Detalles de la búsqueda
1.
Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human.
Xenobiotica
; 54(2): 64-74, 2024 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-38197324
2.
Absorption, Metabolism, and Excretion of Taselisib (GDC-0032), a Potent ß-Sparing PI3K Inhibitor in Rats, Dogs, and Humans.
Drug Metab Dispos
; 51(4): 436-450, 2023 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-36623882
3.
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Bioorg Med Chem Lett
; 59: 128576, 2022 03 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-35065235
4.
Absorption, metabolism and excretion of pictilisib, a potent pan-class I phosphatidylinositol-3-Kinase (PI3K) inhibitor, in rats, dogs, and humans.
Xenobiotica
; 51(7): 796-810, 2021 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-33938357
5.
Investigating the Impact of Albumin on the Liver Uptake of Pitavastatin and Warfarin in Nagase Analbuminemic Rats.
Drug Metab Dispos
; 47(11): 1307-1313, 2019 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-31492695
6.
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Bioorg Med Chem Lett
; 29(16): 2294-2301, 2019 08 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-31307887
7.
Individual serum bile acid profiling in rats aids in human risk assessment of drug-induced liver injury due to BSEP inhibition.
Toxicol Appl Pharmacol
; 338: 204-213, 2018 01 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29146462
8.
Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.
Nat Chem Biol
; 12(10): 779-86, 2016 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-27479743
9.
Generation and Characterization of a Breast Cancer Resistance Protein Humanized Mouse Model.
Mol Pharmacol
; 89(5): 492-504, 2016 May.
Artículo
en Inglés
| MEDLINE | ID: mdl-26893303
10.
Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma.
Drug Metab Dispos
; 44(12): 1881-1889, 2016 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-27638506
11.
Nonselective inhibition of the epigenetic transcriptional regulator BET induces marked lymphoid and hematopoietic toxicity in mice.
Toxicol Appl Pharmacol
; 300: 47-54, 2016 06 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27078884
12.
Determination of GDC-0980 (apitolisib), a small molecule dual phosphatidylinositide 3-kinase/mammalian target of rapamycin inhibitor in dog plasma by LC-MS/MS to support a GLP toxicology study.
Biomed Chromatogr
; 29(8): 1274-9, 2015 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-25677784
13.
Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging.
Drug Metab Dispos
; 42(7): 1110-6, 2014 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-24754926
14.
Evaluation of organic anion transporting polypeptide 1B1 and 1B3 humanized mice as a translational model to study the pharmacokinetics of statins.
Drug Metab Dispos
; 42(8): 1301-13, 2014 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-24855184
15.
Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Bioorg Med Chem Lett
; 24(19): 4714-4723, 2014 Oct 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25193232
16.
Early Stage Preclinical Formulation Strategies to Alter the Pharmacokinetic Profile of Two Small Molecule Therapeutics.
Pharmaceuticals (Basel)
; 17(2)2024 Jan 30.
Artículo
en Inglés
| MEDLINE | ID: mdl-38399394
17.
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation.
J Med Chem
; 67(6): 4819-4832, 2024 Mar 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-38470227
18.
Pharmacokinetics and absorption of the anticancer agents dasatinib and GDC-0941 under various gastric conditions in dogs--reversing the effect of elevated gastric pH with betaine HCl.
Mol Pharm
; 10(11): 4024-31, 2013 Nov 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-23980865
19.
Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.
Bioorg Med Chem Lett
; 23(17): 4953-9, 2013 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23867164
20.
Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.
Bioorg Med Chem Lett
; 23(3): 897-901, 2013 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23265894