Expert-level reference on Antibody-Drug Conjugate (ADC) science and bioanalysis.
Maintained at peer-review publication standard.
Navigation
| # | Section | Core Questions Answered |
|---|
| 01 | Mechanism of Action | How does an ADC kill a tumor cell? What is the bystander effect? |
| 02 | Linker Types | What makes a linker cleavable or stable? How does linker chemistry affect PK? |
| 03 | Payload Types | What cytotoxic warheads are used? What determines potency and selectivity? |
| 04 | Bioanalysis — Non-clinical | Which analytes matter in animal studies? Which assay platforms are used? |
| 05 | Bioanalysis — Clinical | How does bioanalysis evolve from FIH to registrational trials? What does ADA mean for ADCs? |
| 06 | Matrix Effects | How do plasma, serum, blood cells, tissue, and endogenous enzymes affect ADC stability and assay design? |
| 07 | PD Modeling & Dose Projection | How is non-clinical PK/PD data used for human dose projection, toxicity evaluation, and regulatory submissions? |
| 08 | Bilingual Glossary | ADC中英文术语对照表 — complete English ↔ Chinese terminology reference |
| 09 | Regulatory Guidances | Expert synthesis of all key FDA/EMA/ICH guidances and AAPS white papers governing ADC development |
Approved ADCs — Quick Reference
| Brand Name | INN | Target | Linker | Payload | Indication (primary) | Approval |
|---|
| Mylotarg | gemtuzumab ozogamicin | CD33 | Acid-labile hydrazone | Calicheamicin | AML | 2000 (withdrawn 2010, re-approved 2017) |
| Kadcyla | ado-trastuzumab emtansine (T-DM1) | HER2 | Non-cleavable thioether (SMCC) | DM1 | HER2+ breast cancer | 2013 |
| Adcetris | brentuximab vedotin | CD30 | Cleavable Val-Cit dipeptide | MMAE | HL, sALCL | 2011 |
| Polivy | polatuzumab vedotin | CD79b | Cleavable Val-Cit dipeptide | MMAE | DLBCL | 2019 |
| Padcev | enfortumab vedotin | Nectin-4 | Cleavable Val-Cit dipeptide | MMAE | Urothelial carcinoma | 2019 |
| Trodelvy | sacituzumab govitecan | TROP-2 | Cleavable CL2A (pH-sensitive) | SN-38 | TNBC, urothelial | 2020 |
| Enhertu | trastuzumab deruxtecan (T-DXd) | HER2 | Cleavable tetrapeptide (GGFG) | DXd (exatecan) | HER2+ BC, NSCLC, GC | 2019 |
| Zynlonta | loncastuximab tesirine | CD19 | Cleavable Val-Ala dipeptide | SG3199 (PBD dimer) | DLBCL | 2021 |
| Blenrep | belantamab mafodotin | BCMA | Non-cleavable maleimide | MMAF | Multiple myeloma | 2020 |
| Elahere | mirvetuximab soravtansine | FRα | Cleavable sulfo-SPDB | DM4 | Ovarian cancer | 2022 |
| Akalux | cetuximab sarotalocan | EGFR | — | IRDye700DX (photoimmunotherapy) | Head & neck | 2020 (Japan) |
Cross-Cutting Concepts
- DAR (Drug-to-Antibody Ratio): Average payload molecules per antibody. Drives exposure and tolerability. Typical target: DAR 2–4.
- Bystander effect: Membrane-permeable released payload kills neighboring antigen-negative cells — a critical differentiator for heterogeneous tumors.
- Naked antibody: Unconjugated antibody after payload loss in circulation; measured as Total Antibody (TAb).
- Catabolite: Downstream metabolite of an ADC after cellular processing (e.g., lysine-DM1 from Kadcyla).