for ROS1 positive non small cell lung cancer U S Food and Drug Administration FDA 15 November 2023 Archived from the original on 16 November 2023 Retrieved 17 November 2023 nbsp 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 editDrilon 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 Portal nbsp Medicine nbsp This pharmacology related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Repotrectinib amp oldid 1196127567, wikipedia, wiki, book, books, library,

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