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Sotorasib information


Sotorasib
Clinical data
Pronunciation/ˌstəˈræsɪb/
SOH-tə-RAS-ib
Trade namesLumakras, Lumykras
Other namesAMG 510
AHFS/Drugs.comMonograph
MedlinePlusa621036
License data
  • US DailyMed: Sotorasib
Pregnancy
category
  • AU: B3[1][2]
Routes of
administration
By mouth
ATC code
  • L01XX73 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • CA: ℞-only[3]
  • US: ℞-only[4][5]
  • EU: Rx-only[6]
Identifiers
IUPAC name
  • 6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-(1M)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-4-[(2S)-2- methyl-4-(prop-2-enoyl)piperazin-1-yl]pyrido[2,3-d]pyrimidin-2(1H)-one
CAS Number
  • 2296729-00-3 checkY
  • non-specific: 2252403-56-6 checkY
PubChem CID
  • 137278711
DrugBank
  • DB15569
ChemSpider
  • 72380148
UNII
  • 2B2VM6UC8G
KEGG
  • D12055
ChEBI
  • CHEBI:178199
CompTox Dashboard (EPA)
  • DTXSID001099260 Edit this at Wikidata
Chemical and physical data
FormulaC30H30F2N6O3
Molar mass560.606 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CC(C)c1nccc(C)c1N2C(=O)N=C(N3CCN(C[C@@H]3C)C(=O)C=C)c4cc(F)c(nc24)c5c(O)cccc5F
InChI
  • InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3/t18-/m0/s1
  • Key:NXQKSXLFSAEQCZ-SFHVURJKSA-N

Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer.[4][5] It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for various forms of cancer.[7][8] Sotorasib is an inhibitor of the RAS GTPase family.[4]

The most common side effects include diarrhea, musculoskeletal pain, nausea, fatigue, liver damage and cough.[4][5]

Sotorasib is the first approved targeted therapy for patients with tumors with any KRAS mutation, which accounts for approximately 25% of mutations in non-small cell lung cancers.[5] KRAS G12C mutations occur in about 13% of patients with non-small cell lung cancers.[5] Sotorasib was approved for medical use in the United States in May 2021,[5][9] and in the European Union in January 2022.[6] The US Food and Drug Administration considers it to be a first-in-class medication.[10]

  1. ^ a b "Lumakras APMDS". Therapeutic Goods Administration (TGA). 13 April 2022. Archived from the original on 12 April 2022. Retrieved 23 April 2022.
  2. ^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 21 December 2022. Archived from the original on 3 April 2022. Retrieved 2 January 2023.
  3. ^ "Summary Basis of Decision (SBD) for Lumakras". Health Canada. 23 October 2014. Archived from the original on 29 May 2022. Retrieved 29 May 2022.
  4. ^ a b c d "Lumakras- sotorasib tablet, coated". DailyMed. Archived from the original on 6 June 2021. Retrieved 6 June 2021.
  5. ^ a b c d e f "FDA Approves First Targeted Therapy for Lung Cancer Mutation Previously Considered Resistant to Drug Therapy". U.S. Food and Drug Administration (FDA). 28 May 2021. Archived from the original on 28 May 2021. Retrieved 28 May 2021. Public Domain This article incorporates text from this source, which is in the public domain.
  6. ^ a b Cite error: The named reference Lumykras EPAR was invoked but never defined (see the help page).
  7. ^ "KRAS mutant-targeting AMG 510". NCI Drug Dictionary. National Cancer Institute. 2 February 2011. Archived from the original on 10 July 2019. Retrieved 16 November 2019.
  8. ^ Canon J, Rex K, Saiki AY, Mohr C, Cooke K, Bagal D, et al. (November 2019). "The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity". Nature. 575 (7781): 217–223. Bibcode:2019Natur.575..217C. doi:10.1038/s41586-019-1694-1. PMID 31666701. S2CID 204969251.
  9. ^ Cite error: The named reference CNBC 20210528 was invoked but never defined (see the help page).
  10. ^ Advancing Health Through Innovation: New Drug Therapy Approvals 2021 (PDF). U.S. Food and Drug Administration (FDA) (Report). 13 May 2022. Archived from the original on 6 December 2022. Retrieved 22 January 2023. Public Domain This article incorporates text from this source, which is in the public domain.

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