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.