[HTML][HTML] Improved pharmacodynamic (PD) assessment of low dose PARP inhibitor PD activity for radiotherapy and chemotherapy combination trials

R de Haan, D Pluim, B van Triest… - Radiotherapy and …, 2018 - Elsevier
Background PARP inhibitors are currently evaluated in combination with radiotherapy
and/or chemotherapy. As sensitizers, PARP inhibitors are active at very low concentrations …

[HTML][HTML] Study protocols of three parallel phase 1 trials combining radical radiotherapy with the PARP inhibitor olaparib

R De Haan, E Van Werkhoven, MM Van Den Heuvel… - BMC cancer, 2019 - Springer
Abstract Background Poly (ADP-ribose) Polymerase (PARP) inhibitors are promising novel
radiosensitisers. Pre-clinical models have demonstrated potent and tumour-specific …

PARP inhibitors as antitumor agents: a patent update (2013-2015)

Z Yuan, J Chen, W Li, D Li, C Chen… - Expert Opinion on …, 2017 - Taylor & Francis
Introduction: PARP inhibitors have been extensively explored as antitumor agents and have
shown potent efficacy both in vitro and in vivo. They can be used in monotherapy under the …

Extent of radiosensitization by the PARP inhibitor olaparib depends on its dose, the radiation dose and the integrity of the homologous recombination pathway of …

CVM Verhagen, R de Haan, F Hageman… - Radiotherapy and …, 2015 - Elsevier
Background and purpose The PARP inhibitor olaparib is currently tested in clinical phase 1
trials to define safe dose levels in combination with RT. However, certain clinically relevant …

Evaluation of the pharmacodynamics and pharmacokinetics of the PARP inhibitor olaparib: a phase I multicentre trial in patients scheduled for elective breast cancer …

N Bundred, J Gardovskis, J Jaskiewicz, J Eglitis… - Investigational new …, 2013 - Springer
Olaparib (AZD2281) is an oral poly (ADP-ribose) polymerase (PARP) inhibitor with
antitumour activity in cancer patients with BRCA1/2 germline mutations and in patients with …

Phase I study to determine the bioavailability and tolerability of a tablet formulation of the PARP inhibitor olaparib in patients with advanced solid tumors: Dose …

A Gupta, V Moreno, EJ Dean, Y Drew, S Nicum… - 2012 - ascopubs.org
3051 Background: We previously reported the comparative bioavailability of the olaparib
tablet (TAB) up to 200 mg BID, with the initial capsule formulation; gmean AUC0–T following …

PARP inhibitor drugs in the treatment of breast, ovarian, prostate and pancreatic cancers: an update of clinical trials

D Kamel, C Gray, JS Walia, V Kumar - Current drug targets, 2018 - ingentaconnect.com
Background: PARP inhibitors appear to offer a promising role in the accompaniment of many
of the cytotoxic agents used in the present day to combat cancer proliferation in BRCA ½ …

[HTML][HTML] PARP1 rs1805407 increases sensitivity to PARP1 inhibitors in cancer cells suggesting an improved therapeutic strategy

I Abecassis, AJ Sedgewick, M Romkes, S Buch… - Scientific reports, 2019 - nature.com
Personalized cancer therapy relies on identifying patient subsets that benefit from a
therapeutic intervention and suggest alternative regimens for those who don't. A new data …

An adaptive study to determine the optimal dose of the tablet formulation of the PARP inhibitor olaparib

J Mateo, V Moreno, A Gupta, SB Kaye, E Dean… - Targeted …, 2016 - Springer
Background Olaparib is poorly soluble, requiring advanced drug delivery technologies for
adequate bioavailability. Sixteen capsules/day are required for the approved 400 mg twice …

Abstract LB-273: A head-to-head comparison of the properties of five clinical PARP inhibitors identifies new insights that can explain both the observed clinical efficacy …

E Leo, J Johannes, G Illuzzi, A Zhang, P Hemsley… - Cancer Research, 2018 - AACR
Four poly (ADP-ribose) polymerase (PARP) inhibitors have now presented phase 3
monotherapy data showing compelling benefit of targeting tumours enriched with DNA …