Human ADME

Drug metabolites can contribute to inter-subject variability in bioavailability and affect the adverse event or pharmacological profile of a drug. In addition, mammalian species often metabolise drugs differently. As a result, regulatory authorities require human mass balance and metabolite identification data for new drugs.  The recent FDA ‘Safety Testing of Drug Metabolites’ (MIST) guidance published in 2008 (http://www.fda.gov/) has increased focus on the extent and timing of the generation of human metabolism data in the drug development programme.

With more than 20 years experience, we are world leaders in performing human ADME studies. These studies typically use healthy male volunteers, but we are also experienced in conducting them in female subjects and other volunteer populations, including oncology patients. The generation of human ADME data typically involves the administration of pharmacological doses of ¹⁴C-labelled API, enabling an assessment of the mass balance through recovery of the ¹⁴C-label from urine, faeces and, if required, expired air.  The metabolite profile of the drug can also be established and any key metabolites identified and compared with those observed in preclinical toxicology species.

Quotient offers a unique approach to the generation of human ADME data with its Synthesis-to-Clinic platform, bringing together all the required components of these studies from ¹⁴C radiolabelling of the API to final clinical report.

We are also leaders in the conduct of light label ADME studies, which can be particularly effective in facilitiating the generation of  human metabolism data early in the development programme in line with the recommendations presented in the FDA MIST guidance (2008).

For more details on our human ADME capabilities please refer to our Factsheet.