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 | |
3D model (JSmol)
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| ChemSpider | |
| ECHA InfoCard | 100.247.490 |
| KEGG | |
PubChem CID
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CompTox Dashboard (EPA)
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| Properties | |
| C19H18FN3O | |
| Molar mass | 323.371 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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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] It is being developed by Clovis Oncology.
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]
Clinical trials
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]
As of April 2016[update] the ARIEL3 phase III clinical trial for maintenance after platinum-based chemotherapy for serous and endometrioid ovarian cancer is active.[7]
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
- ^ a b "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
- ^ A Study of Rucaparib as Switch Maintenance Following Platinum-Based Chemotherapy in Patients With Platinum-Sensitive, High-Grade Serous or Endometrioid Epithelial Ovarian, Primary Peritoneal or Fallopian Tube Cancer (ARIEL3)
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