Human microdosing will reduce drug discovery time, says Xceleron

Xceleron, specialist in ultra-sensitive analysis techniques for the acceleration of drug development, has announced that the results of the Consortium for Resourcing and Evaluating AMS Microdosing's (CREAM) trial into the efficacy of human microdosing in drug development have been published in Clinical Pharmacology and Therapeutics (2006; 80:203-215).

The publication follows the announcement of the study's preliminary findings at ASCPT in 2005.

Xceleron says that the results of the independent trial demonstrate that microdosing provides a valuable insight into the human pharmacokinetics (PK) of new drug candidates which can be used to assist in the compound candidate selection process, establish the likely pharmacological dose, and select the best animal species for long term toxicological studies from microdose metabolite profiling data.

Colin Garner, ceo of Xceleron, said: 'Publication of these results in a highly cited peer-reviewed publication confirms our belief in the preliminary data last year. Since then we have seen a dramatic up-swing in the number of pharmaceutical and bio-technology companies using microdosing to accelerate drug development through faster candidate selection.'

Working on the principle that 'the best model for humans is human', human microdosing, using Accelerator Mass Spectrometry, enables the introduction of sub-pharmacological doses of new drugs into man much earlier than ever before possible.

However, there has been concern within the pharmaceutical industry that a microdose may not predict the behaviour of clinical doses. It is suggested that non-linearities may be induced when binding, metabolising or eliminating systems become saturated.

The trial by CREAM addressed this issue, using several drugs with known human PK characteristics at pharmacological dose levels. Each compound was administered at a microdose level and at a therapeutic dose level to subjects in an appropriate cross-over design. The trial was set up to be a rigorous test using compounds that were expected to strongly challenge the microdosing concept.