Rucaparib

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Rucaparib
200px
Names
IUPAC name
8-Fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one
Other names
AG014699
Identifiers
283173-50-2 YesY
ChemSpider 8107584
7736
Jmol 3D model Interactive image
KEGG D10079 YesY
PubChem 9931954
  • InChI=1S/C19H18FN3O/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24)
  • Fc4cc2c1c(nc(c1CCNC2=O)c3ccc(cc3)CNC)c4
Properties
C19H18FN3O
Molar mass 323.37 g·mol−1
Vapor pressure {{{value}}}
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Rucaparib (AG 014699) is a PARP inhibitor being investigated as a potential anti-cancer agent. Rucaparib is the first-in-class clinical candidate targeting the DNA repair enzyme poly-ADPribose polymerase-1 (PARP-1), and was first synthesised as part of a collaboration between scientists working in Northern Institute of Cancer Research and Medical School of Newcastle University, alongside Agouron Pharmaceuticals (San Diego).[1] Rucaparib inhibits "the contraction of isolated vascular smooth muscle, including that from the tumours of cancer patients. It also reduces the migration of some cancer and normal cells in culture."[2]

It can be taken orally in tablet form.[3]

It has undergone phase I clinical trials for patients with advanced solid tumours.[4] It is in phase II clinical trials for metastatic breast and ovarian cancer with known BRCA1 or BRCA2 mutation.[3][5]

It is thought that 20% of women with ovarian cancer who are not BRCA positive might also benefit from PARP inhibitors. Clinical trials are beginning (as of April, 2014)

As of November 2012 four clinical trials of rucaparib were recruiting patients.[6]

References

  1. J Med Chem. 2000 Nov 2;43(22):4084-97. DOI: 10.1021/jm000950v
  2. http://www.qub.ac.uk/schools/SchoolofPharmacy/Filestore/Filetoupload,121186,en.pdf
  3. 3.0 3.1 Lua error in package.lua at line 80: module 'strict' not found.
  4. Lua error in package.lua at line 80: module 'strict' not found.
  5. http://science.cancerresearchuk.org/research/loc/newcastle/newcastle_univ/plummerr/plummerrfr/plummerrfrp2/?version=1 URL no longer relevant
  6. Rucaparib trials


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