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Olaparib information


Olaparib
Clinical data
Trade namesLynparza, others
Other namesAZD-2281, MK-7339, KU0059436
AHFS/Drugs.comMonograph
MedlinePlusa614060
License data
  • US DailyMed: Olaparib
Pregnancy
category
  • AU: D[1]
Routes of
administration
By mouth
ATC code
  • L01XK01 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[2]
  • CA: ℞-only[3][4]
  • UK: POM (Prescription only)[5][6]
  • US: ℞-only[7][8]
  • EU: Rx-only[9]
  • In general: ℞ (Prescription only)
Identifiers
IUPAC name
  • 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl) -4-fluorophenyl]methyl(2H)phthalazin-1-one
CAS Number
  • 763113-22-0 ☒N
PubChem CID
  • 23725625
IUPHAR/BPS
  • 7519
DrugBank
  • DB09074 ☒N
ChemSpider
  • 23343272 checkY
UNII
  • WOH1JD9AR8
KEGG
  • D09730
ChEBI
  • CHEBI:83766 ☒N
ChEMBL
  • ChEMBL521686 checkY
PDB ligand
  • 09L (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID60917988 Edit this at Wikidata
ECHA InfoCard100.170.811 Edit this at Wikidata
Chemical and physical data
FormulaC24H23FN4O3
Molar mass434.471 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • c4cccc2c4c(n[nH]c2=O)Cc(ccc1F)cc1C(=O)N3CCN(CC3)C(=O)C5CC5
InChI
  • InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30) checkY
  • Key:FDLYAMZZIXQODN-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Olaparib, sold under the brand name Lynparza, is a medication for the maintenance treatment of BRCA-mutated advanced ovarian cancer in adults. It is a PARP inhibitor, inhibiting poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair. It acts against cancers in people with hereditary BRCA1 or BRCA2 mutations, which include some ovarian, breast, and prostate cancers.[10]

In December 2014, olaparib was approved for use as a single agent by the European Medicines Agency (EMA) in the European Union and by the Food and Drug Administration (FDA) in the United States.[11][12][13][14]

  1. ^ https://www.tga.gov.au/resources/auspar/auspar-olaparib-1
  2. ^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  3. ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  4. ^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
  5. ^ "Lynparza 50 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). 7 October 2019. Archived from the original on 23 September 2020. Retrieved 13 April 2020.
  6. ^ "Lynparza 100mg Film-Coated Tablets - Summary of Product Characteristics (SmPC)". (emc). 7 October 2019. Retrieved 13 April 2020.
  7. ^ Cite error: The named reference Lynparza capsule PI was invoked but never defined (see the help page).
  8. ^ Cite error: The named reference Lynparza FDA label was invoked but never defined (see the help page).
  9. ^ "Lynparza EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 6 October 2020.
  10. ^ Fong PC, Boss DS, Yap TA, Tutt A, Wu P, Mergui-Roelvink M, et al. (July 2009). "Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers". The New England Journal of Medicine. 361 (2): 123–134. doi:10.1056/NEJMoa0900212. PMID 19553641.
  11. ^ "Lynparza (olaparib): An overview of Lynparza and why it is authorised in the EU" (PDF). European Medicines Agency (EMA). Archived from the original (PDF) on 16 March 2018. Retrieved 13 April 2020.
  12. ^ "Lynparza EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 13 April 2020.
  13. ^ "Drug Approval Package: Lynparza (olaparib) Capsules NDA #206162". U.S. Food and Drug Administration (FDA). 22 January 2015. Retrieved 13 April 2020.
  14. ^ "FDA approves Lynparza to treat advanced ovarian cancer". U.S. Food and Drug Administration (FDA) (Press release). 19 December 2014. Archived from the original on 19 December 2014. Retrieved 30 December 2019. Public Domain This article incorporates text from this source, which is in the public domain.

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