What are the advantages of radiolabeled metabolite identification?

Radioactive tracer technology can eliminate the interference from matrix and effectively track the metabolism, distribution, and excretion of drugs in the body. Through the radioactive metabolite profile, we can clearly and accurately understand the number of major metabolites and the proportion of each metabolite, and more accurately determine whether there are major metabolites in circulation that exceed 10% of drug-related substances, and provide a basis for further evaluation of the safety of major metabolites in human plasma. In addition to advantages in tracing, the use of the [14C] isotope also facilitates the identification of metabolites and a more accurate interpretation of their structure.

How do you perform the radiolabeled metabolite identification?

The samples with low radioactivity intensity were separated by high performance liquid chromatography (HPLC), and the fraction was collected into a LunaPlateTM-96-well plate using Fraction Collector, followed by drying with a SpeedVac system. The dried 96-well plates were measured by Solid Scintillation (Microbeta or TopCount）to obtain offline radio-profiles.The samples with high radioactivity intensity were detected by high performance liquid chromatography with on-line radioactivity detector (ARC or β-RAM) to obtain radio-profiles directly.LC-RAM/HRMS and LC-HRMS were used for screening and structure elucidation of major metabolites in samples.

Radiolabeled MetID (Metabolite Profiling and Identification)

The absorption, distribution, metabolism, and excretion (ADME) studies utilizing radiolabeled compounds can provide information on mass balance , metabolism and excretion, which can guide the studies of phenotype, DDI, transporter, etc.

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Radiolabeled ADME

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Overview

WuXi AppTec DMPK can provide the service of radiolabeled MetID studies with [¹⁴C] and [³H] labeled compounds in vitro, in animals and human. Experimental assays include but not limited to: metabolic stability and metabolite identification studies in vitro (plasma, liver S9, liver microsomes or hepatocytes of multiple species), and in vivo (mice, rats, dogs, monkeys, and humans). The radiolabeled metabolite identification platform has been applied to various compound types, including conventional small molecules, high-polar and non-polar small molecules, natural products, nucleotides, Proteolysis-Targeting Chimeras (PROTACs*), peptides, ADCs, PDCs, oligonucleotides, etc.; Involved matrix types include blood, plasma, urine, feces, bile, tissues, etc.

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Assays

In vitro MetID for cross-species comparison
- Multiple species: mouse, rat, dog, monkey, human, etc.
Matrix: plasma, liver microsomes, liver S9, hepatocytes, etc.
Radioactive detector coupled with LC-MS
To compare in vitro metabolism between human and animals
MetID in animal circulation
- Species: mouse, rat, dog, monkey, etc.
Matrix: plasma
Radioactive detector coupled with LC-MS
To evaluate whether there are major metabolites in the circulation of animals
MetID in animal tissues or excreta
- Species: mouse, rat, dog, monkey, etc.
One or more matrices: urine, feces, bile or tissue, etc.
Sample pooled by equal proportion
Radioactive detector coupled with LC-MS
To propose the major metabolic and clearance pathway in animals
MetID in human circulation
- Plasma sample pooled by AUC method or equal volume
Radioactive detector coupled with LC-MS
To evaluate whether there are major metabolites in the circulation of human
MetID in human excreta
- One or more matrices: urine, feces, etc.
Pooled by equal proportion or equal volume/weight
Radioactive detector coupled with LC-MS
To propose the major metabolic and clearance pathway in human

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Case Study

- Metabolite Radio-profiling and Identification of [¹⁴C]Compound A Following a Single Intragastric Administration of 3 mg/100 µCi/kg of [¹⁴C]Compound A to Sprague-Dawley Rats
  
  [¹⁴C]Compound A was intragastric dosed to rats (3 mg /100 µCi/kg). Rat plasma, urine, feces, and bile samples were collected and pooled by AUC/equal volume/equal proportion for metabolite profiling and characterization. Radiolabeled metabolite profiles of rat plasma, bile, urine and feces samples were determined using LC coupled with on-line or off-line radioactivity monitor (LC-RAM) and structures of detected metabolites were characterized by LC coupled with high-resolution mass spectrometry (LC-RAM/HRMS). The Radio-Chromatograms of 0-72h bile was shown in the Figure.

Experience

15+

Years of experience in radiolabeled MetID studies
500+

Radiolabeled rodent and large animal ADME studies

Instruments

- Liquid Scintillation Counter
- β-RAM Online Radioactivity Detector
- β-counter Solid Scintillation Counter
- ARC Online Radioactivity Detector
- High-Resolution MS

FAQs

What are the advantages of radiolabeled metabolite identification?

Radioactive tracer technology can eliminate the interference from matrix and effectively track the metabolism, distribution, and excretion of drugs in the body. Through the radioactive metabolite profile, we can clearly and accurately understand the number of major metabolites and the proportion of each metabolite, and more accurately determine whether there are major metabolites in circulation that exceed 10% of drug-related substances, and provide a basis for further evaluation of the safety of major metabolites in human plasma. In addition to advantages in tracing, the use of the [¹⁴C] isotope also facilitates the identification of metabolites and a more accurate interpretation of their structure.
How do you perform the radiolabeled metabolite identification?

The samples with low radioactivity intensity were separated by high performance liquid chromatography (HPLC), and the fraction was collected into a LunaPlateTM-96-well plate using Fraction Collector, followed by drying with a SpeedVac system. The dried 96-well plates were measured by Solid Scintillation (Microbeta or TopCount）to obtain offline radio-profiles.
The samples with high radioactivity intensity were detected by high performance liquid chromatography with on-line radioactivity detector (ARC or β-RAM) to obtain radio-profiles directly.
LC-RAM/HRMS and LC-HRMS were used for screening and structure elucidation of major metabolites in samples.

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Radiolabeled MetID (Metabolite Profiling and Identification)

Overview

Assays

In vitro MetID for cross-species comparison

MetID in animal circulation

MetID in animal tissues or excreta

MetID in human circulation

MetID in human excreta

Case Study

Experience

Instruments

FAQs

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