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Selpercatinib information


Selpercatinib
Clinical data
Trade namesRetevmo, Retsevmo
Other namesLOXO-292
AHFS/Drugs.comMonograph
MedlinePlusa620036
License data
  • US DailyMed: Selpercatinib
Pregnancy
category
  • AU: D[1]
  • Use should be avoided
Routes of
administration
By mouth
Drug classTyrosine kinase inhibitor
ATC code
  • L01EX22 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1][2][3]
  • CA: ℞-only[4]
  • UK: POM (Prescription only)[5]
  • US: ℞-only[6]
  • EU: Rx-only[7][8]
Identifiers
IUPAC name
  • 6-(2-hydroxy-2-methylpropoxy)-4- (6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3- yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
CAS Number
  • 2152628-33-4
PubChem CID
  • 134436906
DrugBank
  • DB15685
ChemSpider
  • 72379991
UNII
  • CEGM9YBNGD
KEGG
  • D11713
ChEMBL
  • ChEMBL4559134
CompTox Dashboard (EPA)
  • DTXSID901026442 Edit this at Wikidata
Chemical and physical data
FormulaC29H31N7O3
Molar mass525.613 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • COc1ccc(CN2C3CC2CN(c2ccc(-c4cc(OCC(C)(C)O)cn5ncc(C#N)c45)cn2)C3)cn1
InChI
  • InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3
  • Key:XIIOFHFUYBLOLW-UHFFFAOYSA-N

Selpercatinib, sold under the brand name Retevmo among others, is a medication for the treatment of cancers in people whose tumors have an alteration (mutation or fusion) in a specific gene (RET which is short for "rearranged during transfection").[6][7][9] It is taken by mouth.[6]

The most common side effects include changes in laboratory tests (including increased liver enzymes, increased blood sugar, decreased white cell and platelet counts, decreased protein level, decreased calcium, increased total cholesterol, increased creatinine, and decreased sodium) dry mouth, diarrhea, high blood pressure, fatigue, edema, rash, and constipation.[6][9][10]

Selpercatinib is a kinase inhibitor, meaning it blocks a type of enzyme (kinase) and helps prevent the cancer cells from growing.[6][9] Before beginning treatment, the identification of a RET gene alteration must be determined using laboratory testing.[6][9]

Selpercatinib is the first therapy approved specifically for people with cancer and the RET gene alterations.[9] Selpercatinib received accelerated approval for this indication for patients aged twelve years of age and older in 2020.[9][11][12][10] In June 2024, the US Food and Drug Administration granted traditional approval to selpercatinib for people aged two years of age and older.[13]

  1. ^ a b "Retevmo APMDS". Therapeutic Goods Administration (TGA). 13 July 2023. Archived from the original on 20 September 2023. Retrieved 10 September 2023.
  2. ^ "Retevmo (Eli Lilly Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 28 July 2023. Archived from the original on 11 September 2023. Retrieved 10 September 2023.
  3. ^ "AusPAR: Retevmo". Therapeutic Goods Administration (TGA). 1 February 2024. Archived from the original on 31 March 2024. Retrieved 31 March 2024.
  4. ^ "Summary Basis of Decision (SBD) for Retevmo". Health Canada. 23 October 2014. Archived from the original on 29 May 2022. Retrieved 29 May 2022.
  5. ^ "Retsevmo 40 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). 27 June 2022. Archived from the original on 25 February 2022. Retrieved 22 September 2022.
  6. ^ a b c d e f "Retevmo- selpercatinib capsule". DailyMed. Archived from the original on 4 March 2021. Retrieved 31 March 2021.
  7. ^ a b Cite error: The named reference Retsevmo EPAR was invoked but never defined (see the help page).
  8. ^ "Retsevmo Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
  9. ^ a b c d e f "FDA Approves First Therapy for Patients with Lung and Thyroid Cancers with a Certain Genetic Mutation or Fusion" (Press release). U.S. Food and Drug Administration (FDA). 8 May 2020. Archived from the original on 9 May 2020. Retrieved 8 May 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  10. ^ a b "Drug Trials Snapshots: Retevmo". U.S. Food and Drug Administration (FDA). 8 May 2020. Archived from the original on 20 October 2020. Retrieved 1 June 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  11. ^ "Drug Approval Package: Retevmo". U.S. Food and Drug Administration (FDA). 7 August 2020. Archived from the original on 18 January 2022. Retrieved 22 September 2022.
  12. ^ "Lilly Receives U.S. FDA Approval for Retevmo (selpercatinib), the First Therapy Specifically for Patients with Advanced RET-Driven Lung and Thyroid Cancers" (Press release). Eli Lilly and Company. 8 May 2020. Archived from the original on 9 May 2020. Retrieved 8 May 2020 – via PR Newswire.
  13. ^ Cite error: The named reference FDA PR 20240612 was invoked but never defined (see the help page).

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