期刊
FUTURE ONCOLOGY
卷 12, 期 12, 页码 1439-1456出版社
FUTURE MEDICINE LTD
DOI: 10.2217/fon-2016-0002
关键词
CO-338; companion diagnostic; ovarian cancer; PARP inhibitor; rucaparib
类别
Rucaparib camsylate (CO-338; 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one ((1S, 4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl) methane-sulfonic acid salt) is a PARP1, 2 and 3 inhibitor. Phase I studies identified a recommended PhaseyII dose of 600 mg orally twice daily. ARIEL2 Part 1 established a tumor genomic profiling test for homologous recombination loss of heterozygosity quantification using a next-generation sequencing companion diagnostic (CDx). Rucaparib received US FDA Breakthrough Therapy designation for treatment of platinum-sensitive BRCA-mutated advanced ovarian cancer patients who received greater than two lines of platinum-based therapy. Comparable to rucaparib development, other PARP inhibitors, such as olaparib, niraparib, veliparib and talazoparib, are developing CDx tests for targeted therapy. PARP inhibitor clinical trials and CDx assays are discussed in this review, as are potential PARP inhibitor combination therapies and likely resistance mechanisms.
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