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Essential ADME Assays
This assay is used to determine the quasi-equilibrium solubility of a test compound at a specified temperature and pH in a specified matrix using the shake-flask method.
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This assay is used to determine the LogD of a test compound at a specified pH using the shake-flask method.
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In this assay a Sirius GLpKa system is used to determine the pKa, LogP, and LogD values of a test compound.
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This assay is used to determine the solubility of a test compound at room temperature in phosphate buffer at pH 7.4.
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This assay is used to determine the LogD of a test compound at pH 7.4 using the shake-flask method.
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This assay is used to determine the chemical stability of a test compound in simulated or natural gastrointestinal fluids.
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This assay is used to determine the stability of test compound in blood plasma for various species, including humans.
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This assay is used to determine the stability of a test compound in whole blood or plasma from mouse, rat, rabbit, dog, monkey, or human.
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This assay is used to determine the chemical stability of a test compound in buffer.
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This assay is used to determine if a test compound is cytotoxic to mammalian cells.
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This assay is used to determine if a test compound is cytotoxic to animal or human hepatocytes.
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This assay is used to determine the hemolytic effect of a test compound.
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This assay is used to determine the permeability of a test compound through Caco-2 cell monolayers in the apical-to-basolateral direction.
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This assay is used to determine the permeability of a test compound through Caco-2 cell monolayers in the apical-to-basolateral and basolateral- to-apical direction.
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This assay is used to determine the blood-brain barrier (BBB) penetration potential of a test compound using MDR1-MDCK cell monolayers.
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This assay is used to determine the P-gp interaction with a test compound using MDR1-MDCK cell monolayers in both the presence and absence of a P-gp inhibitor.
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This assay is used to determine the unidirectional permeability of a test compound through intestinal tissue segments (duodenum, ileum, jejunum and colon).
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This assay is used to determine the bidirectional permeability of a test compound through intestinal tissue segments (duodenum, ileum, jejunum and colon).
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This assay is used to determine the unidirectional permeability of a test compound through freshly excised porcine buccal epithelium.
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This assay is used to determine the unidirectional permeability of a test compound through freshly excised porcine nasal epithelium.
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This assay is used to determine the unidirectional permeability of a test compound through excised skin from humans or pigs.
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This assay is used to determine the permeability of a test compound through Caco-2 cell monolayers in the apical-to-basolateral direction.
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This assay is used to determine the permeability of a test compound through Caco-2 cell monolayers in both the apical-to-basolateral and basolateral-to-apical direction.
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This assay is used to determine if a test compound is a human P-gp substrate by measuring its bidirectional permeability across MDR1-MDCK and MDCK cell monolayers in the presence and absence of P-gp inhibitors.
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This assay is used to determine if a test compound is a P-gp inhibitor by measuring its effect on the bidirectional permeability of the P-gp substrate, digoxin, through MDR1-MDCK or Caco-2 cell monolayers.
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This assay is used to screen for inhibition of P-gp by a test compound, by measuring its effect on the bidirectional permeability of a P-gp substrate through Caco-2 cell monolayers.
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This assay is used to identify active uptake of a test compound by PepT1, using the Caco-2 cell monolayer system.
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This assay is used to assess the potential of a test compound to induce P-glycoprotein (P-gp) in a human intestinal cell line.
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This assay is used to determine the unidirectional permeability (anterior-to-posterior) of a test compound through rabbit corneal or conjunctival tissue.
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This assay is used to determine the unidirectional permeability (anterior-to-posterior) of a test compound through rabbit corneal or conjunctival tissue.
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This assay is used to determine the IC50 of a test compound for inhibition of OATP1B1 in OATP1B1-transfected HEK293 cells.
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This assay is used to evaluate the potential of a test compound to inhibit OATP1B1 in OATP1B1-transfected HEK293 cells at a single concentration.
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This assay is used to determine the IC50 of a test compound for inhibition of OATP1B3 in OATP1B3-transfected HEK293 cells.
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This assay is used to evaluate the potential of a test compound to inhibit OATP1B3 in OATP1B3-transfected HEK293 cells at a single concentration.
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This assay is used to determine the P-gp interaction with a test compound using CellPort™ CPT-B1 BCRP-knockdown cell monolayers in both the presence and the absence of a P-gp inhibitor.
