ADME-PK

ADME Tox is an area of drug development for assessing the potential safety concerns for new compound entities (NCEs). ADME tox studies evaluate how a drug and/or its metabolites are absorbed, distributed, metabolized, and excreted from the body. Drug metabolism issues is one of the primary reasons why drug candidates fail in clinical trials.

Traditionally, ADME studies were performed later in the drug development process. However, more than half of the compounds failed to make it to the market due to poor ADME Tox properties. As a result, in vitro screening of drug candidates in the early phases of development is now used as a more cost-effective and timely approach to identify compounds that may have unfavorable ADME characteristics.

PerkinElmer's Contract Research Services offers a comprehensive range of in vitro assays and programs, ADMEScreen™, to assist you in improving your turnaround time in candidate selection for further development.

ADMEScreenTM  

ADMEScreen is a suite of offerings aimed at different stages of ADME drug development ranging from in vitro DMPK (Discovery ADME) to Maximum Tolerated Dose and PK studies (Development ADME) to Pharmacokinetic Characterization. Our staff can provide you with bioavailability of your compound by designing PK studies followed by a thorough analysis of your sample through LC/MS method development and bioanalysis.

PerkinElmer's Contract Research Services also offers customized ADME Tox assays where you can create your own ADME tox panel. View our complete list of ADME-Tox assays.

Discovery ADME
In vitro DMPK screens are tools for early stage lead candidate assessments. PAMPA (membrane permeability), CaCO-2 and MDCK (gut and renal absorption), CYP450 inhibition (of over 30 isoforms) and induction, S9 and microsomal stability (metabolic stabilities), as well as other in vitro metabolic screens, are a suite of useful yet inexpensive tools necessary to triage, characterize, and rank lead compounds which have the potential to become useful drug candidates.

As with all of PerkinElmer's assay services, our Cytochrome, P450 assays are available as 'one-offs' where you can select which assay is of interest or you may select our prepackaged CYP assay panels. CYP assay panels available include:

  • CYP Basic - total of 6 CYP assays all using human source material
  • CYP Regulatory - total of 17 CYP assays all using human source material
  • CYP Explorer - total of 31 CYP assays covering all isoforms currently available

Development ADME

Our Development ADME program is for those researchers with drug candidates further in development. PerkinElmer's Contract Research Services currently offers the following services within our Development ADME program:

  • Formulation
  • Rat PK
  • Mouse PK
  • Mouse Maximum Tolerated Dose
  • Rat Maximum Tolerated Dose
Pharmacokinetic Characterization
For those researchers ready for in vivo optimization, PerkinElmer's Contract Research Services' pharmacokinetic characterizations are a useful tool providing researchers a first glimpse at the fate of their lead compounds in vivo. The studies characterize and provide an array of pharmacokinetic parameters of a chemical in a defined rodent species via a specific route or routes of drug administration. The study provides drug concentration at specific time points of specified organs, such as the brain, liver, heart, lung, kidney, pancreas, and plasma; non-compartmentalized analysis of AUC (area under the curve), Tmax, Cmax and calculated bioavailability. With this information, the subsequent dosing and efficacy assessment maybe performed with a specified lead candidate in an appropriate time frame and routine.