Rucaparib
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Names | |
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IUPAC name
8-Fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one
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Other names
AG014699
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Identifiers | |
283173-50-2 | |
ChemSpider | 8107584 |
7736 | |
Jmol 3D model | Interactive image |
KEGG | D10079 |
PubChem | 9931954 |
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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).
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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[update] four clinical trials of rucaparib were recruiting patients.[6]
References
- ↑ J Med Chem. 2000 Nov 2;43(22):4084-97. DOI: 10.1021/jm000950v
- ↑ http://www.qub.ac.uk/schools/SchoolofPharmacy/Filestore/Filetoupload,121186,en.pdf
- ↑ 3.0 3.1 Lua error in package.lua at line 80: module 'strict' not found.
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ http://science.cancerresearchuk.org/research/loc/newcastle/newcastle_univ/plummerr/plummerrfr/plummerrfrp2/?version=1 URL no longer relevant
- ↑ Rucaparib trials
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