Therefore, determining the level of binding is critical and will directly correlate with efficacy and metabolism of the molecule. Pharmacelsus, a reliable CRO for in vitro ADME and in vivo pharmacokinetic services, offers the determination of the microsomal protein binding by Ultrafiltration.
But not only protein binding of the parent drug might interfere with drug metabolism and saftety issues also reactive metabolites, predominantly formed by oxidative reactions, have been implicated in many drug side effects, e.g. toxicity, hypersensitivity or ideosyncratic reactions.
These unwanted effects are mostly due to covalent binding of reactive metabolites to cellular macromolecules, resulting in altered cell functions and organ toxicity.
Therefore, screening for reactive metabolites using trapping agents such as glutathione (GSH) or semicarbazide (SCZ) is an important part in the drug development process to reduce late attrition rates.
In order to determine the binding of reactive metabolites, Pharmacelsus has established a method for the trapping of reactive metabolites using stable isotope labeled trapping agents and high resolution LC/MS.
Get more details on the experiments and its output in the download area, available on www.pharmacelsus.de.
Services available at Pharmacelsus: ADME & in vitro Pharmacology, Target Finding & Biological Profiling, in vivo Pharmacology & PK, Bioanalytics, Target-Based Bioassays.
About Pharmacelsus
Pharmacelsus - Your reliable CRO for in vitro ADME and in vivo pharmacokinetic services.
Pharmacelsus provides the pharmaceutical and biotech industry with a range of high quality drug discovery and development solutions enabling them to make decisions at critical steps of the drug development process.