Human AME (hAME) Studies with Radiolabelled Compounds
Human AME (hAME) Studies with Radiolabelled Compounds
Pharmaron is a Clinical Research Organisation (CRO) offering comprehensive human AME services to support a wide range of 14C radiolabelled studies in humans, including mass balance, metabolite profiling/metabolite identification (MetID), absolute bioavailability (ABA), and IVPK. We are unique in providing fully integrated solutions that include radiosynthesis, in vitro and preclinical ADME, QWBA, human dosimetry, 14C dose formulation, radio-analysis including AMS, and the conduct of your definitive 14C human clinical studies.
Ultra-sensitive AMS and HP(UP)LC+AMS analysis can be utilized for the quantitation of total radioactivity and 14C parent/metabolites in human metabolism and absolute bioavailability clinical studies. Phase l clinical protocols can include either micro tracer or macro tracer doses of radioactivity and employ both LSC and AMS analytical support. Hybrid study designs can take advantage of LSC analysis for early time points and AMS analysis for later time points.
We also offer Phase 0 microdose studies under an eIND (exploratory investigational new drug) to evaluate the PK and excretion of early-stage compounds. 14C studies can be conducted at Phamraron’s Clinical Pharmacology Center (CPC) in Baltimore, or we can support third-party clinical research units (CRU).
Capabilities
Clinical Protocols
- Absorption, Metabolism, Excretion (hAME) – Low 14C radioactive dose micro tracer studies administering ~1-5 µCi of radioactivity compounded with a therapeutic, pharmacologically-relevant mass dose
- Absorption, Metabolism, Excretion (hAME) – High 14C radioactive dose macro tracer studies administering ~100-200 µCi of radioactivity compounded with a therapeutic, pharmacologically-relevant mass dose
- Absolute Bioavailability (hABA) – Low 14C radioactive IV microdose studies administering ~1-5 µCi of radioactivity intravenously concomitant with a therapeutic extravascular mass dose administered by the intended therapeutic route
Radiolabelled Metabolism Studies
- Phase l hAME studies employing 14C macro tracers or 14C mictrotracers
- Mass balance, metabolite profiling, and metabolite identification for metabolite safety testing (MIST)
- IV 14C micro tracers for hABA
- Phase 0 microdosing studies under eIND
- Ultra-sensitive 14C total radioactivity by AMS, metabolite profiling, and 14C-parent/metabolite quantitation by LC-AMS
- Metabolite identification (MetID) by HRMS
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Radiosynthesis
- Standard 14C and 3H radiosynthesis
- GMP preparation of both 14C-drug substance and 14C-drug product
- Non-GMP clinical-grade re-purification of 14C-drug substance for dose formulation in human micro tracer studies
- 14C and 3H radiolabelling of large molecules e.g., oligonucleotides, peptides, proteins
- Expert metabolism and biotransformation advice for the position of label in the molecule
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Download PDF to learn more about Pharmaron’s Integrated Radiolabelled Metabolism & PK Programs.
