Considerations for human ADME strategy and design paradigm shift (s)–an industry white paper

…, B van Groen, AA Romeo, KC Cassidy… - Clinical …, 2023 - Wiley Online Library
The human absorption, distribution, metabolism, and excretion (hADME) study is the
cornerstone of the clinical pharmacology package for small molecule drugs, providing …

Discovery of cathepsin S inhibitor LY3000328 for the treatment of abdominal aortic aneurysm

…, DS Coffey, BW Shaw, KC Cassidy… - ACS medicinal …, 2014 - ACS Publications
Cathepsin S (Cat S) plays an important role in many pathological conditions, including
abdominal aortic aneurysm (AAA). Inhibition of Cat S may provide a new treatment for AAA. To …

Total synthesis of streptonigrone

DL Boger, KC Cassidy, S Nakahara - Journal of the American …, 1993 - ACS Publications
The first total synthesis of streptonigrone (1) is detailed and is based on the implementation
of a room-temperature, inverse electron demand Diels-Alder reaction of the A-sulfonyl-1-aza-…

Disposition and metabolism of LY2452473, a selective androgen receptor modulator, in humans

P Yi, JF Rehmel, K Cassidy, C Hadden… - Drug Metabolism and …, 2012 - ASPET
The disposition and metabolism of isopropyl N-[(2S)-7-cyano-4-(2-pyridylmethyl)-2,3-dihydro-1H-cyclopenta[b]indol-2-yl]carbamate
(LY2452473; a selective androgen receptor …

Identification and mitigation of reactive metabolites of 2-aminoimidazole-containing microsomal prostaglandin E synthase-1 inhibitors terminated due to clinical drug …

…, NE Hughes, BA Czeskis, KC Cassidy… - Journal of medicinal …, 2018 - ACS Publications
Two 2-aminoimidazole-based inhibitors, LY3031207 (1) and LY3023703 (2), of the microsomal
prostaglandin E synthase-1 (mPGES-1) enzyme were found to cause drug-induced liver …

Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by …

…, S Anderson, NA Furr, RJ Barbuch, KC Cassidy - Drug Metabolism and …, 2013 - ASPET
LY2090314 (3-[9-fluoro-2-(piperidin-1-ylcarbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-4-imidazo[1,2-a]pyridin-3-yl-1H-pyrrole-2,5-dione)
is an intravenous glycogen …

Non‐Labeled, Stable Labeled, or Radiolabelled Approaches for Provision of Intravenous Pharmacokinetics in Humans: A Discussion Piece

…, I Bjornsdottir, AA Romeo, KC Cassidy… - Clinical …, 2023 - Wiley Online Library
A review of the use of microdoses and isotopic microtracers for clinical intravenous
pharmacokinetic (iv PK) data provision is presented. The extent of application of the varied …

Diastereoselective alkylation guided by electrophile-nucleophile. pi.-interactions

…, RK Leavitt, P Mishra, KC Cassidy… - The Journal of …, 1988 - ACS Publications
Alkylation of the enolate la obtained from the (fi)-camphor imine of fert-butyl glycinate with a
variety of alkylating agents gives products whose trendsin diastereomeric excesses appear …

Difference in the pharmacokinetics and hepatic metabolism of antidiabetic drugs in zucker diabetic fatty and sprague-dawley rats

…, NA Calvert, RD Moulton, KC Cassidy… - Drug Metabolism and …, 2016 - ASPET
The Zucker diabetic fatty (ZDF) rat, an inbred strain of obese Zucker fatty rat, develops early
onset of insulin resistance and displays hyperglycemia and hyperlipidemia. The phenotypic …

Abstract CT153: Pharmacokinetic drug interactions between abemaciclib and CYP3A inducers and inhibitors

…, J Royalty, WT Ng, P Yi, J Rehmel, K Cassidy… - Cancer Research, 2016 - AACR
Abemaciclib is a selective and potent small-molecule inhibitor of cyclin-dependent kinases
4 and 6 (CDK4 and CDK6) being investigated for treatment of refractory hormone-receptor …