A phase 1 safety and bioimaging trial of antibody DS-8895a against EphA2 in patients with advanced or metastatic EphA2 positive cancers

…, IJG Burvenich, C Paine, MJ Macri, M Kotsuma… - Investigational new …, 2022 - Springer
Ephrin type-A 2 (EphA2) is a transmembrane receptor expressed in epithelial cancers. We
report on a phase I dose escalation and biodistribution study of DS-8895a, an anti-EphA2 …

Molecular simulation of receptor occupancy and tumor penetration of an antibody and smaller scaffolds: application to molecular imaging

…, J Hoppin, M Matsumura, M Kotsuma… - Molecular imaging and …, 2017 - Springer
Purpose Competitive radiolabeled antibody imaging can determine the unlabeled intact
antibody dose that fully blocks target binding but may be confounded by heterogeneous tumor …

[HTML][HTML] Molecular imaging of T cell co-regulator factor B7-H3 with 89Zr-DS-5573a

…, YW Goh, H Tochon-Danguy, FE Scott, M Kotsuma… - Theranostics, 2018 - ncbi.nlm.nih.gov
B7-H3 is a transmembrane protein widely expressed in a variety of cancers and has been
shown to play a role in anti-tumor immunity. This study aims to develop a molecular imaging …

Phase I imaging and pharmacodynamic trial of CS-1008 in patients with metastatic colorectal cancer

…, M Jansen, M Matsumura, M Kotsuma… - Journal of clinical …, 2015 - ascopubs.org
Purpose CS-1008 (tigatuzumab) is a humanized, monoclonal immunoglobulin G1 (IgG1)
agonistic antibody to human death receptor 5. The purpose of this study was to investigate the …

Molecular imaging and quantitation of EphA2 expression in xenograft models with 89Zr-DS-8895a

…, H Tochon-Danguy, M Kotsuma… - Journal of Nuclear …, 2016 - Soc Nuclear Med
Subtype A2 of the erythropoietin-producing hepatocellular tyrosine kinase (EphA2) cell surface
receptor is expressed in a range of epithelial cancers. This study evaluated the molecular …

Physiologically based pharmacokinetic modeling to predict the clinical effect of azole antifungal agents as CYP3A inhibitors on azelnidipine pharmacokinetics

A Watanabe, M Kotsuma - Drug Metabolism and Pharmacokinetics, 2024 - Elsevier
In this study, a physiologically based pharmacokinetic (PBPK) model of the cytochrome P450
3A (CYP3A) substrate azelnidipine was developed using in vitro and clinical data to predict …

[HTML][HTML] Predictive modeling of drug response in non-hodgkin's lymphoma

HB Frieboes, BR Smith, Z Wang, M Kotsuma, K Ito… - PloS one, 2015 - journals.plos.org
We combine mathematical modeling with experiments in living mice to quantify the relative
roles of intrinsic cellular vs. tissue-scale physiological contributors to chemotherapy drug …

Regression of inflammation in atherosclerosis by the LXR agonist R211945: a noninvasive assessment and comparison with atorvastatin

…, T Tanimoto, K Brown, M Kotsuma… - JACC: Cardiovascular …, 2012 - jacc.org
Objectives : The aim of this study was to noninvasively detect the anti-inflammatory properties
of the novel liver X receptor agonist R211945. Background : R211945 induces reversal …

Current practices, gap analysis, and proposed workflows for PBPK modeling of cytochrome P450 induction: an industry perspective

…, L De Zwart, M Dowty, M Kotsuma… - Clinical …, 2022 - Wiley Online Library
The International Consortium for Innovation and Quality (IQ) Physiologically Based
Pharmacokinetic (PBPK) Modeling Induction Working Group (IWG) conducted a survey across …

Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and …

…, M Takei, E Suzuki, H Takakusa, M Kotsuma… - Xenobiotica, 2017 - Taylor & Francis
Esaxerenone (CS-3150) is a novel non-steroidal mineralocorticoid receptor antagonist. The
pharmacokinetics, tissue distribution, excretion, and metabolism of esaxerenone were …