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Integrated DMPK services for lead optimization and IND filing

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Integrated DMPK Services from HIT to Lead Optimization and IND/IMPD Filing
Aragen’s uniqueness comes from its ability to provide comprehensive DMPK expertise and technologies from the early drug discovery (High-throughput profiling/rank order) to lead optimization and IND/IMPD filing for all modalities of small and large molecules in rodents and non-rodents. We work for customer delight, using biomatrices from certified vendors and animals from CRL subsidiaries. Our two mirror image facilities at Hyderabad and Bangalore have 2.5 dozen of high-end LC-MS/MS and HRMS, to eradicate bottlenecks in bioanalyses and produce quality data in best timelines.
TIER 1 ASSAYS
  • Solubility (Kinetic and Thermodynamic,
    SIF, SGF)
  • Log P and Log D
  • PAMPA (GIT, BBB and Skin)
  • Metabolic stability in microsomes and
    hepatocytes (2 time points, Multispecies)
  • Protein binding (Single concentration)
  • Cocktail CYP inhibition, HLM (Single
    concentration, 5 CYPs)
  • Cassette IV PK
  • Cassette PO PK
TIER 2 ASSAYS
  • Plasma protein binding (3 concentrations, 3-5 species)
  • Metabolic stability (Intrinsic Clearance)
  • Plasma/blood stability
  • CYP Inhibition (IC50, Ki)
  • Met ID (soft spot), species comparison
  • Blood / plasma Partitioning
  • Time dependent inhibition / Mechanism
    based inactivation
  • Reactive metabolites
  • MDCK and Caco-2 permeability
  • Rat IV PO PK
  • Mouse IV PO PK
  • Dog IV PO PK
  • Blood brain barrier penetration studies
    (Brain and CSF) in rodents
TIER 3 ASSAY
  • Reaction Phenotyping
  • Single raising dose in rat
  • Single raising dose in mouse
  • Single raising dose in dog
  • CYP Induction
  • Tissue distribution studies
  • MTD studies in rat and mouse
  • Mechanistic PK studies (Biliary excretion, First pass metabolism, BAL study)
  • Metabolic Characterization and Identification of In vivo samples
IND/IMPD PACKAGE
  • Bioanalytical method validation in rodent and non-rodents
  • Single and multiple dose pharmacokinetics
  • Dose proportionality and absolute
    bioavailability in mouse, rat, and dog
  • Plasma protein binding in mouse, rat, dog, and human plasma
  • In vitro CYP450 inhibition (1A2, 2B6, 2C8, 2C9,
    2C19, 2D6, 3A4/5) in human liver microsomes
  • CYP induction in human hepatocytes
  • In vitro metabolism in, mouse, dog, and human hepatic preparations
  • Reaction phenotyping in recombinant CYPs or UGTs or other enzyme systems
  • Mini Ames
  • Contribution of P-glycoprotein (P-gp) and breast cancer resistant protein (BCRP) in limiting drug absorption or flux