NAEJA Pharmaceutical Research And Development
Drug Discovery Solutions
Early Drug Development Solutions
Lead Optimization (Early-ADME)
Drug Candidate Selection
Chemical Process Development
Pharmaceutical Profiling (DM & PK)
Bioanalytical & Pharmacokinetics
Selectivity Testing
Cellular Toxicity
Efficacy Testing (Cellular and Animal)
       
Early Drug Development Solutions

Lead Optimization-Early ADME

NAEJA Pharmaceutical Inc. offers a range of assays for evaluation of the pharmaceutical properties of drug discovery compounds in the lead optimization process. 

  • Solution properties & preformulation (activities focus on physico-chemical characterization):
    • Solubility screening studies ( intrinsic, pH, solvent and solubility enhancement trials)
    • Partition coefficient (log D), solution stability studies (buffer/plasma)
    • Protein binding

  • In vitro absorption 
    • Caco-2 permeability Screen 
    • P-glycoprotein inhibition ( Taxol substrate )

  • In vitro metabolism
    • Primary metabolic stability: Screening is done using liver S9 fraction, microsomes and cDNA expressed isozymes from different animal species
      (mouse, rat, rabbit, guinea pig, dog, monkey) and humans.
    • Secondary evaluation:  
      •  CYP 450 pathway identification for metabolites and greater understanding of the principal enzyme (CYP450) involved in drug metabolism.
      •  Preliminary enzyme kinetic experiments in vitro to determine km and Vmax 
    • Tertiary evaluation:  
      •  Inhibition of CYP 450 isozymes. Primary drug-drug interaction & its implication in drug development. 
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