|
|
Available services 2010
Metabolism studies - in vitro - Metabolic stability
- Metabolite identification: biotransformations
- Metabolite identification: structural analysis (MS and NMR)
- Kinetics of metabolic stability
- Kinetics of metabolite formation
- Prediction of in vivo kinetics
- Identification of rate-limiting CYP enzyme
- Identification of rate-limiting UGT enzyme
- Metabolic profiles human vs animals
- Organ specific metabolism
- Reactive metabolite trapping
Metabolism studies - in vivo - Bioavailability
- Metabolite identification: biotransformations
- Metabolite isolation
- Metabolite identification: structural analysis (MS and NMR)
- Tissue homogenate analysis
- Pharmacokinetic calculations for parent and metabolites
- Quantitative bioanalysis (DMPK)
- Vehicle finding, vehicle stability
- Validation of bioanalytical methods
| Available species for DMPK: mouse, rat, rabbit, dog (longer lead time |
Drug interaction studies
- CYP inhibition prediction in microsomes: cocktail study
- CYP induction prediction: nuclear receptor activation
- CYP inhibition confirmation in hepatocytes: cocktail study
- CYP induction confirmation in hepatocytes: cocktail study
- Identification of CYP enzymes responsible for oxidative metabolism
- by recombinant CYP enzymes
- by specific inhibitors
- by antibodies
- Mechanism based inhibition (time dependent inhibition)
CYP450s: CYP1A2, CYP2A6, CYP3A4, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1
Available receptors: PXR, CAR, PPAR, LXR, FXR |
Permeability studies- Caco-2 (subcontracted)
- MDCK (subcontracted)
- LLC (subcontracted)
- PAMPA (hexadecane/phospholipid)
- Skin and placenta permeability (subcontracted)
- Transporter interaction assessment
- ATPase
- transporter inhibition (subcontracted)
- accumulation (subcontracted)
- Efflux transporter interaction: Calcein-AM extrusion (long lead time)
- BBB in vitro: bovine brain microcapillary endothelial cell model (long lead time)
- BBB in vivo: whole or dissected brain homogenate analysis
- BBB in vivo: micro-dialysis (long lead time)
Available cell lines: For other cell lines (e.g. Calu-3 REK) request for availability and lead time.
Available tissues: Isolated human skin, Human placenta |
Basic property characterisation - Solubility
- pKa
- Lipophilicity (logD, logP)
- Protein binding (equilibrium dialysis or ultrafiltration)
- Plasma stability
- Chemical stability
- Degradation product identification
- Impurity identification
- Analytical method development and validation
Custom analytical capabilities - UPLC/TOF-MS, HPLC/TOF-MS, UPLC/MS/MS, 2xHPLC/MS/MS and HPLC/RAD
- Access to 200, 300, 400 and 500 MHZ NMR, 500 MHz LC/NMR and GC/MS
Consultation - Second opinion of existing reports in bioanalytics and metabolism
- Evaluation of existing ADME data
- Interpreting of existing ADME data
- Study planning
- Go / no-go criteria selection
Novamass is a provider of ADME studies in late screening phase where tailoring is needed to find optimum study conditions for each individual molecule.
For further information, prices, study fact sheets and model reports, please contact us at info@novamass.net. |
|
|
