Determination of drug or drug metabolite concentrations in biological samples, particularly in serum or plasma, is fundamental to describe the relationships between administered dose, the route of administration, and the time after administration for achieving the optimal clinical response. Rapid metabolism lowers drug exposure at the therapeutic target. Certain types of drug molecules, such as those containing ester or amide-linked groups are prone to enzymatic hydrolysis by plasma esterases, amidases or proteases. On the other hand, enzymatic activation of some prodrugs that takes place in plasma is critical for their function. Hence, plasma enzymes can significantly alter the bioavailability of the active compounds, and therefore determination of the compound stability in plasma has both pharmacokinetic and clinical significance.

Screening of plasma and blood stability provides useful information:

  • In addition to hepatic metabolism, compounds may be degraded/modified by enzymes in plasma, particularly hydrolases and esterases. Unstable compounds tend to have rapid clearance and short half-life, resulting in poor in vivo efficacy.
  • The plasma stability assay can be used to alert teams to labile structural motifs, to prioritize compounds for in vivo studies, and to screen prodrugs.
  • Instability in plasma can result in misleading in vitro data which is difficult to interpret. It may also be challenging to store and analyze clinical samples from in vivo pharmacokinetic studies.
  • Investigation of plasma stability should be performed early in the discovery process in order to assess potential degradation and/or protein binding issues.
  • Compounds with the following functional groups tend to be more susceptible to hydrolysis in plasma: esters, lactones, amides, lactams, sulphonamides, carbamides, and peptic mimetics.
  • Compounds may exhibit interspecies differences in their stability in plasma.

Plasma stability assay is one of our in vitro ADME screening services. Creative Bioarray delivers consistent, high quality data with cost-efficiency that comes from a highly automated approach.

Deliverables

%disappearance of parent compound, Half-life (t1/2) (multiple time-points assay)

Turnaround Time

2-3 Days

Species

Human, rat, mouse, dog and monkey (additional species are available on request)

Time Points

Time points (0, 60, 120, 240 minutes) for half-life determinations; 0 and 240 minutes for %disappearance of parent compound

Detection Method

LC-MS/MS

Test Compound

Incubation concentration 1┬ÁM

Creative Bioarray has an experienced team of experts dedicated to providing customers with the most reliable and highest quality services. For further information on plasma stability assays and to discuss your specific requirements, please contact us at 1-631-626-9181 or email info@creative-bioarray.com.


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