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An antibody-drug conjugate is an antibody that homes to a protein on the tumour cell, is swallowed, and releases a chemotherapy payload inside it. That widens chemotherapy's safe dose window about a hundredfold, which is why payloads too toxic to give alone can be used, though lung inflammation, neutropenia and eye toxicity from the payload still occur.
Fifteen-plus ADCs are approved. Components: antibody (target, internalisation), linker (cleavable or not, stability), payload (tubulin inhibitors MMAE/DM1; TOP1 inhibitors DXd/SN-38; PBD dimers; calicheamicin), and drug-to-antibody ratio (DAR). Third-generation ADCs (T-DXd, sacituzumab govitecan, Dato-DXd, enfortumab vedotin) with high DAR and bystander-capable TOP1 payloads changed breast, lung, and bladder cancer. Key issues: target heterogeneity, payload cross-resistance, ILD and ocular toxicities, and sequencing multiple ADCs.
Antigen binding → receptor-mediated endocytosis → lysosomal degradation or linker cleavage → payload release → tumour cell death and, with permeable payloads, killing of neighbouring antigen-negative cells.
Dependencies are what this technology cannot be delivered without: manufacturing steps, instruments, software, upstream methods. See its full chain on the map.
Anetumab ravtansine was the first antibody-drug conjugate tested in a randomised trial in mesothelioma, aimed at the mesothelin protein that nearly all mesotheliomas carry; it was no better than vinorelbine chemotherapy as second-line treatment, and is now being tried with pembrolizumab.
ARX788 is a HER2 ADC with a precisely placed, non-cleavable payload that beat lapatinib-capecitabine in China and showed activity in brain metastases.
A myeloma ADC that was withdrawn in 2022 then came back in 2025 after strong trials in earlier lines.
BIO-106 is an experimental antibody-drug conjugate from BiOneCure Therapeutics in phase 2 trials, aimed at TROP2.
The ADC that made the modern field credible (2011), for Hodgkin lymphoma and CD30+ lymphomas.
Datopotamab deruxtecan (Datroway) is the second TROP2 ADC and shares Enhertu's payload. In 2026 it became a first-line option for triple-negative breast cancer patients who cannot receive immunotherapy.
Depatuxizumab mafodotin carried a cell-killing payload to glioblastomas with extra copies of the EGFR gene. It caused serious eye problems and, in the phase 3 INTELLANCE-1 trial, did not help patients live longer, so development stopped in 2019.
Disitamab vedotin is a Chinese HER2 ADC approved for gastric and bladder cancer, now in global trials with Pfizer.
Enfortumab vedotin is an ADC against Nectin-4 that, combined with pembrolizumab, nearly doubled survival in advanced bladder cancer.
Gemtuzumab ozogamicin (Mylotarg) is an anti-CD33 antibody linked to the DNA-cutting payload calicheamicin, the first ADC approved, in 2000 for relapsed acute myeloid leukaemia. An unstable linker and no benefit in a confirmatory trial led to withdrawal in 2010; it returned in 2017 at a lower fractionated dose, with liver toxicity, including veno-occlusive disease, its defining risk.
Ifinatamab deruxtecan is a B7-H3 ADC showing some of the best response rates ever seen in relapsed small-cell lung cancer.
Inotuzumab ozogamicin is an antibody carrying a DNA-cutting toxin to CD22 on leukaemia cells. It gets far more relapsed ALL patients into remission than chemotherapy and bridges them to transplant.
Izalontamab brengitecan is the first bispecific ADC to succeed in a phase 3 trial, hitting two growth receptors at once in triple-negative breast cancer.
Loncastuximab tesirine (Zynlonta) is a CD19 ADC with a DNA-crosslinking payload for relapsed large B-cell lymphoma.
A folate-receptor ADC designed to work across low and high receptor levels, in a pivotal ovarian cancer trial.
Mirvetuximab soravtansine (Elahere) is the first ADC for ovarian cancer, for tumours with high folate receptor alpha.
An immunotoxin for hairy cell leukaemia that produced lasting remissions in relapsed patients but was withdrawn from sale in 2023 for commercial reasons.
A HER3-directed ADC with Enhertu's payload, active in lung and all subtypes of breast cancer, but with a bumpy regulatory road.
Pivekimab sunirine is an antibody-drug conjugate against CD123, approved in 2026 for blastic plasmacytoid dendritic cell neoplasm as the second targeted drug for this rare cancer.
Polatuzumab vedotin is an ADC against CD79b that, swapped into the classic R-CHOP regimen, became the first improvement on frontline lymphoma therapy in twenty years.
Puxitatug samrotecan is a B7-H4 ADC targeting a checkpoint-like protein enriched in breast, ovarian, and endometrial cancers.
