R
Rachel E. Kosa
Researcher at Pfizer
Publications - 14
Citations - 553
Rachel E. Kosa is an academic researcher from Pfizer. The author has contributed to research in topics: Pharmacokinetics & In vivo. The author has an hindex of 12, co-authored 14 publications receiving 464 citations. Previous affiliations of Rachel E. Kosa include University of Manchester & RMIT University.
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Journal ArticleDOI
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Jeffrey A. Pfefferkorn,Angel Guzman-Perez,John Litchfield,Robert J. Aiello,Judith L. Treadway,John C. Pettersen,Martha L. Minich,Kevin J. Filipski,Christopher S. Jones,Meihua Tu,Gary Erik Aspnes,Hud Lawrence Risley,Jianwei Bian,Benjamin D. Stevens,Patricia Bourassa,Theresa D’Aquila,Levenia Baker,Nicole Barucci,Alan Robertson,Francis Bourbonais,David R. Derksen,Margit MacDougall,Over Cabrera,Jing Chen,Amanda L. Lapworth,James A. Landro,William J. Zavadoski,Karen Atkinson,Nahor Haddish-Berhane,Beijing Tan,Lili Yao,Rachel E. Kosa,Manthena V.S. Varma,Bo Feng,David B. Duignan,Ayman El-Kattan,Sharad B. Murdande,Shenping Liu,Mark Ammirati,John D. Knafels,Paul DaSilva-Jardine,Laurel Sweet,Spiros Liras,Timothy P. Rolph +43 more
TL;DR: 19 is identified as a potent glucokinase activator with a greater than 50-fold liver-to-pancreas ratio of tissue distribution in rodent and non-rodent species, leading to its selection as a clinical development candidate for treating type 2 diabetes.
Journal ArticleDOI
Relative Contributions of Cytochrome CYP3A4 Versus CYP3A5 for CYP3A-Cleared Drugs Assessed In Vitro Using a CYP3A4-Selective Inactivator (CYP3cide)
Elaine E. Tseng,Robert L. Walsky,Ricardo A. Luzietti,Jennifer J. Harris,Rachel E. Kosa,Theunis C. Goosen,Michael Zientek,R. Scott Obach +7 more
TL;DR: Comparison of the in vitro observations to clinical pharmacokinetic data showed only a weak relationship between estimated contribution by CYP3A5 and impact of CYP 3A5 genotype on oral clearance, in large part because of the scatter in clinical data and the low numbers of study subjects used in CYP2A5 pharmacogenetics studies.
Assessed in vitro using a cyp3a4 selective inactivator (cyp3cide)
Elaine E. Tseng,Robert L. Walsky,Ricardo A. Luzetti,Jennifer J. Harris,Rachel E. Kosa,Theunis C. Goosen,Michael Zientek,R. Scott Obach +7 more
Journal ArticleDOI
Hepatobiliary Clearance Prediction: Species Scaling From Monkey, Dog, and Rat, and In Vitro–In Vivo Extrapolation of Sandwich-Cultured Human Hepatocytes Using 17 Drugs
TL;DR: SCHH is a useful tool to predict human hepatobiliary clearance, whereas BDC monkey model may provide further confidence in the prospective predictions, although dog SSS also showed reasonable predictions, rat overpredicted hepatOBiliary clearance for 13 of 24 compounds.
Journal ArticleDOI
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate
Samit Kumar Bhattacharya,Kim M. Andrews,Beveridge Ramsay,Kimberly O. Cameron,Chiliu Chen,Matthew F. Dunn,Dilinie P. Fernando,Hua Gao,David Hepworth,V. Margaret Jackson,Vishal Khot,Jimmy Kong,Rachel E. Kosa,Kimberly Lapham,Paula M. Loria,Allyn T. Londregan,Kim F. McClure,Suvi T. M. Orr,Jigna D. Patel,Colin R. Rose,James Saenz,Ingrid A. Stock,Gregory Storer,Maria A. Vanvolkenburg,Derek Vrieze,Guoqiang Wang,Jun Xiao,Yingxin Zhang +27 more
TL;DR: The identification of potent, highly selective orally bioavailable ghrelin receptor inverse agonists from a spiro-azetidino-piperidine series has promising in vivo pharmacokinetics and increase glucose-stimulated insulin secretion in human whole and dispersed islets.