MicroConstants performs industry-standard assays, custom drug metabolism research, and IND-enabling studies to assess drug-drug interaction potential, metabolic stability, metabolite formation, and protein binding. Whether you are in discovery, lead optimization, or collecting data for regulatory submissions, we will work with you to define the level of research appropriate for your compounds. Results can be presented as a formal report suitable for regulatory submissions, or as an informal report (i.e. raw data tables in Excel).

1. Metabolic Stability Assays
• Determine the extent of metabolic stability in
vitro to help determine the potential half-life of
a compound when dosed to animals or humans
• Evaluate the stability of a test article in a variety
of enzyme sources, including: hepatocytes,
liver microsomal preparations, hepatic cytosol,
hepatic mitochrondrial fraction, hepatic S9
fraction, and membrane preparations from
recombinant bacteria or eukaryotic cells
Metabolite Profiling & Identification
• Identify the candidate’s metabolic pathway
to understand the fate of the drug and
metabolites, and to assist with species selection
for toxicology studies
• Analyze samples generated either in vivo or in
vitro using accurate mass spectrometry
• Search data sets for potential metabolites and
compare the time profiles of parent compound
loss and metabolite formation using enzyme
sources from various animal species
Protein Binding Assays
• Use equilibrium dialysis, ultrafiltration, or
ultracentrifugation methods to determine the
extent of drug binding to plasma, serum, tissue,
or to proteins such as human serum albumin or
α1-acid glycoprotein
• Perform regulatory submission-quality studies
or screening assays to assess binding values
in vitro Drug-Drug Interaction Studies
Studies are performed in accordance with FDA
Guidance on Drug-Drug Interaction Studies:
CYP Induction Studies
• Understand possible drug-drug interaction
liabilities of a compound by assessing it’s
potential to induce drug metabolizing enzymes
and transporters in plateable cryopreserved
hepatocytes from one or more donors
• Receptors tested include AhR, PXR, and CAR
CYP/UGT Inhibition Studies
• Assess whether your compound inhibits drug
metabolizing enzymes
• Human liver microsomes, FDA-accepted probe
substrates, and control inhibitors are used to
assess IC50
and Ki
values for CYP1A2, 2A6, 2B6,
2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 isoforms
• Recombinant UGT enzymes are used to assess
IC50
values of a test article with respect to the
most common isoforms including UGT1A1, 1A3,
1A4, 1A6, 1A9, 2B7, and 2B15 enzymes
CYP/UGT Reaction Phenotyping
• Determine CYP/UGT enzymes involved in the
metabolism of a compound
• Three FDA approved methods may be used,
including correlation analysis, isoform-specific
chemical or antibody inhibition, and/or
recombinant CYP/UGT enzymes
MicroConstants performs industry-standard assays,
custom drug metabolism research, and IND-enabling
studies to assess drug-drug interaction potential,
metabolic stability, metabolite formation, and protein
binding. Whether you are in discovery, lead optimization,
or collecting data for regulatory submissions, we will work
with you to define the level of research appropriate for your
compounds. Results can be presented as a formal report suitable for
regulatory submissions, or as an informal report (i.e. raw data tables in Excel).
DRUG METABOLISM ASSAYS
DMPK SERVICES
9050 Camino Santa Fe
San Diego, CA 92121
PHONE
+1.858.652.4600
TOLL FREE
+1.866.232.9497 (U.S.)
WEB
microconstants.com
Contact us for more info
or to request a quote.