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This assay is used to determine the BCRP interaction with a test compound using CellPort™ CPT-B1 BCRP-knockdown cell monolayers and wild-type Caco-2 cell monolayers.
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This assay is used to determine the P-gp interaction with a test compound using CellPort CPT-P1 Pgp-knockdown cell monolayers and Caco-2 cell monolayers.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled human liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled rat liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with liver microsomes in the presence and absence of NADPH.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with S9 fraction in the presence and absence of cofactors.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with either cryopreserved or fresh hepatocytes.
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This assay uses fluorogenic substrates to determine the potency with which a test compound inhibits recombinant human cytochrome P450 (CYP) enzymes.
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This assay is used to screen for inhibition of cytochrome P450 (CYP) enzymes by a test compound.
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Cytochrome P450 reaction phenotyping using CYP-specific Supersomes™
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This assay is used to assess the potential of a test compound to induce CYP1A2, CYP2B6, and CYP3A4 in fresh or cryopreserved human hepatocytes.
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This assay is used to determine the inhibition constant (Ki ) of a test compound and the mechanism of inhibition of CYPs in human liver microsomes (HLM). The IC50 of the test compound for a given CYP must be known or determined with EA407, CYP Inhibition, prior to Ki determination.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with human intestinal microsomes in the presence and absence of NADPH.
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This assay is used to determine the potency with which a test compound inhibits cytochrome P450 (CYP) enzymes.
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This assay is used to determine whether a test compound is a mechanism-based inhibitor of cytochrome P450 (CYP) enzymes.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled mouse liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled primate liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled dog liver microsomes in the presence of NADPH.
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This assay uses fluorogenic substrates to determine the potency with which a test compound inhibits recombinant human cytochrome P450 (CYP) enzymes.
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This assay is used to generate, isolate, and characterize multi-mg quantities of targeted metabolite(s) of a test compound using biomimetic oxidations.
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This assay is used to assess the potential of a test compound to inhibit individual human UDP-glucuronosyltransferase (UGT) isoforms.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with liver S9 fraction (mouse, rat, dog, monkey, or human) in the presence of cofactors.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with cryopreserved hepatocytes (mouse, rat, dog, monkey, or human).
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This assay is used to screen for reversible inhibition of individual cytochrome P450 (CYP) enzymes by a single concentration of a test compound.
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This assay is used to determine the IC50 for reversible inhibition of individual cytochrome P450 (CYP) enzymes by a test compound.
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This assay is used to screen for time-dependent inhibition of individual cytochrome P450 (CYP) enzymes by a test compound before and after pre-incubation with NADPH.
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This assay is used to screen for time-dependent inhibition of individual cytochrome P450 (CYP) enzymes by a test compound after pre-incubation with and without NADPH.
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This assay is used to identify time-dependent inhibition of individual cytochrome P450 (CYP) enzymes by a test compound using the IC50 shift approach.
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This assay is used to assess the potential of a test compound to inhibit individual human UDP-glucuronosyltransferase (UGT) isoforms.
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This assay is used to detect glucuronidation of a test compound after incubation with human liver microsomes in the presence of UDPGA.
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This assay is used to detect a glutathione conjugate of a test compound, due to formation of a reactive metabolite, after incubation with human liver microsomes in the presence of NADPH and GSH.
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This screening assay is used to detect putative metabolites of a test compound produced by expected biotransformations in pooled liver microsomes, S9 fraction, or hepatocytes.
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This screening assay is used to detect metabolites from expected biotransformations and perform putative structure assignment, after incubation of a test compound with pooled liver microsomes, S9 fraction, or hepatocytes.
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This assay is used to identify metabolites of a test compound produced by pooled liver microsomes, S9 fraction, or hepatocytes.
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This assay is used to identify and elucidate structures of metabolites of a test compound after incubation with pooled liver microsomes, S9 fraction, or hepatocytes.
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This assay is used to assess the potential of a test compound to induce CYP3A activity in rabbit or dog hepatocytes.
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This assay uses human liver microsomes and selective enzyme inactivation to determine if a test compound is metabolized by flavin-containing monooxygenase (FMO).
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This assay uses human liver S9 fraction and a chemical inhibitor to determine if a test compound is metabolized by monoamine oxidase (MAO).
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This assay uses fluorogenic substrates to screen for inhibition of recombinant human cytochrome P450 (CYP) enzymes by a single concentration of a test compound.
