Domainex offers you a comprehensive suite of assays that provide essential information on the absorption, distribution, metabolism and excretion of your novel compounds, determined via our suite of bioanalytical services.
ADME testing results can be used to predict how they will behave in the body, and to assess their potential for adverse interactions with other drugs. This valuable information is used by our medicinal chemists, combined with biological screening data, in order to select compounds for progression and to identify candidate drugs in the shortest time possible.
In Vitro ADME Assays
Our ADME services are provided to you as part of our integrated drug discovery services. We can provide a range of in vitro tests including:
- Physico-chemical property profiling:
- LogD and ChromLogD
- Solubility (kinetic and thermodynamic) in phosphate-buffered saline (PBS) and biological fluids, and at a range of pH values
- Stability in PBS or biological fluids (e.g. plasma, blood and cerebrospinal fluid)
- Metabolic stability (as % turnover, half-life or intrinsic clearance):
- Liver microsomes
- Cryopreserved hepatocytes
- Other tissues and fluids
- CYP450 inhibition
- Plasma protein binding
- Plasma and blood stability
- Cell accumulation and permeability
- Permeability in a Caco-2 cell assay
- Tissue bioanalysis
- Metabolite identification (in liver microsomes and hepatocytes)
- Reactive metabolite screening
- Design of experimental formulations (for IV, PO, SC and IP dosing)
Figure 1: Example cellular accumulation data
Figure 2: Example data from Microsomal and Tissue Homogenate assays by LCMSMS
For the next stage of ADME assessment, we can arrange for your compounds to be tested by our closely located research partner, Pharmidex, in routine or customised pharmacokinetic assays. Domainex and Pharmidex have built up an excellent working relationship of over a decade, giving you a seamless solution of PK profiling during Lead Optimisation.