AMG 416 is a novel D-amino acid–containing peptide agonist of the calcium-sensing receptor (CaSR) that is being evaluated for the treatment of secondary hyperparathyroidism in chronic kidney disease patients receiving hemodialysis. The principal amino acid residues and their location in the CaSR that accommodate AMG 416 binding and mode of action have not previously been reported. Herein we est...

Published and unpublished observations on geographical distribution of Biomphalaria snails in the State of Minas Gerais, Brazil, were compiled. This work is aimed at knowing the present occurrence of Biomphalaria species in this region, and at contributing to the elaboration of the planorbid chart of Minas Gerais. In malacological surveys, performed by several researchers, the presence of seven...

In your June editorial, “Is Blockade of Pancreatic Lipase the Answer?” (1), you suggest that the success of the 2-y clinical trials of orlistat is diminished by the propensity of obese patients to regain weight. I disagree. The North American Association for the Study of Obesity (NAASO) considers a weight loss of ≥ 5% to be clinically significant (2). In each of the published clinical trials of...

Executive Summary ................................................ 850 Summary of Findings ............................................... 850 Recommendations ............................................... 850 Introduction ............................................... 850 Cardiovascular Disease Prevalence and Cost ................................................ 851 Prevalence .................

curve; C max , peak drug concentration observed in plasma This article has not been copyedited and formatted. The final version may differ from this version. Abstract AMG 853 is an orally bioavailable and potent dual antagonist of the D-prostanoid (DP) and chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2) receptors. The drug interaction potential of AMG 853, both as a ...

2-(4-(4-(tert-Butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid (AMG 853) is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. The drug interaction potential of AMG 853, both as a victim and a perpetrator, was investigated using in v...

JTK-853 is a novel piperazine derivative nonnucleoside inhibitor of hepatitis C virus (HCV) RNA-dependent RNA polymerase. JTK-853 showed potent inhibitory activity against genotype 1 HCV polymerase, with a 50% inhibitory concentration in the nanomolar range, and showed potent antiviral activity against the genotype 1b replicon, with a 50% effective concentration of 0.035 μM. The presence of hum...

JTK-853 is a novel, non-nucleoside, palm site-binding hepatitis C virus (HCV) polymerase inhibitor that has demonstrated antiviral activity in HCV-infected patients during 3 days of treatment. To estimate the genetic barrier of JTK-853 to resistance in vitro, colony formation assays were conducted using HCV replicon cells (genotypes 1a and 1b). The colony formation assays revealed that the numb...

Inhibitors of mammalian multidrug efflux, such as the plant alkaloid reserpine, are also active in potentiating antibiotic activity by inhibiting bacterial efflux. Based on this precedent, two novel mammalian multiple drug resistance inhibitors, biricodar (VX-710) and timcodar (VX-853), were evaluated for activity in a variety of bacteria. Both VX-710 and VX-853 potentiated the activity of ethi...