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This screening assay is used to identify the CYP(s) involved in the metabolism of a test compound, through the use of CYP-specific Supersomes.
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This screening assay is used to identify the CYP(s) involved in the metabolism of a test compound, through the use of human liver microsomes and CYP-specific chemical inhibitors.
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This assay uses recombinant human enzymes (Supersomes) to determine if a test compound is metabolized by flavin-containing monooxygenase (FMO).
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This assay uses recombinant human enzymes (Supersomes) to determine if a test compound is metabolized by monoamine oxidase (MAO).
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This study design is used to determine the maximum tolerated dose (a dose that does not produce mortality or overt clinical signs of toxicity) of a test article in male and female rats after single and repeat dosing (non-GLP).
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This GLP study design is used to determine the toxicity of a test article in male and female rats after repeat dosing for 14 days followed by a 7 day recovery period.
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This study design is used to determine the maximum tolerated dose (a dose that does not produce mortality, more than a 10% decrease in body weight or overt clinical signs of toxicity) of a test article in male and female dogs after single and repeat dosing (non-GLP).
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This assay is used to determine the acute systemic toxicity of a device or device material in mice or rabbits and is required for most medical-grade materials and devices that are intended to make contact with the patient for more than 24 hours.
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These tests assess the local irritation potential of a test material, using sites such as skin or mucous membranes, in rabbits.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to human plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to rat plasma proteins.
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Ultracentrifugation is used in this assay to determine the percentage of test compound that binds to plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to plasma proteins.
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Determination of the fractional binding of test compound to plasma proteins using an ultrafiltration technique.
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This assay is used to determine the unbound fraction of test compound in a rat brain homogenate via equilibrium dialysis.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to mouse plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to primate plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to dog plasma proteins.
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This assay is used to determine the blood-to-plasma partition coefficient of a test compound in mice, rats, or humans in vitro.
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This assay is used to determine the blood-to-plasma partition coefficient of a test compound in mice, rats, and humans in vitro.
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This screening assay is used to determine the bioavailability of test compounds relative to a reference compound after oral administration to rats.
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Determination of brain-to-plasma ratio of a test compound in rats or mice following IV or oral dosing.
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This assay uses in situ brain perfusion to determine both the potential brain penetration of test compound and whether it is a P-gp substrate.
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This assay is used to determine the absolute bioavailability of a test compound in mice.
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This assay is used to determine the bioavailability of a test compound in dogs when the compound is administered by at least two different routes.
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This screening assay is used to determine the bioavailability / exposure of test compounds after two routes of administration to male mice.
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This screening assay is used to determine the bioavailability / exposure of test compounds after two routes of administration to male rats.
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This assay is used to determine the bioavailability / exposure of test compounds in male dogs after two routes of administration.
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This assay uses in vivo carotid infusion to determine the extent of brain penetration of test compound in a physiological setting, including plasma protein binding.
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This assay is used to determine the bioavailability / exposure of a test compound in dogs after two routes of administration (non-crossover).
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This screening assay uses the general CYP inhibitor, 1-aminobenzotriazole (ABT), to determine the role of absorption vs. first-pass metabolism in limiting the systemic exposure of a test compound in rats.
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This assay uses oral, intravenous, intraduodenal, and intraportal vein dosing in rats to evaluate the barriers to bioavailability of a test compound.
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This non-GLP assay is used to determine a preliminary BCS solubility classification by measuring the quasi-equilibrium solubility of a test compound in aqueous USP buffer systems at two pH values between 1.0 and 7.4.
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This GLP assay is used to determine a BCS solubility classification by measuring the quasi-equilibrium solubility of a test compound in aqueous USP buffer systems at four pH values between 1.0 and 7.4.
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This non-GLP assay is used to determine a preliminary BCS permeability classification by measuring the permeability of a test compound through Caco-2 cell monolayers in both the apical-to-basolateral and basolateral-to-apical direction.
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This GLP assay is used to determine the BCS permeability classification of a test compound across Caco-2 cell monolayers at three concentrations and two pH values.
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This assay is used to develop dose vehicle(s) for a test compound, as a solution or suspension prior to in vivo pharmacokinetic testing.
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Overview Sheets
Drug Interaction Studies — Study Design, Data Analysis, and Implications for Dosing and Labeling
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The benefits of knowing if your compound crosses the blood-brain barrier (BBB)
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Poster Presentations
Research Reports