Document Detail


Pharmacodynamics, Pharmacokinetics, and Safety of AM211: A Novel and Potent Antagonist of the Prostaglandin D2 Receptor Type 2.
MedLine Citation:
PMID:  22110163     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The prostaglandin D(2) receptor type 2 (DP2) and its ligand, PGD(2), have been implicated in the development of asthma and other inflammatory diseases. The authors evaluated the pharmacodynamics, pharmacokinetics and safety of [2'-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4'-trifluoromethyl-biphenyl-3-yl]-acetic acid sodium salt (AM211), a novel and potent DP2 antagonist, in healthy participants. Single and multiple doses of AM211 demonstrated dose-dependent inhibition of eosinophil shape change in blood with near-complete inhibition observed at trough after dosing 200 mg once daily for 7 days. Maximum plasma concentrations and exposures of AM211 increased in a greater-than-dose-proportional manner after single and multiple dosing. After multiple dosing, the exposures on day 7 were higher than on day 1 with accumulation ratio values ranging from 1.4 to 1.5. Mean terminal half-life values ranged from 14 to 25 hours across the dose range of 100 to 600 mg. AM211 was well tolerated at all doses in both the single- and multiple-dose cohorts. These data support additional clinical studies to evaluate AM211 in asthma and other inflammatory diseases.
Authors:
G Bain; C D King; J Brittain; J P Hartung; I Dearmond; B Stearns; Y P Truong; J H Hutchinson; J F Evans; K Holme
Related Documents :
2709333 - Parallel first-order and michaelis-menten elimination kinetics of ethanol. respective r...
7420073 - Antidepressant drugs and ethanol: behavioral and pharmacokinetic interactions in mice.
24735473 - Bioavailability and pharmacokinetic profile of levofloxacin following intravenous, intr...
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-11-22
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  -     ISSN:  1552-4604     ISO Abbreviation:  -     Publication Date:  2011 Nov 
Date Detail:
Created Date:  2011-11-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Amira Pharmaceuticals.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  Population pharmacokinetics of unbound mycophenolic acid in pediatric and young adult patients under...
Next Document:  Circadian Intraocular Pressure and Blood Pressure Reduction With Timolol 0.5% Solution and Timogel 0...