The DMPK team has extensive pharma and biotech experience delivering high-quality data, helping medicinal chemists design better compounds, and supporting better decisions throughout drug discovery. From the hit-to-lead through lead optimization, DMPK parameters help direct resources to the most promising chemical series and ensure the selection of the drug candidate.
Our comprehensive portfolio includes in vitro ADME, in vivo PK, Discovery Bioanalysis, PreFormulation as well as DMPK consultancy services.
in vitro ADME
Early assessment of in vitro absorption, distribution, metabolism and excretion (ADME) is fully integrated in today’s drug discovery efforts to fuel and enhance the design of new compounds to get drug candidate like properties.
Novalix offers a selection of well-established in vitro ADME assays to assess physicochemical properties of compounds, as well as metabolism, binding, permeability and drug-drug interactions.
Range of services and capabilities
| Absorption | Distribution | Metabolism | Drug Drug Interaction |
| • Chrom LogD, LogD & LogP • pKa • Kinetic solubility & Thermodynamic solubility • Chemical stability • Caco2 permeability | • Plasma protein binding • Blood plasma partitioning • Tissue binding | • Microsomal stability • Hepatocyte stability • Long Term plated Hepatocytes stability • Metabolite Identification (microsomes/hepatocytes) | • CYP inhibition • CYP3A Time Dependant Inhibition (KI / kinact) |
in vivo Pharmacokinetics
Assessment of in vivo pharmacokinetic (PK) properties is a key requirement in the evaluation of new compounds in Drug Discovery projects. This allows to validate some in vitro to in vivo hypothesis/correlations and help to discharge risks in the progression of would-be drug candidates.
Range of services and capabilities
We have AAALAC-accredited in-house facilities housing mice and rats.
Various PK studies designs can be proposed, depending on the question asked.
It can be done using standardized or customized protocols.
PK parameters are analyzed using pharmacokinetic equations.
Obtained data can be further modelled for PK/PD purpose in support of pharmacodynamic or safety studies.
Examples and features of PK studies
• Cassette and single compound PK studies
• Tissue distribution (kinetic or single timepoint) studies
• Ascending dose and multiple dose studies
• Excretion studies
• Various routes of administration (intravenous, oral, intraperitoneal, subcutaneous)
• Microsampling
Discovery Bioanalysis
Novalix offers non-GLP bioanalytical services to support fit-for-purpose analyses. For routine screening of compounds, a number of generic LC-MS/MS optimization and analytical procedures can be used to ensure high quality, while minimizing time and cost and are accepted based on pre-defined acceptance criteria. On the other end, some specific analytes will require a dedicated analytical method development.
Range of services and capabilities
• Mass spectrometry including high-resolution MS
• Bioanalytical method development
• Support to in vitro ADME, in vivo PK and in vitro / in vivo pharmacology studies
• Microsampling analysis (from 10µL samples)
• Dose formulation analysis
• Analysis of biomarkers and endogenous compounds
• Analysis in a wide range of biological matrices like plasma, serum, whole blood, urine, bile, faeces as well as tumor and tissues
• Generation of PK parameters
Mass Spectrometry platforms
• Liquid chromatography-tandem mass spectrometry (LC-MS/MS)
• Liquid chromatography-high resolution mass spectrometry (LC-MS, HRMS)
Discovery Formulation and solid form analysis
Understanding well the solid form of a given batch of a test compound as well as developing an appropriate formulation to maximize in vivo exposure of the test compound can be critical for their early evaluation.
Novalix offers a range of services to characterize batches as well as to design early formulations using different technologies with just few mg material.
Range of services and capabilities
• Design of a stable non-precipitating solution
• Early formulation development
• Advanced formulation for poorly soluble compounds
• Batch analysis and control
• Physicochemical properties of compounds
Discovery Formulation equipments platform
• Sirius T3 (Pion) : pKa, LogP, solubility
• Aeris X Ray (Panalytical) : Solid state
• DSC (Meetler Toledo): Thermal event
• TGA (Meetler Toledo): Weight loss
• Mastersizer 3000 (Malvern): Particule size
• Morphologi 4 (Malvern): Particule size morphology
• Microdissolution (Pion): Dissolution
• Spray dryer (Buchi): Amorphous solid dispersion manufacture
• Precellys (Bertin technologies): Particule size reduction (micro)
• Pulverisette (Fritsch): Particule size reduction (micro)
• Roller Mill (Exmore): Particule size reduction (nano)
DMPK Consultancy
During the course of a drug discovery project, a variety of DMPK assays are run and a large number of DMPK data are generated. DMPK experts can help to guide in the selection of the suited ADME-DMPK assays to run as well as to interpret the data obtained.
Range of services and capabilities
Novalix provides access to DMPK Consultants to support Drug Discovery projects or to answer specific questions a project team might have. Our experts have large Pharma and Biotech experience in Drug Discovery projects. The DMPK expertise support can be provided as a stand-alone activity or as an integral part of a drug discovery project.
Common DMPK consultancy activities include
• Interface with chemists for molecule optimization
• Drug Drug Interaction risk assessment
• PK/PD support
• Human dose prediction
• Modelling
Leverage our ADME-PK, and preformulation capabilities to drive your discovery — contact us.