Plasma Stability Assay
Creative Animodel provides plasma stability assays for the prediction of physicochemical parameters that describe the PK characteristics of new drug candidates in early stages of drug discovery. We have a broad platform and rich experience to guarantee our clients consistent and high-quality data with cost-efficiency that come from a highly automated approach.
Why Plasma Stability Assay Is Important?
Stability of compounds in the plasma is essential for both bioavailability and in vivo therapeutic efficacy. However, certain classes of candidate drugs are potentially unstable due to the hydrolysis resulting from plasma enzymes, of which proteases and esterases are the most relevant in the pharmaceutical development process. Unstable compounds tend to exhibit rapid clearance, short half-lives and consequently poor in vivo activity. Thus, such drugs, including esters, amides, lactones, lactams, carbamides, sulfonamides and peptide mimetic, require screening for plasma stability.
How Is Plasma Stability Assay Performed?
The aim of plasma stability assay is to investigate the degradation of your drug for the screening of prodrug stability and active compounds. We provide in vitro plasma stability assay in human and diverse animal species (mouse, rat, dog, pig and monkey). Instead of plasma, stability in particular solutions and other matrices (such as tissue homogenates) can also be measured.
Generally, the tested compounds are incubated in plasma at 37℃, and each group is conducted in duplicate. After incubation, the parent compound is investigated by LC-MS/MS analysis at five-time points over 120 minutes (0, 15, 30, 60 and 120 min). The percentage of parent compound remaining in plasma is plotted at each time point, and the half-life (T½) is calculated from the obtained curve. For the use of prodrugs screening, the disappearance of prodrugs and the appearance of active compounds can be investigated simultaneously.
Figure 1. Plasma stability of two compounds tested by Plasma Stability Assay in human plasma over 120 min: Compound 1 (poor plasma stability, blue line) and Compound 2 (high plasma stability, red line). Data are shown as mean ± standard deviation.
What Can Plasma Stability Assay Do?
• Screen prodrugs and antedrugs
• Monitor and modify labile structural motifs
• Prioritize compounds for in vivo studies
Creative Animodel provides plasma stability assays to improve the physicochemical properties of new drug candidates. With years of experience, our in-sight scientists devote to helping our customers to increase the chance of finding the optimal bioavailability and pharmacokinetic profile in the drug development process.