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Conferences

2025 DMDG | 51st Open Meeting: Shaping the future of DMPK

  • 2 - 4 September 2025

  • Cambridge, England, GB

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The DMDG is excited to announce the title and session synopses for the 51st Open Meeting: Shaping the future of DMPK taking place in Cambridge, UK this September.

WuXi AppTec DMPK will participate in this meeting and deliver a scientific presentation and posters. We look forward to meeting you at DMDG 2025!

Featured Presentations

Radiolabeling Synthesis and ADME Profiling of GLP-1 Analogs: Challenges and Preclinical Insights

GLP-1 receptor agonists, including mono-, dual-, and triple-receptor analogs engineered through sequence and fatty acid chain modifications, have gained significant momentum in treating type 2 diabetes and obesity. Understanding the absorption, distribution, metabolism, and excretion (ADME) of these large peptides (3,000~6,000 Da) necessitates radiolabeling techniques.


14C is the preferred isotope for GLP-1 analogs, consistent with clinical requirements. However, their low administered doses (0.15~3 mg/kg) demand high specific activity (~200 mCi/mmol). Prolonged half-lives further complicate ADME studies: excretion profiling and quantitative whole-body autoradiography (QWBA) often require >30 days of urine, feces, and carcass collection. Metabolite identification in excreta, bile, and plasma is particularly challenging due to catabolic pathways (e.g., β-oxidation of fatty acid moieties) beyond amide hydrolysis.


This presentation will detail:

  1. Radiolabelling synthesis strategies for linear and cyclic GLP-1 peptides.

  2. Complete excretion recovery methodologies in rodents and non-human primates.

  3. Key metabolite profiling/identification of modified amino acids and fatty acid chains, supported by case studies.

Speaker

张玲玲.jpg
​Dr. Lingling Zhang

Dr. Lingling Zhang currently serves as the director of the DMPK Department of WuXi AppTec, focusing on radiolabeled synthesis and the ADME field to aid the development of new drug candidates, involving small molecules, peptides, ADCs, and Oligos. Dr. Zhang has over 10 years of experience in industry and has supported the approval of dozens of new drugs. Dr. Zhang has authored 9 patents and 5 peer-reviewed publications and has been a participant in the Human Radiolabeled Mass Balance Guidance of NMPA.

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Our posters

Other Resources

  • Our posters
  • Other Resources
    • The Application of Bile Duct Cannulation Animal Models in Radiolabeled Preclinical ADME Studies

      Radiolabeled absorption, distribution, metabolism, and excretion (ADME) studies in preclinical species (rodent and large animal) generate comprehensive quantitative profiles of drug disposition, delineating metabolic pathways and excretion patterns across plasma, bile, urine, and faeces. As a critical methodology of excretion characterisation, bile duct cannulation (BDC) studies utilise surgical cannulation models to quantify biliary elimination (expressed as % of administered dose) and achieve three key objectives: Mechanistic confirmation of enterohepatic recirculation pathways; Structural elucidation of major biliary metabolites; Bioavailability assessment through urinary and biliary excretion data.

    • Evaluation of the Safety and Cross-Species Tolerability of Solutol HS 15 via Intravenous Administration in Various Animals

      This study aimed to explore concentration-dependent safety limits and evaluate the risk of combined solvent use via intravenous administration of Solutol HS 15 in Beagle dogs. Additionally, we assessed tolerability differences across species, including mini-pigs, cynomolgus monkeys, and Dutch belted rabbits, to inform species-appropriate formulation design.

    • Bioanalytical Strategy for Antibody-Drug Conjugates (ADCs) Based on an Integrated Mass Spectrometry Bioanalytical Platform

      In this study, we summarised a comprehensive bioanalytical strategy of ADCs based on mass spectrometry platforms, including tandem mass spectrometry (MS/MS) and high-resolution mass spectrometry (HRMS). Including measurement for total antibody, conjugated antibody, free payload, conjugated payload, total payload, drug-to-antibody ratio (DAR), and biotransformation. A deep understanding of these contents is key to characterising ADC behaviour through drug discovery to development stages.

    • Evaluation of Clearance Prediction Methods for Vepdegestrant (ARV-471) Using PBPK Modelling: Insights into PROTAC Clinical Pharmacokinetics

      Recently, vepdegestrant (ARV-471), an orally bioavailable Proteolysis-targeting chimaeras (PROTACs, proteolysis-targeting chimaeras) targeting the estrogen receptor (ER, estrogen receptor), was submitted as a New Drug Application (NDA, New Drug Application) to the U.S. Food and Drug Administration (FDA, Food and Drug Administration) for the treatment of ESR1-mutated (Estrogen Receptor 1-mutated), ER+ (Estrogen Receptor-positive), HER2- (Human Epidermal Growth Factor Receptor 2-negative) advanced or metastatic breast cancer. This submission represents a significant milestone, as ARV-471 may become the first FDA-approved PROTAC degrader, highlighting the growing clinical potential of PROTAC technology.

    • Optimisation of an In Vitro Plated Monkey Hepatocyte Model and Comparative Metabolite Profiling of a GalNAc-Conjugated siRNA, siRNA01, in Monkey Liver Homogenate and Hepatocytes

      In this study, the culture conditions for plated monkey hepatocytes were optimised by adjusting cell density and evaluating different lots of hepatocytes from multiple vendors. After optimising conditions, the expected metabolism profile for our model compound, siRNA01, a commercially available GalNAc-conjugated siRNA, was obtained. Furthermore, comparative metabolite profiling of siRNA01 in optimised plated monkey hepatocytes and monkey liver homogenate revealed highly similar profiles.

    • Optimising Oral Drug Delivery: A Novel Multi-Segment Intestinal Cannulation Approach in Beagle Dogs

      The discovery and development of oral drug candidates during the preclinical stage require a thorough understanding of how various segments of the gastrointestinal (GI) tract influence absorption. Both small molecule compounds and biologics face significant challenges, such as poor solubility, chemical and enzymatic degradation, variable permeability, first-pass metabolism, efflux mechanisms, immunogenicity, and stability issues. Traditional animal models, including single-segment perfusion in rodents, are limited by their inability to compare across intestinal segments and the non-reusability of animals.

    • Biomimetic Chromatography Method to Estimate Human Plasma Protein Binding for Peptides

      Peptides, as targeted therapeutics for metabolic disorders and cancer, have profoundly reshaped our modern pharmaceutical industry. Understanding the pharmacokinetic behaviour and pharmacological/toxicological effects of these drugs critically depends on determining the unbound fraction (fu) in plasma. However, inherent challenges such as stability and non-specific binding issues make obtaining reliable fu values particularly difficult for peptides using traditional plasma protein binding (PPB) experiments, such as equilibrium dialysis, ultracentrifugation, or ultrafiltration. To address these issues, this study developed a biomimetic chromatography method to evaluate human plasma protein binding. 

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