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  5. Translational Imaging

At every phase during the drug development process there are times when an imaging experiment can produce data that cannot be obtained as well, as quickly, as inexpensively ... or at all by other means. Effective use of imaging for drug development involves identification of those opportunities and exploiting them to speed the drug development process.

In early discovery, radiolabeling a drug candidate can provide rapid information concerning whole body and individual organ distribution and clearance.

  • Does the drug enter the brain?
  • Is hepatobiliary clearance significant?
  • Which drug candidates have the better profiles?
Such answers can be obtained using small numbers of animals in data-rich experimental protocols.

Using a tracer that shows available binding sites or enzyme activity. can permit functional evaluation of drugs without radiolabeling the drugs themselves. This permits rapid comparison of the biochemical targeting in vivo of large numbers of drug candidates at relatively low expense. Which of your candidates does the better job at the biochemical target, and does it for the optimum duration of action?

Formulations development: Which formulations provide the best delivery profile and how long do they maintain action at the target? What is the optimum dose and dosage schedule to maintain effectiveness?

Toxicity: Does the drug accumulate in ways that enhance toxicity? Does it penetrate to a fetus?

Imaging can be accomplished:

  • On your, or your contractor's, site
  • At our Arkansas location in collaboration with UAMS researchers and InviCRO
    • Access to specialized academic skills and translational research
  • At our Michigan location in collaboration MPI and InviCRO
    • Access to expert data modeling and analysis
    • Access to expert animal study design and animal models
    • Access to a variety of species including several NHP's
    • Access to a variety of disease models
    • State of the art histology and toxicology

Custom labeling services are available to label your drug for in-vivo pharmacokinetic studies. Determine penetration into the brain, penetration into target organs, accumulation in tumors, patterns and kinetics of distribution after adminstration by intravenous, and intrathecal injection, oral and pulmonary inhalation, and oral dosing. Determine the optimum formulation and dosing parameters based on targeted distribution, not just blood concentrations.

Biologicals (antibodies, other proteins, oligonucleotides, nanoparticles) can be labeled with F-18, radioIodines, Zr-89, In-111, Tc-99m with relative ease and used to obtain quantitative biodistribution and kinetic information.

Small molecule drugs can often be radiolabeled through a collaboration between our laboratory and yours. The methods depend upon the structure of each drug molecule. A short consultation can determine the potential methods and degree of effort that would be required to radiolabel any individual drug candidate.

A rapidly growing variety of functional probes exists to measure the effects of your drug on

  • regional tissue metabolism of
    • glucose
    • amino acids
    • nucleic acids
  • tissues via reporter gene technology (FIAU, Nal)
  • action at receptors
  • action at transporters

Check out our lists of existing C-11, F-18, I-124 and Zr-89 tracers for such uses, and keep in mind that new items are being constantly added, and can be added to your specifications.