Article
The poly(ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial.
The Lancet. Oncology - 1 Aug 2013
Sandhu Shahneen K, Schelman William R, Wilding George, Moreno Victor, Baird Richard D, Miranda Susana, Hylands Lucy, Riisnaes Ruth, Forster Martin, Omlin Aurelius, Kreischer Nathan, Thway Khin, Gevensleben Heidrun, Sun Linda, Loughney John, Chatterjee Manash, Toniatti Carlo, Carpenter Christopher L, Iannone Robert, Kaye Stan B, de Bono Johann S, Wenham Robert M
Abstract excerpt
BACKGROUND: Poly(ADP-ribose) polymerase (PARP) is implicated in DNA repair and transcription regulation. Niraparib (MK4827) is an oral potent, selective PARP-1 and PARP-2 inhibitor that induces synthetic lethality in preclinical tumour models with loss of BRCA and PTEN function. We investigated the safety, tolerability, maximum tolerated dose, pharmacokinetic and pharmacodynamic profiles, and preliminary...
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