Pharmaceutical profiles complete microdosing study
schedule and with improved accuracy, could herald a new era in drug
development in which human ADME data is involved in candidate
selection or deselection.
The microdosing approach has provided pivotal early human PK data on the performance of the candidate drug much more quickly and accurately thus allowing improved compound selection and reduced attrition rates in early clinical development.
In microdosing studies, one or more drug candidates is administered to humans in single, sub-pharmacological (microgram) levels to obtain early PK and ADME data in order to select the candidate with the optimal PK characteristics. Microdosing studies have been endorsed by the European Medicines Agency (EMEA), who have determined that a microdose is 100 times below the level calculated to yield a pharmacological effect or 100 micrograms, whichever is the lower.
Clinical development specialist Pharmaceutical Profiles took less than six months from inception to completion to examine the pharmacokinetics (PK) of the HIV inhibiting molecule, alphaHGA in healthy subjects, following dosing with sub-pharmacological, microgram quantities of drug candidate.
The study was carried out for Tripep, a biotech research company that develops and commercialises candidate drugs based on patented and patent-pending technologies.
The microdose study has shown 100 per cent oral bioavailability for alphaHGA allowing fast tracking of the molecule into 'proof-of-concept' studies with an enhanced chance of success and significantly reduced risk.
Tripep's Dr Anders Vahlne, acting CEO and head of research said: "The results will help us design the clinical study on HIV infected individuals expected to start by the end of this year or early next year."
Human microdosing offers the promise of selecting the best drug candidates before advancing into full development, increasing the chance of success.
Accelerator mass spectrometry (AMS) is the key biomedical application that is used in the area of human microdosing. It is one of the most precise bioanalytical approaches currently available - up to 100,000 times more sensitive than LC-MS/MS and 1,000,000 times more sensitive than liquid scintillation counting (LSC).
The importance of PK and ADME data in early phase drug development has become increasingly significant especially when 40 per cent of new drugs 'fail' during Phase I trials. Human microdosing offers the promise of selecting the best drug candidates before advancing into full development, increasing the chance of success.
