Antibody–Drug Conjugates (ADCs) are a class of targeted cancer therapies composed of a potent cytotoxic payload chemically linked to a monoclonal antibody (mAb) via a specialized chemical linker. This design enables the precise delivery of the drug to tumor cells, helping to minimize systemic toxicity and enhance treatment efficacy.
The history of ADC development began with the first clinical trial in 1983, in which an anti-carcinoembryonic antigen antibody conjugated to vindesine was tested in patients with advanced metastatic carcinomas. In 2000, the U.S. FDA approved gemtuzumab ozogamicin (Mylotarg) as the first ADC on the market, targeting CD33-positive acute myeloid leukemia. As of November 2025, there are 20 ADCs approved globally for the treatment of various hematologic malignancies and solid tumors (see table below).
|
ADC Name |
Company |
Payload |
Linker |
Indication |
Antibody |
DAR |
Target Antigen |
Approval year |
|
Becotatug vedotin 美佑恒® |
Lepu Biopharma |
MMAE |
MC-Val-Cit-PAB |
Recurrent/metastatic nasopharyngeal carcinoma |
Human IgG1 |
4 |
EGFR |
2025 (NMPA) |
|
Trastuzumab botidotin 舒泰莱® |
Kelun Biotech |
Duostatin 5 |
Val-Cit |
HER2-positive breast cancer |
Humanized IgG1 |
2 |
HER2 |
2025 (NMPA) |
|
Trastuzumab rezetecan 爱维达® |
Hengrui Pharma |
SHR9265 |
MC-Gly-Gly-Phe-Gly |
HER2-mutated non-small cell lung cancer |
Humanized IgG1 |
6 |
HER2 |
2025 (NMPA) |
|
Telisotuzumab vedotin Emrelis® |
Abbvie |
MMAE |
MC-Val-Cit-PAB |
c-Met-overexpressing non-small cell lung cancer |
Humanized IgG1 |
3 |
c-Met |
2025 |
|
Datopotamab deruxtecan Datroway® |
Daiichi Sankyo and AstraZeneca |
Deruxtecan |
MC-Gly-Gly-Phe-Gly |
HR+/HER2− metastatic breast cancer |
Humanized IgG1 |
4 |
Trop-2 |
2025 (FDA) |
|
Sacituzumab tirumotecan 佳泰莱® |
Kelun biotech |
KL610023 |
CL2A |
TROP2-positive solid tumors |
Human IgG1 |
7.4 |
Trop-2 |
2024 (NMPA) |
|
Mirvetuximab soravtansine Elahere® |
Abbvie |
DM4 |
Sulfo-SPDB |
Platinum-resistant ovarian cancer |
Human IgG1 |
3.4 |
Folate receptor α |
2022 (FDA) |
|
Tisotumab vedotin Tivdak® |
Genmab/Seagen |
MMAE |
MC-Val-Cit-PAB |
Recurrent/metastatic cervical cancer |
Humanized IgG1 |
4 |
Tissue factor |
2021 (FDA) |
|
Disitamab Vedotin 爱地希® |
RemeGen |
MMAE |
MC-Val-Cit-PAB |
HER2-positive cervical cancer |
Humanized IgG1 |
4 |
HER2 |
2021 (NMPA) |
|
Loncastuximab tesirine Zynlonta® |
ADC Therapeutics |
PBD dimer |
Mal-Amide-PEG8-Val-Cit-PAB |
Large B-cell lymphoma |
Humanized IgG1 |
2.3 |
SG3199/CD19 |
2021 (FDA) |
|
Cetuximab sarotalocan Akalux® |
Rakuten medical |
Photosensitizer IR700 |
N/A |
Advanced head and neck cancer |
Chimeric IgG1 |
1.3-3.8 |
EGFR |
2020 (PMDA) |
|
Belantamab mafodotin Blenrep® |
GSK |
MMAF |
Non-cleavable |
relapsed and refractory multiple myeloma |
Humanized IgG1 |
4 |
BCMA |
2020 (FDA) 2025 reapproval (FDA) |
|
Sacituzumab govitecan Trodelvy® |
Gilead |
SN-38 |
CL2A |
Triple-negative breast cancer (TNBC), HR+/HER2− breast cancer |
Humanized IgG1 |
7.6 |
Trop 2 |
2020 (FDA) |
|
Trastuzumab deruxtecan Enhertu® |
AstraZeneca and Daiichi Sankyo |
Deruxtecan (DXd) |
MC-Gly-Gly-Phe-Gly |
HER2-positive breast, gastric, and lung cancers |
Humanized IgG1 |
8 |
HER2 |
2019 (FDA) |
|
Enfortumab vedotin Padcev® |
Genmab /Seagen |
MMAE |
MC-Val-Cit-PAB |
Urothelial cancer |
Human IgG1 |
3.8 |
Nectin-4 |
2019 (FDA) |
|
Polatuzumab vedotin Polivy® |
Genetech /Roche |
MMAE |
MC-Val-Cit-PAB |
diffuse large B-cell lymphoma |
Humanized IgG1 |
3.5 |
CD79 |
2019 (FDA) |
|
Inotuzumab ozogamicin Besponsa® |
Pfizer |
Calicheamicin |
Acid-labile (hydrazone) |
Relapsed/refractory B-cell precursor acute lymphoblastic leukemia |
Humanized IgG4 |
6 |
CD22 |
2017 (FDA) |
|
Trastuzumab emtansine Kadcyla® |
Roche |
DM1 |
Non-cleavable MCC |
HER2-positive breastcancer |
Humanized IgG1 |
3.5 |
HER2 |
2013 (FDA) |
|
Brentuximab vedotin Adcetris®
|
Seagen /Takeda |
MMAE |
MC-Val-Cit-PAB |
relapsed or refractory Hodgkin lymphoma (HL) and systemic anaplastic large cell lymphoma |
Chimeric IgG1 |
4 |
CD30 |
2011 (FDA) |
|
Gemtuzumab ozogamicin Mylotarg® |
Pfizer |
Calicheamicin |
Acid-labile (hydrazone) |
Acute myeloid leukemia |
Humanized IgG4 |
2-3 |
CD33 |
2000 (FDA) 2017 reapproval (FDA) |
Among the key components of ADCs, the linker plays a pivotal role not only in attaching the payload to the antibody, but also in determining the stability in circulation, drug release profile, and overall therapeutic index. Advances in linker chemistry—such as cleavable vs. non-cleavable designs, site-specific conjugation strategies, and hydrophilic masking groups—have been instrumental in overcoming early challenges related to toxicity and efficacy, and continue to drive innovation in the next-generation ADC platforms.
As a leading bioconjugation linker supplier, PrecisePEG offers a comprehensive portfolio of customized and off-the-shelf ADC linkers to support cutting-edge therapeutic development and translational research.
References:
1. Food and Drug Administration Website. Drugs@FDA: FDA-Approved Drugs. Accessed Nov. 2025.
2. ADC Database (ADCdb). https://adcdb.idrblab.net/. Accessed Nov. 2025.