Title : Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules.

Pub. Date : 2014 Apr 15

PMID : 24556618






3 Functional Relationships(s)
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1 Early clinical trial data with rucaparib suggested that it caused sustained PARP inhibition. rucaparib poly (ADP-ribose) polymerase family, member 1 Mus musculus
2 Rucaparib is retained in cells and inhibits PARP >=50% for >=72 h days after a 30-min pulse of 400 nM. rucaparib poly (ADP-ribose) polymerase family, member 1 Mus musculus
3 CONCLUSIONS: Rucaparib accumulates and is retained in tumour cells and inhibits PARP for long periods such that weekly schedules have equivalent anticancer activity to daily dosing in a pre-clinical model, suggesting that clinical evaluation of alternative schedules of rucaparib should be considered. rucaparib poly (ADP-ribose) polymerase family, member 1 Mus musculus