Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of pharmaceutical sciences"
DOI: 10.1016/j.xphs.2020.06.013
Abstract: Receptor Interacting Protein 2 (RIP2) kinase inhibitors have been reported for therapeutic opportunities in inflammatory bowel diseases such as Ulcerative Colitis and Crohn's disease. During lead optimization, team identified 4-aminoquinoline series and several compounds from… read more here.
Keywords: permeability high; high glycoprotein; efflux ratio; glycoprotein efflux ... See more keywords
In vitro metabolism of [14C]‐benalaxyl in hepatocytes of rats, dogs and humans
Sign Up to like & getrecommendations! Published in 2017 at "Regulatory Toxicology and Pharmacology"
DOI: 10.1016/j.yrtph.2016.12.006
Abstract: Abstract The in vitro comparative animal metabolism study is now a data requirement under EU Directive 1107/2009 for registration of plant protection products. This type of study helps determine the extent of metabolism of a… read more here.
Keywords: metabolism; benalaxyl; human hepatocytes; rat dog ... See more keywords
Testosterone-induced benign prostatic hyperplasia rat and dog as facile models to assess drugs targeting lower urinary tract symptoms
Sign Up to like & getrecommendations! Published in 2018 at "PLoS ONE"
DOI: 10.1371/journal.pone.0191469
Abstract: Benign prostatic hyperplasia (BPH) is an age-related disease, affecting a majority of elderly men worldwide. Medical management of BPH is an alternative to surgical treatment of this disease. Currently, α1-adrenergic receptor (α1-AR) antagonists are among… read more here.
Keywords: benign prostatic; testosterone induced; testosterone; bph ... See more keywords
In Vitro Pharmacokinetic Behavior of Antiviral 3-Amidinophenylalanine Derivatives in Rat, Dog and Monkey Hepatocytes
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DOI: 10.3390/biomedicines11030682
Abstract: Type II transmembrane serine proteases represent pharmacological targets for blocking entry and spread of influenza or coronaviruses. In this study, the depletion rates of the 3-amidinophenylalanine (3-APhA)-derived matriptase/TMPRSS2 inhibitors MI-463, MI-472, MI-485 or MI-1900 were… read more here.
Keywords: pharmacokinetic behavior; vitro pharmacokinetic; rat dog; dog monkey ... See more keywords