Stability in plasma, Bloood/Plasma (B/P) ratio, Plasma Protein Binding (PPB) and quantification in samples from Pharmacokinetics/Toxicokinetics
Aim of the study
The determination of plasma stability, B/P ratio and PPB of a theragnostic compound (peptide) and its quantification in samples deriving from PK/TK studies.
The analyte was incubated in plasma deriving from different species, then extracted and analyzed by LC-MS/MS to evaluate its stability in plasma.
The analyte was incubated in blood from different species, then blood was separated in plasma and red cells by centrifugation. Analyte was extracted and analyzed by LC-MS/MS to evaluate its partitioning between plasma and red cells.
The analyte was incubated in plasma deriving from different species, then protein-bound analyte was separated from unbound analyte by equilibrium dialysis or ultrafiltration. Analyte was extracted and analyzed by LC-MS/MS to evaluate the level of its PPB.
The analyte was extracted from samples deriving from in vivo PK/TK studies and quanti-fied by LC-MS/MS.
Analyte: A theragnostic peptide.
System: Plasma or blood from different species.
Therapeutic area: Oncology
Development stage Preclinical
Customer: An innovative radiopharmaceutical company developing, producing and commercializing molecular nuclear medicine theragnostics.
Plasma stability, B/P ratio and PPB of a theragnostic peptide were successfully determined. Moreover, its plasma PK/TK profile after in vivo administration was obtained.
Advantage of the methodology
LC-MS/MS allowed the accurate quantification of the theragnostic peptide after plasma stability, B/P ratio, PPB and PK/TK experiments. All these data were fundamental for the successful development of the theragnostic peptide from being a lead compound to become a new pharmaceutical drug.