Raludotatug deruxtecan is a CDH6 ADC in phase 3 for platinum-resistant ovarian cancer.
Rinatabart sesutecan is a next-generation folate-receptor ADC with a topoisomerase payload that responds in both ovarian and endometrial cancer regardless of receptor level.
Rovalpituzumab tesirine (Rova-T) was the first drug against DLL3 in small-cell lung cancer. AbbVie bought it for $5.8B and abandoned it after two failed phase 3 trials. The target later worked with a different weapon.
The first TROP2-targeted ADC. It delivers a strong chemotherapy directly to breast and bladder cancer cells and is now a first-line option in triple-negative breast cancer.
Sacituzumab tirumotecan is Kelun-Biotech's TROP2 ADC, approved in China in 2024 for pretreated triple-negative breast cancer and then EGFR-mutant lung cancer. Merck holds rights outside Greater China and runs the TroFuse programme of more than ten phase 3 trials across breast, lung, endometrial and cervical cancer; in the US it holds a priority voucher but no approval yet.
Sonesitatug vedotin is a Claudin 18.2 ADC in phase 3 for gastric cancer, licensed by AstraZeneca from KYM Biosciences.
Telisotuzumab vedotin (Emrelis) is the first c-MET-directed ADC, approved in 2025 for lung cancer with high c-MET protein.
Tisotumab vedotin is an ADC against tissue factor, the first to show a survival benefit in recurrent cervical cancer.
SystImmune's HER2 ADC, sharing its payload with iza-bren, now in a 1,450-patient trial to replace Kadcyla after surgery.
Trastuzumab deruxtecan (Enhertu) is the most successful ADC ever. It redefined HER2 by working in tumours with only tiny amounts of the protein, and in 2026 moved into early-stage breast cancer.
A HER2 ADC with a DNA-alkylating payload that beat chemotherapy in a phase 3 trial yet never reached the market, because eye and lung toxicity and a stronger rival arrived first.
Trastuzumab emtansine (Kadcyla, T-DM1) was the first ADC for a solid tumour (2013). It is still standard after surgery for HER2+ breast cancer patients whose tumour did not fully respond to pre-surgery treatment.
Trastuzumab pamirtecan is DualityBio and BioNTech's HER2 antibody-drug conjugate, in phase 3 trials in breast cancers with high and with modest HER2 expression and in HER2-expressing endometrial cancer.
Hengrui's HER2 ADC, approved in China for lung cancer and showing Enhertu-scale results in breast cancer, part of a wave of Chinese ADCs heading for global trials.
Tusamitamab ravtansine was Sanofi's ADC against the classic CEA tumour marker, stopped for futility in lung cancer in 2023.
Zanidatamab zovodotin joined the two-armed HER2 antibody zanidatamab to a cell-killing payload. It was tested in early trials in HER2-expressing cancers; the plain antibody went on to approval, the conjugate did not progress beyond phase 1.
Zilovertamab vedotin is a ROR1-directed ADC in phase 3 for large B-cell lymphoma.
The first-line overall survival result that made an antibody-drug conjugate the standard for PD-L1-negative or immunotherapy-ineligible metastatic triple-negative disease, and the reason the sequencing question (which TROP2 drug first, what after it) is now urgent.
An option with a demonstrated survival benefit for transplant-ineligible relapsed diffuse large B-cell lymphoma, a group for whom very little has ever shown one. The fatal adverse event imbalance belongs in the conversation alongside the survival figure.
The evidence behind the United States approval of brentuximab vedotin with lenalidomide and a rituximab product for relapsed or refractory diffuse large B-cell lymphoma after two or more lines in patients not eligible for an autologous transplant or CAR-T. It is also the first demonstration that a CD30-directed conjugate helps in a disease where CD30 expression is variable.
Patients with hormone-receptor-positive metastatic breast cancer that has stopped responding to endocrine therapy can be offered trastuzumab deruxtecan as their first chemotherapy-type treatment if the tumour shows any HER2 staining, rather than waiting until after conventional chemotherapy. Whether to use it before or after chemotherapy is now a choice, since overall survival was not shown to differ and the drug carries a risk of lung inflammation.
Almost every patient newly diagnosed with advanced bladder or urothelial cancer should now be offered enfortumab vedotin plus pembrolizumab rather than chemotherapy, with median survival extended from about 16 months to over two and a half years. Neuropathy and skin toxicity need monitoring and dose adjustment, and patients with severe diabetes or pre-existing neuropathy need care. Platinum chemotherapy remains an option for those who cannot receive the combination.
For hormone-receptor-positive metastatic breast cancer that has already had chemotherapy, Dato-DXd controls the disease for longer with fewer severe side effects than chemotherapy, but does not help patients live longer, so it is not a standard option here. The result is a reminder that progression-free survival is a surrogate; regulators and clinicians should wait for survival data before adopting an ADC in a setting where later therapies are effective.
