Preclinical characterization of AZD5305, a next-generation, highly selective PARP1 inhibitor and trapper
G Illuzzi, AD Staniszewska, SJ Gill, A Pike… - Clinical cancer …, 2022 - AACR
Purpose: We hypothesized that inhibition and trapping of PARP1 alone would be sufficient
to achieve antitumor activity. In particular, we aimed to achieve selectivity over PARP2 …
to achieve antitumor activity. In particular, we aimed to achieve selectivity over PARP2 …
[HTML][HTML] Inhibition of PARP1-dependent end-joining contributes to Olaparib-mediated radiosensitization in tumor cells
A Kötter, K Cornils, K Borgmann, J Dahm-Daphi… - Molecular …, 2014 - Elsevier
Poly-ADP-ribose-polymerase inhibitors (PARPi) are considered to be optimal tools for
specifically enhancing radiosensitivity. This effect has been shown to be replication …
specifically enhancing radiosensitivity. This effect has been shown to be replication …
Opportunities for the repurposing of PARP inhibitors for the therapy of non‐oncological diseases
NA Berger, VC Besson, AH Boulares… - British journal of …, 2018 - Wiley Online Library
The recent clinical availability of the PARP inhibitor olaparib (Lynparza) opens the door for
potential therapeutic repurposing for non‐oncological indications. Considering (a) the …
potential therapeutic repurposing for non‐oncological indications. Considering (a) the …
Olaparib tablet formulation: effect of food on the pharmacokinetics after oral dosing in patients with advanced solid tumours
R Plummer, H Swaisland, K Leunen… - Cancer chemotherapy …, 2015 - Springer
Background The oral PARP inhibitor olaparib has shown efficacy in patients with BRCA-
mutated cancer. This Phase I, open-label, three-part study (Parts A–C) in patients with …
mutated cancer. This Phase I, open-label, three-part study (Parts A–C) in patients with …
Development and validation of a high-performance liquid chromatography–tandem mass spectrometry assay quantifying olaparib in human plasma
CM Nijenhuis, L Lucas, H Rosing… - … of Chromatography B, 2013 - Elsevier
Olaparib is an inhibitor of poly ADP ribose polymerase 1 (PARP-1). Phase I and II trials
showed promising results of olaparib against tumours in BRCA mutation carriers. Currently …
showed promising results of olaparib against tumours in BRCA mutation carriers. Currently …
Pre-clinical and clinical evaluation of PARP inhibitors as tumour-specific radiosensitisers
C Powell, C Mikropoulos, SB Kaye, CM Nutting… - Cancer treatment …, 2010 - Elsevier
Approximately two million fractions of radiotherapy are administered in the UK every year, as
part of adjuvant, radical or palliative cancer treatment. For many tumour types, radiotherapy …
part of adjuvant, radical or palliative cancer treatment. For many tumour types, radiotherapy …
PARP inhibitors combined with radiotherapy: are we ready?
C Sun, A Chu, R Song, S Liu, T Chai… - Frontiers in …, 2023 - frontiersin.org
PARP was an enzyme found in the nucleus of eukaryotic cells that played a crucial role in
repairing damaged DNA. Recently, PARP inhibitors have demonstrated great potential in …
repairing damaged DNA. Recently, PARP inhibitors have demonstrated great potential in …
Safety and efficacy results from two randomized expansions of a phase I study of a tablet formulation of the PARP inhibitor, olaparib, in ovarian and breast cancer …
LR Molife, J Mateo, T McGoldrick, M Krebs, Y Drew… - 2012 - ascopubs.org
3048 Background: We previously reported the comparative bioavailability of the capsule
(CAP) formulation of olaparib and the more convenient new tablet (TAB) formulation (Molife …
(CAP) formulation of olaparib and the more convenient new tablet (TAB) formulation (Molife …
Iodinated benzimidazole PARP radiotracer for evaluating PARP1/2 expression in vitro and in vivo
RC Anderson, M Makvandi, K Xu, BP Lieberman… - Nuclear medicine and …, 2016 - Elsevier
Background PARP inhibitors (PARPi) have the potential to impact cancer therapy in a
selective patient population; however, despite current patient selection methods clinical …
selective patient population; however, despite current patient selection methods clinical …
PARP-inhibitor potpourri: A comparative review of class safety, efficacy, and cost
ER Hennes, EN Dow-Hillgartner… - Journal of Oncology …, 2020 - journals.sagepub.com
Purpose To summarize similarities and differences in efficacy, safety, and cost of available
PARP-inhibitors and offers pearls to distinguish subtle nuances between each agent to help …
PARP-inhibitors and offers pearls to distinguish subtle nuances between each agent to help …