Radiolabeled In Vivo PK/ADME Study

Radiolabeled In Vivo PK/ADME Study

Platform Introduction

Lead Optimization (LO)

If the test article is found easy to bind and challenging to extract in specific test systems (cells, plasma, and other biological matrices), 14C- and 3H- labeled test articles can be used to reduce the difficulty of sample treatment and eliminate the effect of low recoveries. It is recommended to use radiolabeled test articles for endogenous substances to avoid endogenous interference and obtain accurate exogenous data.

Pre-Clinical Candidate (PCC)

A following administration of the radiolabeled test article is typically performed when the test article has a low bioavailability. It is determined to be due to poor absorption or rapid metabolism by comparing the post-labeled results (parent and metabolites) and pre-labeled (only parent) results. The results can help to optimize the chemical designs.

Investigational New Drug (IND) application

Radiolabeled test articles can solve the low recovery issue in the mass balance studies. The Quantitative Whole-Body Autoradiography study (QWBA) can obtain complete and detailed tissue distribution information by scanning the animals’ whole body. This can be used to predict the drug efficacy and accumulation degree comprehensively to guide clinical medication.

Our Radiolabled Research Platform

Key Features

Dares to Develop

14C- and 3H- radiolabeled test articles are applied in preclinical and clinical studies to meet NMPA and FDA submission requirements and successfully fill the research field gap in China.

Strive For Excellence

By optimizing the collection and detection methods, the total recoveries of most radiolabeled test articles can exceed 90% in the mass balance studies. For those below 90% (rare), the 14C CO2 collection apparatus can help to increase the recovery rate and achieve the excretion route.

Customized Design

We can combine the non-labeled and radiolabeled methods to provide a personalized study design for customers based on the characteristics of test articles. This includes and is not limited to in vitro plasma protein binding studies, in vitro metabolite profiling in various incubation systems (plasma, S9, liver microsomes, hepatocytes), and in vitro CYP/UGT enzymes phenotyping studies.

Our Strengths

Experienced and Comprehensive

WuXi AppTec has over ten years and more than 300 IND and NDA submission experience, we provide radio-related preclinical and clinical analysis studies.

Well Controlled Timeline and Cost

14C-labeled test articles can be provided by the client or synthesized directly in WuXi AppTec. We reduce the cost, shorten shipping time, and design reasonable labeling sites based on chemical structure, synthetic process, and early-stage metabolite identification results.

Quick Turnaround Time

By collaborating with multiple hospitals, the shortest time to submit mass balance results can be 24-48 hours. Preliminary data can help determine whether the experimental expectation is achieved or the clinical volunteers can be out of the group.

Main Assay Type

Radiolabeled In Vivo PK/ADME Study Main Assay Type

Representative Quantitative Whole-body Autoradiography (QWBA) Images following Administration of 14C- labeled Test Article to Rats

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