For HER2-positive metastatic breast cancer that has progressed after trastuzumab and a taxane, trastuzumab deruxtecan is now the standard second-line treatment and T-DM1 has moved later in the sequence. The benefit is large enough that ADC design, not just the target, is understood to be what matters. Patients need lung monitoring because of the risk of pneumonitis.
Patients whose breast cancer was previously called HER2-negative may now be eligible for an effective HER2-directed drug if their tumour has even low-level HER2 staining, so pathology reports must now distinguish HER2-low (1+ or 2+/ISH-negative) from HER2-zero. This applies to metastatic disease after at least one line of chemotherapy; it does not mean these patients benefit from trastuzumab or other older HER2 drugs.
Query for this technology: (TITLE:"antibody-drug conjugate" OR ABSTRACT:"antibody-drug conjugate" OR TITLE:"antibody drug conjugate" OR ABSTRACT:"antibody drug conjugate" OR TITLE:"antibody-drug conjugates" OR ABSTRACT:"antibody-drug conjugates") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Antibody-drug conjugate (ADC), not a curated reading list.
Shares A Study of Ifinatamab Deruxtecan in Pediatric Participants With Relapsed or Refractory Solid Tumors (MK-9999-01D/LIGHTBEAM-U01), A Study of Patritumab Deruxtecan in Pediatric Participants With Relapsed or Refractory Solid Tumors (MK-9999-01C/LIGHTBEAM-U01), A Study of Raludotatug Deruxtecan (R-DXd) in People With Gastrointestinal Cancers (MK-5909-005), A Study of Raludotatug Deruxtecan in Participants With Advanced/Metastatic Solid Tumors (REJOICE-PanTumor01).
Shares A Study of Ifinatamab Deruxtecan in Pediatric Participants With Relapsed or Refractory Solid Tumors (MK-9999-01D/LIGHTBEAM-U01), A Study of Patritumab Deruxtecan in Pediatric Participants With Relapsed or Refractory Solid Tumors (MK-9999-01C/LIGHTBEAM-U01), A Study of Raludotatug Deruxtecan (R-DXd) in People With Gastrointestinal Cancers (MK-5909-005), A Study of Raludotatug Deruxtecan in Participants With Advanced/Metastatic Solid Tumors (REJOICE-PanTumor01).
Shares A Study of T-DXd for the Treatment of Solid Tumors Harboring HER2 Activating Mutations, A Study of Trastuzumab Deruxtecan in People With Non-Small Cell Lung Cancer, Puxitatug Samrotecan (AZD8205) Monotherapy vs Chemotherapy in B7-H4-selected Endometrial Cancer (Bluestar-Endometrial01), Moxetumomab pasudotox.
Shares Circulating Tumor DNA to Guide Changes in Standard of Care Chemotherapy, Multicenter, Phase II Clinical Study of Sacituzumab Tirumotecan (Sac-TMT) in Combination With KL-A167 for Neoadjuvant Treatment of Triple-Negative Breast Cancer, NeoAdjuvant Therapy Comparing Sacituzumab Govitecan+Pembrolizumab vs. SoC Chemotherapy in Clinical Stage II-III, Triple-negative Early Breast Cancer, PREDICT-RD: ctDNA Surveillance in TNBC With Residual Disease.
Shares A Study in Patients With Advanced Cancers, A Prospective, Single-center, Phase II Study of Sacituzumab Tirumotecan in Combination With Pembrolizumab for Neoadjuvant Treatment of Triple-Negative Breast Ca, NeoAdj. Therapy Comparing Sacituzumab Govitecan (SG) vs. SG+Pembrolizumab in Low-risk, Triple-neg. EBC (ADAPT-TN-III), Sacituzumab Govitecan +/- Pembrolizumab in Metastatic TNBC.
Shares Circulating Tumor DNA to Guide Changes in Standard of Care Chemotherapy, Sacituzumab Tirumotecan Plus Tagitanlimab in Previously Treated Locally Advanced or Metastatic Triple Negative Breast Cancer, DATO-BASE: DATOpotamab-deruxtecan for Breast Cancer Brain metAstaSEs, First-Line Sacituzumab Govitecan in Advanced Untreated Triple-Negative Breast Cancer Patients..
Shares A Study in Patients With Advanced Cancers, Find the lowest effective doses of both drugs in a combination, not the highest tolerated, Retire the 3+3: model-based dose finding that counts late and chronic side effects, A Prospective, Single-center, Phase II Study of Sacituzumab Tirumotecan in Combination With Pembrolizumab for Neoadjuvant Treatment of Triple-Negative Breast Ca.