Rucaparib (phosphate)

Rucaparib is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor.¹ It reduces PARP1 activity in D283 Med medulloblastoma cells by 91.7% when used at a concentration of 1 µM. Rucaparib selectively inhibits the proliferation of MDA-MB-436 breast cancer cells expressing mutant BRCA1 (IC₅₀s = 1.3 µM) over MCF-7 breast cancer cells expressing wild-type BRCA1 and BRCA2 (IC₅₀s = 20.2 µM).² It potentiates the growth inhibition induced by the DNA alkylating agent prodrug temozolomide (Item No. 14163) in D283 Med and D384 Med medulloblastoma cells when used at a concentration of 0.4 µM.¹ In vivo, rucaparib (1 mg/kg per day) potentiates temozolomide-induced delays in tumor growth in D283 Med and D384 Med mouse xenograft models. Formulations containing rucaparib have been used in the treatment of BRCA mutation-associated, drug-resistant ovarian, fallopian tube, or primary peritoneal cancers.

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1. Daniel, R.A., Rozanska, A.L., Mulligan, E.A., et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br. J. Cancer 103(10), 1588-1596 (2010).

2. Drew, Y., Mulligan, E.A., Vong, W.T., et al. Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2. JNCI 103(4), 334-346 (2011).