4th-6th March 2019


Day One
Tuesday 5th March 2019

Day Two
Wednesday 6th March 2019

Chair’s Opening Remarks

  • Alain Beck Senior Director, Biologics CMC and developability, Pierre Fabre Laboratories

Revealing Next Generation ADC Technologies

Exploring Site Directed Mutations on Native Antibodies to Allow Payload Conjugation

  • Pedro Cal Post-Doctoral Fellow, University of Cambridge


  • Novel reagents for protein modification
  • Site-selective lysine and cysteine modifications
  • Protein microenvironment importance for bioconjugation.

Cytotoxic & Steroid ADCs for Cancer & Inflammation

  • William Olson Vice President, Therapeutic Proteins, Regeneron Pharmaceuticals


• Cytotoxic ADCs targeting tubulin
• Non-cytotoxic ADCs targeting the glucocorticoid receptor
• Approaches to discovery and validation of targets for ADC therapy

Morning Refreshments & Networking

Exploring New Frontiers in ADC Research

11.00 Molecular Features of an Antibody-antibiotic Conjugate Targeting Staphylococcus Aureus

  • MOA and POC of an anti-S. aureus antibody-antibiotic conjugate (AAC) combining an anti-S. aureus antibody with an antibiotic and a cleavable linker
  • Correlations between intracellular antibiotic activity and anti-S. aureus AAC potency
  • Modulation of anti-S. aureus AAC potency

Wouter Hazenbos, Scientist, Department of Infectious Diseases, Genentech

11.30 Betalutin® - An Antibody- radionuclide-conjugate (ARC) for the Treatment of Relapsed Non-Hodgkin’s Lymphoma

Betalutin® – An Antibody-radionuclide-conjugate (ARC) for the Treatment of Relapsed Non-Hodgkin’s Lymphoma

  • Introduction to Nordic Nanovector ASA
  • Introduction to Betalutin
  • Summary of clinical data and development program of Betalutin

Dr. Reza Safaei, Head, Medical Affairs, Nordic Nanovector

12:00 BT5528: A Bicycle Toxin Conjugate Targeting EphA2 for the Treatment of Solid Tumours

  • BT5528 comprises a Bicyclic peptide binder of EphA2 linked to the cleavable linker & toxin vcMMAE
  • The small size and hydrophilicity of Bicycle Toxin Conjugates offers rapid and complete tumour penetration, efficient delivery of toxin and rapid renal elimination of unbound drug
  • BT5528 offers profound efficacy across a range of EphA2- expressing tumour models, including large heterogeneous PDX models, without the profound toxicity seen with previous antibody conjugate approaches

Gavin Bennet, Director, Project Leader, Bicycle Therapeutics

Clinical Considerations for Developing Disease Modifying ADCs

11.00 Applying Mechanistic Models to Better Predict Clinical Pharmacology of ADCs

  • ABBV-085 in Sarcoma
  • LRRC15 target biology
  • ABBV-085 preclinical efficacy and safety
  • Phase 1 design and preliminary findings

James Purcell, Senior Scientist & Program Director, Oncology Discovery, AbbVie

11.30 Challenges & Opportunities in Developing ADCs

  • Main challenge in developing ADCs is the therapeutic index
  • Innovative clinical trials to decrease toxicity and improve efficacy
  • Patient selection strategies that incorporate genomic markers of ADC sensitivity
  • Novel combination approaches that increase the activity of the ADC and reduce toxicities

Steve Coats, Vice President, Research & Development, MedImmune

12.00 MORAb-202 – a Potent Human Folate Receptor Alpha-Targeting ADC that Utilises the Anti-tubulin Agent Eribulin as Payload

  • MORAb-202 is a cleavable cysteine-based conjugate of farletuzumab, a humanised antihuman folate receptor alpha antibody in Phase II clinical trials,
    and eribulin, an anti-tubulin agent approved for the treatment of certain metastatic breast cancers
  • MORAb-202 exhibits clear bystander effects on the tumour microenvironment, in addition to its direct cytotoxic effects on folate receptor-positive tumour cells
  • MORAb-202 is currently in a Phase I clinical trial in Japan

Earl Albone, Director, Biochemistry Discovery, Morphotek

Manufacturing Next Generation ADC Technologies: Optimising Processes & Technical Operations

11.00 Structural & Dynamic Reporters of the Aggregation of ADCs

  • In ADCs, the drug and the distribution of its attachment points to the antibody affect the folding, the stability, and interactions between these macromolecules
  • Advanced characterization techniques applied to study the onset of aggregation
  • Using these could help deciphering whether non-specific interaction is important or whether a subpopulation in the formulation is more prone to aggregation
  • Guiding CMC development for better stability and allow for elaborating a formulation platform for ADCs

