ADC Drugs by Target in 2026: Full List of 21 Approved Antibody-Drug Conjugates

Antibody-drug conjugates (ADCs) are one of the fastest-growing classes of therapies in precision oncology. In this guide to ADC drugs by target in 2026, we provide a comprehensive overview of approved antibody-drug conjugates and their classification based on tumor targets.

By combining highly potent cytotoxic drugs with monoclonal antibodies, ADCs enable “targeted delivery,” directing drugs specifically to tumor cells while minimizing damage to normal tissues.

With advances in antibody engineering, linker technology, and payload design, ADCs have entered rapid development, with growing clinical efficacy and global approvals.

🚀 As of March 2026, approximately 21 ADC drugs have been approved worldwide, targeting multiple tumor antigens such as HER2, TROP2, CD antigens, EGFR, BCMA, and Nectin-4. These ADC drugs play critical roles in the treatment of breast cancer, lung cancer, lymphoma, urothelial carcinoma, ovarian cancer, and multiple myeloma.

DengYueMed, a global pharmaceutical distributor, provides a systematic overview of these therapies through a structured analysis of ADC drugs by target in 2026.

I. Overview of ADC Drugs

This overview provides a structured understanding of adc drugs by target in 2026, highlighting how different targets correspond to specific therapies.

Their core structure includes:

1. Monoclonal Antibody (Antibody)

Responsible for recognizing specific antigens on tumor cell surfaces, enabling precise targeting.

2. Linker

Connects the antibody to the payload, remaining stable in circulation and releasing the drug inside tumor cells.

3. Cytotoxic Payload (Payload)

Typically consists of highly potent microtubule inhibitors or DNA-damaging agents that kill cancer cells.

The mechanism of action includes:

1. The antibody binds to a tumor-specific antigen
2. The ADC is internalized into tumor cells
3. The linker is cleaved
4. The payload is released, damaging DNA or microtubules and inducing cell death

This mechanism underpins the classification of adc drugs by target in 2026, combining the advantages of targeted therapy and chemotherapy.

II. Global List of Approved ADC Drugs

As of March 2026, approximately 21 ADC drugs have been approved by the U.S. Food and Drug Administration (FDA) and other global regulatory authorities.

Key details are summarized below:

Drug	Brand Name	Company	First Approval	Target	Main Indication
Gemtuzumab ozogamicin	Mylotarg	Pfizer	2000	CD33	Acute Myeloid Leukemia
Brentuximab vedotin	Adcetris	Seagen/Takeda	2011	CD30	Hodgkin Lymphoma
Trastuzumab emtansine	Kadcyla	Roche	2013	HER2	HER2+ Breast Cancer
Inotuzumab ozogamicin	Besponsa	Pfizer	2017	CD22	Acute Lymphoblastic Leukemia
Moxetumomab pasudotox	Lumoxiti	AstraZeneca / MedImmune	2018	CD22	Hairy Cell Leukemia
Polatuzumab vedotin	Polivy	Roche	2019	CD79b	DLBCL
Enfortumab vedotin	Padcev	Astellas/Seagen	2019	Nectin-4	Urothelial Cancer
Trastuzumab deruxtecan	Enhertu	Daiichi Sankyo	2019	HER2	Breast Cancer, Lung Cancer
Sacituzumab govitecan	Trodelvy	Gilead	2020	TROP2	TNBC
Belantamab mafodotin	Blenrep	GSK	2020	BCMA	Multiple Myeloma
Cetuximab sarotalocan	Akalux	Rakuten	2020	EGFR	Head and Neck Cancer
Loncastuximab tesirine	Zynlonta	ADC Therapeutics	2021	CD19	Lymphoma
Disitamab vedotin	Aidixi	RemeGen	2021	HER2	Gastric Cancer
Tisotumab vedotin	Tivdak	Seagen	2021	Tissue Factor	Cervical Cancer
Mirvetuximab soravtansine	Elahere	ImmunoGen	2022	FRα	Ovarian Cancer
Sacituzumab tirumotecan	Jiataile	Kelun-Biotech	2024	TROP2	TNBC, NSCLC
Datopotamab deruxtecan	Datroway	AstraZeneca	2024	TROP2	Breast Cancer
Telisotuzumab vedotin	Emrelis	AbbVie	2025	c-MET	NSCLC
Trastuzumab rezetecan	Aiweida	Hengrui	2025	HER2	NSCLC
Trastuzumab botidotin	Shutailai	Kelun	2025	HER2	Breast Cancer
Becotatug vedotin	Meiyouheng	Lepu	2025	EGFR	Nasopharyngeal Cancer

III. ADC Drugs by Target in 2026 (Target-Based Classification)

1. HER2-Targeted ADC Drugs

HER2 (Human Epidermal Growth Factor Receptor 2) is one of the most actively studied targets in ADC development. It belongs to the EGFR receptor family and plays a critical role in cell proliferation and signaling pathways.

In breast cancer, gastric cancer, and lung cancer, HER2 gene amplification or protein overexpression promotes tumor growth and progression, making it an important therapeutic target.

HER2-targeted ADCs use anti-HER2 monoclonal antibodies to precisely recognize tumor cells and deliver cytotoxic payloads into cancer cells.

Representative drugs include:

● Trastuzumab emtansine (Kadcyla)
● Trastuzumab deruxtecan (Enhertu)
● Disitamab vedotin (Aidixi)
● Trastuzumab rezetecan (Aiweida)
● Trastuzumab botidotin (Shutailai)

Among them, Enhertu is considered one of the most successful ADC drugs. Its DXd payload has a strong bystander effect, enabling efficacy even in HER2-low tumors.

