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abstract
Drug Evaluation
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)methanesulfonic acid
salt) is a PARP1, 2 and 3 inhibitor. Phase I studies identified a
recommended Phase II 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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