Generating Robust and Informative Nonclinical In Vitro and In Vivo Bacterial Infection Model Efficacy Data To Support Translation to Humans

JB Bulitta, WW Hope, AE Eakin, T Guina… - Antimicrobial agents …, 2019 - Am Soc Microbiol
ABSTRACT In June 2017, the National Institute of Allergy and Infectious Diseases, part of
the National Institutes of Health, organized a workshop entitled “Pharmacokinetics …

SARS‐CoV‐2–host proteome interactions for antiviral drug discovery

X Liu, S Huuskonen, T Laitinen, T Redchuk… - Molecular Systems …, 2021 - embopress.org
Abstract Treatment options for COVID‐19, caused by SARS‐CoV‐2, remain limited.
Understanding viral pathogenesis at the molecular level is critical to develop effective …

[PDF][PDF] Discovery of novel blood-brain barrier targets to enhance brain uptake of therapeutic antibodies

YJY Zuchero, X Chen, N Bien-Ly, D Bumbaca… - Neuron, 2016 - cell.com
The blood-brain barrier (BBB) poses a major challenge for developing effective antibody
therapies for neurological diseases. Using transcriptomic and proteomic profiling, we …

The application of cassette dosing for pharmacokinetic screening in small-molecule cancer drug discovery

NF Smith, FI Raynaud, P Workman - Molecular Cancer Therapeutics, 2007 - AACR
Pharmacokinetic evaluation is an essential component of drug discovery and should be
conducted early in the process so that those compounds with the best chance of success are …

Non-compartmental analysis

J Gabrielsson, D Weiner - Computational Toxicology: Volume I, 2012 - Springer
When analyzing pharmacokinetic data, one generally employs either model fitting using
nonlinear regression analysis or non-compartmental analysis techniques (NCA). The …

Physiologically-based pharmacokinetic (PBPK) model to predict IgG tissue kinetics in wild-type and FcRn-knockout mice

A Garg, JP Balthasar - Journal of pharmacokinetics and …, 2007 - Springer
Although it is known that FcRn, the neonatal Fc-receptor, functions to protect immune
gamma globulin (IgG) from elimination, the influence of FcRn on the tissue distribution of IgG …

Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in …

JJ Gills, J LoPiccolo, J Tsurutani, RH Shoemaker… - Clinical cancer …, 2007 - AACR
Purpose: The development of new cancer drugs is slow and costly. HIV protease inhibitors
are Food and Drug Administration approved for HIV patients. Because these drugs cause …

Mechanisms limiting distribution of the threonine-protein kinase B-RaFV600E inhibitor dabrafenib to the brain: implications for the treatment of melanoma brain …

RK Mittapalli, S Vaidhyanathan, AZ Dudek… - … of Pharmacology and …, 2013 - ASPET
Brain metastases are a common cause of death in stage IV metastatic melanoma.
Dabrafenib is a BRAF (gene encoding serine/threonine-protein kinase B-Raf) inhibitor that …

Identification of OATP1B3 as a high-affinity hepatocellular transporter of paclitaxel

NF Smith, MR Acharya, N Desai, W Figg, II… - Cancer biology & …, 2005 - Taylor & Francis
Interindividual variability in paclitaxel and docetaxel pharmacokinetics, toxicity and response
is extensive, and largely unexplained. We hypothesized that this is due to affinity of taxanes …

The role of the breast cancer resistance protein (ABCG2) in the distribution of sorafenib to the brain

S Agarwal, R Sane, JR Ohlfest, WF Elmquist - Journal of Pharmacology and …, 2011 - ASPET
ATP-binding cassette transporters P-glycoprotein (P-gp) and breast cancer resistance
protein (BCRP) have been shown to work in concert to restrict brain penetration of several …