Few contract research laboratories maintain the rigorous cGMP-compliant environment required to produce certified radiolabeled APIs suitable for human clinical trials. While CMC requirements for traditional “cold” CTMs are well understood, successfully incorporating “hot” or “blended” versions of drugs into your development plan requires specialized expertise.
Clinical studies conducted using 14C-radiolabeled clinical trial materials (CTMs) result in detailed DMPK, ADME and mass balance information, providing great insight into a drug’s behavior in vivo. Before proceeding with the synthesis, you must first determine the optimal position of the radiolabel in the test substance.
Ideally, the 14C-label should be incorporated in the drug molecule at a metabolically stable site, so that it will be conserved in the degradation products observed in plasma, tissue, and/or excreta. Incorporating the radioactive isotope into your CTM sometimes involves developing a new synthetic pathway. EAG has the expertise to advise on preferred position(s) of the radiolabel and suggest synthetic pathways.
Effective, timely, and quality production of radiolabeled CTMs requires radiochemistry expertise and rigorous cGMP-compliant facilities, processes and systems. Once synthesized, radiolabeled drugs often exhibit different stability and impurity profiles; and to ensure the validity of studies, these variances must be understood. These and other issues present special challenges related to cGMP compliance and patient safety during the clinical trial.
EAG maintains four Class 10,000 cGMP Synthesis suites, a dedicated Quality Assurance staff and a group of analytical chemists with years of experience supporting labeled isotope studies. This unique capability complements in-house drug metabolism and impurity ID expertise and streamlines project management.
Let us show you how to expedite the path to your next development milestone using expertly radiolabeled compounds.
GMP Radiolabeling Clinical Support
- Human ADME/Mass Balance under cGMP
- GMP API suitable for early clinical trials, including Phase 0 microdosing studies
- Lead optimization
- Metabolite identification – Metabolites in Safety Testing (MIST)
- Radiolabeled (14C and 3H) GMP API for early clinical trials
- Analytical support dedicated to synthesis activities
- Method development and early phase validation
- Certificate of analysis generation
EAG possesses deep experience with all types of chemistries: Lithiation, Grignard, epoxidation, nitration, metal catalysis–as well as chiral separation and asymmetric synthesis and all types of compounds, including carbohydrates, amino acids, peptides and steroids.