L
Loren Berry
Researcher at Amgen
Publications - 27
Citations - 1236
Loren Berry is an academic researcher from Amgen. The author has contributed to research in topics: In vivo & Pharmacokinetics. The author has an hindex of 17, co-authored 27 publications receiving 1123 citations.
Papers
More filters
Journal ArticleDOI
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
Brian K. Albrecht,Jean-Christophe Harmange,David Bauer,Loren Berry,Christiane Bode,Alessandro Boezio,April Chen,Deborah Choquette,Isabelle Dussault,Cary Fridrich,Satoko Hirai,Doug Hoffman,Jay Larrow,Paula Kaplan-Lefko,Jasmine Lin,Julia Lohman,Alexander M. Long,Jodi Moriguchi,Anne B. O’Connor,Michele Potashman,Monica Reese,Karen Rex,Aaron C. Siegmund,Kavita Shah,Roman Shimanovich,Stephanie Springer,Yohannes Teffera,Yajing Yang,Yihong Zhang,Steven F. Bellon +29 more
TL;DR: The discovery of potent and selective triazolopyridazine small molecules that inhibit c-Met activity is reported, which has been observed in multiple tumor types.
Journal ArticleDOI
Esterase Activities in the Blood, Liver and Intestine of Several Preclinical Species and Humans
TL;DR: Substantial species differences in activity of these esterases were observed between the mouse, rat, dog monkey and human, and such species differences must be considered when using these preclinical species to optimize the pharmacokinetic properties of ester compounds intended for human use.
Journal ArticleDOI
Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)
Longbin Liu,Aaron C. Siegmund,Ning Xi,Paula Kaplan-Lefko,Karen Rex,April Chen,Jasmine Lin,Jodi Moriguchi,Loren Berry,Liyue Huang,Yohannes Teffera,Yajing Yang,Yihong Zhang,Steven F. Bellon,Matthew R. Lee,Roman Shimanovich,Annette Bak,Celia Dominguez,Mark H. Norman,Jean-Christophe Harmange,Isabelle Dussault,Tae-Seong Kim +21 more
TL;DR: When dosed orally, 17 significantly inhibited tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight.
Journal ArticleDOI
An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes.
Loren Berry,Zhiyang Zhao +1 more
TL;DR: The relationship between time-dependent inactivation (TDI) and IC50 is examined using a consolidated method for evaluating CYP450 inhibition during drug discovery and the "shifted IC50" could be used to estimate, the K(I) and TDI potency ratio k(inact)/K( I) to within 2-fold in most cases.
Journal ArticleDOI
Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
Thomas A. Munro,Loren Berry,Ashlee Van't Veer,Cécile Béguin,F. Ivy Carroll,Zhiyang Zhao,William A. Carlezon,Bruce M. Cohen +7 more
TL;DR: The very slow elimination of JDTic from brain is surprising given that it undergoes active efflux, has modest affinity for homogenate, and has a shorter duration of action than nor-BNI under these conditions, and it is proposed that this persistence may result from entrapment in cellular compartments such as lysosomes.