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

Background: Poly(ADP-ribose) polymerase-1 (PARP) inhibitors (PARPi) exploit tumour-specific defects in homologous recombination DNA repair and continuous dosing is most efficacious. Early clinical trial data with rucaparib suggested that it caused sustained PARP inhibition. Here we investigate the m...

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Veröffentlicht in:	British journal of cancer 2014-04, Vol.110 (8), p.1977-1984
Hauptverfasser:	Murray, J, Thomas, H, Berry, P, Kyle, S, Patterson, M, Jones, C, Los, G, Hostomsky, Z, Plummer, E R, Boddy, A V, Curtin, N J
Format:	Artikel
Sprache:	eng
Schlagworte:	631/92/436/108 631/92/436/2388 692/308/2778 692/699/67 Animals Biological and medical sciences Biomedical and Life Sciences Biomedicine Cancer Research Cancer therapies Cell Line, Tumor Chemotherapy Clinical trials Cytotoxicity DNA repair DNA Repair - drug effects Drug Administration Schedule Drug Resistance Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - blood Enzyme Inhibitors - pharmacokinetics Epidemiology Homologous Recombination - drug effects Humans Indoles - administration & dosage Indoles - blood Indoles - pharmacokinetics Medical research Medical sciences Mice Molecular Medicine Oncology Pharmacodynamics Pharmacokinetics Poly(ADP-ribose) Polymerase Inhibitors Poly(ADP-ribose) Polymerases - genetics R&D Research & development Schedules Translational Therapeutics Tumors Xenograft Model Antitumor Assays
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