Prediction of Nonlinear Intestinal Absorption of CYP3A4 and P-Glycoprotein Substrates from their In Vitro Km Values

T Tachibana, M Kato, Y Sugiyama - Pharmaceutical research, 2012 - Springer
ABSTRACT Purpose CYP3A4 and P-glycoprotein (P-gp) are present in the human intestine
and mediate intestinal first-pass metabolism and the efflux of oral drugs, respectively. We …

Drug–drug interactions related to altered absorption and plasma protein binding: Theoretical and regulatory considerations, and an industry perspective

J Hochman, C Tang, T Prueksaritanont - Journal of pharmaceutical …, 2015 - Elsevier
Drug–drug interactions (DDIs) related to altered drug absorption and plasma protein binding
have received much less attention from regulatory agencies relative to DDIs mediated via …

Vinorelbine delivery and efficacy in the MDA-MB-231BR preclinical model of brain metastases of breast cancer

R Samala, HR Thorsheim, S Goda, K Taskar… - Pharmaceutical …, 2016 - Springer
Purpose To evaluate vinorelbine drug exposure and activity in brain metastases of the
human MDA-MB-231BR breast cancer model using integrated imaging and analysis …

[HTML][HTML] Rifampicin induces gene, protein, and activity of P-glycoprotein (ABCB1) in human precision-cut intestinal slices

O Martinec, C Biel, IAM De Graaf, M Huliciak… - Frontiers in …, 2021 - frontiersin.org
P-glycoprotein (ABCB1), an ATP-binding cassette efflux transporter, limits intestinal
absorption of its substrates and is a common site of drug–drug interactions. Drug-mediated …

QSAR Model of Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain: Incorporating P-glycoprotein Efflux as a Variable

E Dolgikh, IA Watson, PV Desai… - Journal of Chemical …, 2016 - ACS Publications
We report development and prospective validation of a QSAR model of the unbound brain-to-
plasma partition coefficient, K p, uu, brain, based on the in-house data set of∼ 1000 …

Development and validation of RP-HPLC-UV method for simultaneous determination of buparvaquone, atenolol, propranolol, quinidine and verapamil: a tool for the …

G Venkatesh, S Ramanathan, SM Mansor… - … of pharmaceutical and …, 2007 - Elsevier
A simple, sensitive and specific reversed phase high performance liquid chromatographic
(RP-HPLC) method with UV detection at 251nm was developed for simultaneous …

[HTML][HTML] PHLPP inhibitor NSC74429 is neuroprotective in rodent models of cardiac arrest and traumatic brain injury

TC Jackson, C Dezfulian, VA Vagni, J Stezoski… - Biomolecules, 2022 - mdpi.com
Pleckstrin homology domain and leucine rich repeat protein phosphatase (PHLPP) knockout
mice have improved outcomes after a stroke, traumatic brain injury (TBI), and decreased …

Preclinical development for suspensions

S Garad, J Wang, Y Joshi, R Panicucci - … Suspensions: From Formulation …, 2009 - Springer
This chapter summarizes the significance of suspension in preclinical development. Majority
of the preclinical studies are carried out using suspension. Therefore, it is important to know …

[HTML][HTML] In silico prediction of intestinal permeability by hierarchical support vector regression

MH Lee, GH Ta, CF Weng, MK Leong - International Journal of Molecular …, 2020 - mdpi.com
The vast majority of marketed drugs are orally administrated. As such, drug absorption is
one of the important drug metabolism and pharmacokinetics parameters that should be …

Pharmacokinetics in cancer chemotherapy

S Garattini - European Journal of Cancer, 2007 - Elsevier
Pharmacokinetics is the study of how the body causes changes in drugs, and includes
analysis of absorption, distribution, metabolism and excretion. It is essential to understand …