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 | |
Other names
AG014699 | |
Identifiers | |
283173-50-2 ![]() | |
ChemSpider | 8107584 |
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Jmol-3D images | Image |
KEGG | D10079 ![]() |
PubChem | 9931954 |
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Properties | |
Molecular formula |
C19H18FN3O |
Molar mass | 323.36 g·mol−1 |
Except where noted otherwise, data is 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 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."[1]
It can be taken orally in tablet form.[2]
It has undergone phase I clinical trials for patients with advanced solid tumours.[3] It is in phase II clinical trials for metastatic breast and ovarian cancer with known BRCA1 or BRCA2 mutation.[4][2]
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.[5]
References
- ↑ http://www.qub.ac.uk/schools/SchoolofPharmacy/Filestore/Filetoupload,121186,en.pdf
- ↑ 2.0 2.1 "Cancer Research launches new drug trial". 11 Jan 2011.
- ↑ "First in human phase I trial of the PARP inhibitor AG-014699 with temozolomide (TMZ) in patients (pts) with advanced solid tumors".
- ↑ http://science.cancerresearchuk.org/research/loc/newcastle/newcastle_univ/plummerr/plummerrfr/plummerrfrp2/?version=1 URL no longer relevant
- ↑ Rucaparib trials