Sylvain Huille, Senior Scientist,BioDevelopment, Sanofi

11.30 Process Understanding and Automated Processing in Development to Ensure First Pass Manufacturing Success of ADCs

  • Studies needed for clinical supplies and for commercial readiness with the goal of providing evidence of process consistency
  • Use of automated systems for gathering information for early phase process transfers to manufacturing
  • DOEs that ensure appropriate ranges are evaluated and ensure deep process understanding

Mary Robinette, Principal Project Engineer, Merck

12.00 Stability Investigations on ADCs Model Compounds with Defined Hydrophobicity Levels

  • Identifying representative model compounds for formulation and process development studies
  • Property alterations upon conjugation
  • Impact of payload hydrophobicity on stability and stress tolerance

Matthias Winzer, Associate Director, Parenteral Development, Merck KGaA

Lunch & Networking

Optimising Payload-Linker Combinations

13.30 Novel Linker Payload Combination

  • Discovering novel payloads and assessing various combinations of linkers and payloads
  • Evaluating these combinations ensuring optimised affinity
  • Reviewing combinations and how they can be improved to increase therapeutic window

Yiqing Feng, Senior Research Fellow, Eli Lilly

14.00 Exploring a Next Generation ADC: TRPH-CD22

  • TRPH-222 is a CD22-directed ADC, constructed via a novel, site-specific (SMARTagTM) conjugation approach, resulting in highly controlled and reproducible drug loading
  • The molecule was very well tolerated in IND-enabling studies in the non-human primate at repeat doses up to 50 mg/kg administered IV, and demonstrated
    superior pharmacokinetics relative to ADCs using conventional conjugation approaches
  • TRPH-222 is currently being studied in relapsed and/or refractory B-cell lymphoma patients in a phase 1 clinical trial (NCT03682796)

Nancy Levin, Vice President Development, Triphase

Bullseye: Validating Novel Formats, Engineering Antibodies & Discovering Appropriate Targets

13.30 Dosing Optimisation & Mechanism Assessment of CD33- ADC Antibodies in AML Disease Models: Translating Preclinical Science to the Clinic

  • Exploring the dosing options of CD33-ADC preclinical models
  • Ensuring smooth transition into the clinic
  • Assessing the mechanism of action of CD33-ADC

Cathy Zhang, Senior Principal Scientist, Pfizer

14.00 Vicinium: An anti-EpCAM scFV/Pseudomonas Exotoxin A Fusion Protein in Advanced Development for the Treatment of Non-Muscle Invasive Bladder Cancer

  • Vicinium has been designed for local-regional treatment of cancer, providing the opportunity to both localize the therapeutic agent at
    the site of disease and reduce the potential for systemic toxicity
  • Ongoing results of the phase 3 VISTA trial evaluating Vicinium in the setting of non-muscle invasive bladder cancer will be presented
  • The ability of Vicinium to mediate immunogenic cell death potentially initiating host anti-tumor immune responses will be discussed

Gregory Adams, Chief Scientific Officer, Sesen Bio

Simplifying Process Development to Efficiently Manufacture ADCs

13.30 Scalable Synthesis of of Aza-Cryptophycin, a highly Active Payload for ADCs

  • Evaluated as stand alone agent, but dropped due to tox reason in 2002, Cryptophycin regains attention as highly potent payload for ADCs
  • Synthesis of Cryptophycin and its aza analogues have been hampered by poor overall yield
  • We will describe in this talk a highly efficient synthesis that provided access to multigram of the compound, in order to provide material for tox evaluation
  • In particular, this talk will demonstrate an efficient answer to the 20 + year-old problem of the  epoxide introduction

Antony Bigot, Section Head, Sanofi

14.00 Strategies for Scaling-Up ADC Payload Production

  • An overview of what to consider when scaling-up the synthesis of ADC payloads
  • The importance of route design linker to safety and cost
  • Case study 1: Tubulysin
  • Case study 2: Tesirine

William Goundry, Associate Principal Scientist, AstraZeneca

Afternoon Refreshments & Networking

Driving Synergy: Assessing ADCs as a Combination Therapies

Review of the ADC Clinical Pipeline


• Update on the key movements in the clinic
• Insight into the rapidly evolving pipeline
• Analysis of novel clinical ADCs

Single-Cell Pharmacokinetics & Pharmacodynamics of Biologics: Designing Effective Antibody Drug Conjugates & Checkpoint Inhibitors


• Biologics have unique distribution in the body that can impede or enhance efficacy depending on the particular drug and target
• Measuring the single-cell delivery and efficacy of these agents can help design more effective therapeutics and delivery strategies
• The local degradation of these agents in the tumour microenvironment can result in counter-intuitive results, but these can be leveraged to improve therapy as illustrated with several examples

Chair’s Closing Remarks

  • Alain Beck Senior Director, Biologics CMC and developability, Pierre Fabre Laboratories