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P-Glycoprotein (ABCB1/MDR1) Controls Brain Penetration and Intestinal Disposition of the PARP1/2 Inhibitor Niraparib.
F Martins ML, Loos NHC, Mucuk S, de Jong D, Lebre MC, Rosing H, Tibben M, Beijnen JH, Schinkel AH. F Martins ML, et al. Mol Pharm. 2021 Dec 6;18(12):4371-4384. doi: 10.1021/acs.molpharmaceut.1c00553. Epub 2021 Nov 3. Mol Pharm. 2021. PMID: 34730366
In vitro, human ABCB1 and mouse Abcg2 transported niraparib moderately. Compared to wild-type mice, niraparib brain-to-plasma ratios were 6- to 7-fold increased in Abcb1a/1b(-/-) and Abcb1a/1b;Abcg2(-/-) but not in single Abcg2(-/-) mice, while niraparib plas …
In vitro, human ABCB1 and mouse Abcg2 transported niraparib moderately. Compared to wild-type mice, niraparib brain-to-plasma …
Quantification of cobimetinib, cabozantinib, dabrafenib, niraparib, olaparib, vemurafenib, regorafenib and its metabolite regorafenib M2 in human plasma by UPLC-MS/MS.
Krens SD, van der Meulen E, Jansman FGA, Burger DM, van Erp NP. Krens SD, et al. Biomed Chromatogr. 2020 Mar;34(3):e4758. doi: 10.1002/bmc.4758. Epub 2020 Jan 13. Biomed Chromatogr. 2020. PMID: 31758580 Free PMC article.
A sensitive and selective ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous determination of seven oral oncolytics (two PARP inhibitors, i.e. olaparib and niraparib, and five tyrosine kinase inhibitors, i.e. cobi …
A sensitive and selective ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous det …
Human mass balance study and metabolite profiling of (14)C-niraparib, a novel poly(ADP-Ribose) polymerase (PARP)-1 and PARP-2 inhibitor, in patients with advanced cancer.
van Andel L, Zhang Z, Lu S, Kansra V, Agarwal S, Hughes L, Tibben MM, Gebretensae A, Lucas L, Hillebrand MJX, Rosing H, Schellens JHM, Beijnen JH. van Andel L, et al. Invest New Drugs. 2017 Dec;35(6):751-765. doi: 10.1007/s10637-017-0451-2. Epub 2017 Mar 16. Invest New Drugs. 2017. PMID: 28303528 Free PMC article.
Oral absorption of (14)C-niraparib was rapid, with niraparib concentrations peaking at 2.49 h, and reaching a mean maximum concentration of 540 ng/mL. Two major metabolites were found: the known metabolite M1 (amide hydrolysed niraparib) and the …
Oral absorption of (14)C-niraparib was rapid, with niraparib concentrations peaking at 2.49 h, and reaching a mean maximum con …
Liquid chromatography-tandem mass spectrometry assay for the quantification of niraparib and its metabolite M1 in human plasma and urine.
van Andel L, Zhang Z, Lu S, Kansra V, Agarwal S, Hughes L, Tibben MM, Gebretensae A, Rosing H, Schellens JHM, Beijnen JH. van Andel L, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Jan 1;1040:14-21. doi: 10.1016/j.jchromb.2016.11.020. Epub 2016 Nov 19. J Chromatogr B Analyt Technol Biomed Life Sci. 2017. PMID: 27898364
Niraparib (MK-4827) is a novel poly(ADP-Ribose) polymerase (PARP) inhibitor currently investigated in phase III clinical trials to treat cancers. ...This article describes the development and validation of a bioanalytical assay for niraparib and its carboxylic acid …
Niraparib (MK-4827) is a novel poly(ADP-Ribose) polymerase (PARP) inhibitor currently investigated in phase III clinical trials to tr …
Treatment with the PARP inhibitor, niraparib, sensitizes colorectal cancer cell lines to irinotecan regardless of MSI/MSS status.
Genther Williams SM, Kuznicki AM, Andrade P, Dolinski BM, Elbi C, O'Hagan RC, Toniatti C. Genther Williams SM, et al. Cancer Cell Int. 2015 Feb 4;15(1):14. doi: 10.1186/s12935-015-0162-8. eCollection 2015. Cancer Cell Int. 2015. PMID: 25685067 Free PMC article.
We compiled a large panel of MSI and MSS CRC cell lines and evaluated the anti-proliferative activity of niraparib. In addition to testing single agent cytotoxic activity of niraparib, we also tested irinotecan (or SN-38, the active metabolite of irinotecan) …
We compiled a large panel of MSI and MSS CRC cell lines and evaluated the anti-proliferative activity of niraparib. In addition to te …