2. TROP2-Targeted ADC Drugs

TROP2 (Trophoblast Cell Surface Antigen 2) is a transmembrane glycoprotein highly expressed in various epithelial tumors, including breast, lung, pancreatic, and colorectal cancers.

TROP2 is involved in tumor proliferation, migration, and invasion, making it a major focus of ADC development.

TROP2-targeted ADCs typically carry topoisomerase inhibitors and deliver them selectively to tumor cells.

Representative drugs:

● Sacituzumab govitecan (Trodelvy)
● Sacituzumab tirumotecan (Jiataile)
● Datopotamab deruxtecan (Datroway)

These drugs are mainly used in triple-negative breast cancer (TNBC), HR+/HER2- breast cancer, and non-small cell lung cancer.

Trodelvy was the first approved TROP2 ADC, delivering SN-38 as its payload. With the emergence of DXd-based ADCs, TROP2-targeted therapies are becoming increasingly important.

3. CD-Targeted ADC Drugs

CD antigens are widely expressed on immune cells and are key therapeutic targets in hematologic malignancies.

These targets are highly stable and specific, making them ideal for ADC-based therapies.

CD-targeted ADCs bind to leukemia or lymphoma cells and release potent cytotoxic agents.

Representative drugs include:

● Gemtuzumab ozogamicin (CD33)
● Brentuximab vedotin (CD30)
● Inotuzumab ozogamicin (CD22)
● Loncastuximab tesirine (CD19)
● Polatuzumab vedotin (CD79b)

These drugs are used in:

• Acute Myeloid Leukemia (AML)
• Hodgkin Lymphoma
• Diffuse Large B-Cell Lymphoma (DLBCL)
• Acute Lymphoblastic Leukemia (ALL)

Brentuximab vedotin is a landmark CD30-targeted ADC with significant clinical impact.

4. EGFR-Targeted ADC Drugs

EGFR is a key oncogenic driver in many solid tumors, including head and neck cancer, nasopharyngeal carcinoma, and some lung cancers.

It regulates cell proliferation, differentiation, and angiogenesis.

Recent research has focused on EGFR-targeted ADCs as an alternative to traditional EGFR inhibitors.

Relevant ADC drugs:

• Cetuximab sarotalocan (Akalux)
• Becotatug vedotin (Meiyouheng)

Akalux uses an innovative Photoimmunotherapy (PIT) approach. After binding tumor cells, it is activated by near-infrared light, causing membrane disruption and tumor cell death.

5. Tissue Factor-Targeted ADC Drugs

Tissue Factor (TF) is a transmembrane protein involved in the coagulation cascade and is highly expressed in multiple solid tumors, including cervical, ovarian, and pancreatic cancers.

TF also contributes to tumor angiogenesis and metastasis.

Representative drug:
Tisotumab vedotin (Tivdak)

This is the first ADC approved for recurrent or metastatic cervical cancer. It delivers MMAE payload and has shown strong response rates in clinical trials.

6. BCMA-Targeted ADC Drugs

BCMA (B-cell maturation antigen) is highly expressed on multiple myeloma cells.

It is also widely used in CAR-T and bispecific antibody development.

Representative drug:
Belantamab mafodotin (Blenrep)

It delivers MMAF payload to myeloma cells. Although withdrawn in some markets, BCMA remains a highly promising target.

7. Nectin-4-Targeted ADC Drugs

Nectin-4 is a cell adhesion molecule highly expressed in urothelial carcinoma, with expression rates exceeding 90% in advanced bladder cancer.

Representative drug:
Enfortumab vedotin (Padcev)

Padcev delivers MMAE payload and has become a standard treatment. It is also used in combination with pembrolizumab (Keytruda).

8. FRα-Targeted ADC Drugs

FRα (Folate Receptor Alpha) is highly expressed in ovarian cancer and minimally expressed in normal tissues.

Representative drug:
Mirvetuximab soravtansine (Elahere)

It delivers DM4 payload and provides a targeted treatment option for platinum-resistant ovarian cancer.

9. c-MET-Targeted ADC Drugs

c-MET is a receptor tyrosine kinase involved in tumor growth, invasion, and metastasis.

It is overexpressed in some NSCLC patients.

Representative drug:
Telisotuzumab vedotin (Emrelis)

This ADC delivers MMAE payload and has shown promising response rates in c-MET overexpressing NSCLC.

IV. ADC Technology Development Trends

With ongoing innovation, ADCs are rapidly evolving toward improved precision, efficacy, and safety. Recent studies published in Nature Reviews Drug Discovery highlight rapid advances in ADC design and payload optimization.

In the era of adc drugs by target in 2026, technological advances are expanding their role across multiple tumor types.

Next-generation ADCs are evolving toward:

• More stable linker technology
  Enhances stability in circulation and reduces premature payload release, improving safety.
• More potent payloads (e.g., DXd)
  Enables stronger antitumor activity and effectiveness in low-expression tumors.
• Higher drug-to-antibody ratio (DAR)
  Increases payload delivery while requiring optimized balance for safety and stability.
• Stronger bystander effects
  Allows killing of neighboring tumor cells, especially in heterogeneous solid tumors.
• Broader target exploration
  New targets such as TROP2 and Nectin-4 are expanding the landscape of ADC drugs.

These advancements are driving ADCs to become a cornerstone of modern cancer therapy.

Conclusion

Since the first ADC drug was approved in 2000, the field has undergone more than two decades of rapid innovation.

As of March 2026, 21 ADC drugs have been approved globally, covering multiple tumor targets and indications.

Understanding adc drugs by target in 2026 is essential for researchers, clinicians, and pharmaceutical partners.

✨ As a global distributor focusing on innovative oncology therapies, DengYueMed continues to track the development of ADC technologies and provide reliable drug information and supply support for international partners.

FAQ about ADC Drugs by Target in 2026