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D. Dua
Freeman Hospital
CancerB-cell lymphomaPARP inhibitorPancreatic cancerPoly (ADP-Ribose) Polymerase Inhibitor
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#1Ruth Plummer (Newcastle University)H-Index: 32
#2D. Dua (Freeman Hospital)H-Index: 1
Last. D. Sarker (St Thomas' Hospital)H-Index: 2
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ABSTRACT Aim: E7449 is an orally bioavailable, brain penetrable, potent small-molecule inhibitor of poly (ADP-ribose) polymerase (PARP) 1 and PARP 2 with an IC50 of 1.0 and 1.2 nmol/L respectively. E7449 is a poor P-gp substrate. Preclinically, E7449 potentiates the antitumour activity of chemotherapy and radiotherapy and has activity as a single-agent in BRCA-deficient and other tumours. A Phase 1 study of E7449 as a single agent is underway to determine the MTD, safety, PK, PD, preliminary act...
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