Degrader-Antibody Conjugates: Risks on the Path from Concept to Reality

Degrader-Antibody Conjugates: Risks on the Path from Concept to Reality

01 DAC‘s Emergence and Advantages Cancer therapeutics need to balance efficacy and safety, even targeted chemotherapy does not always only kill abnormal cancer cells, and non-specific toxicity can lead to a low therapeutic index and side effects. The technology of Proteolysis-targeting chimeras (PROTACs), which achieve therapeutic effects by promoting the degradation of target proteins, is … Read more

A Journey into ADC Innovation

A Journey into ADC Innovation

After 2019, ADC drugs have been approved for marketing one after another, and the approval of Aidiqi in 2021 marked a milestone in the development of domestic ADC innovative drugs. The broad therapeutic prospects and huge market size have stimulated many pharmaceutical companies to ignite their enthusiasm for ADC drug research and development, leading the … Read more

In-Depth Analysis of ADCs: Part Two

In-Depth Analysis of ADCs: Part Two

Introduction Antibodies are one of the key components of ADC drugs, serving as precise guiding components with the functions of targeting and toxin delivery. They can specifically recognize the target antigens on the surface of tumor cells, delivering toxins to the tumor cells and mediating the localization and endocytosis of ADCs in tumor cells[1]. After … Read more

ADC Technology: Innovations from Five Key Elements

ADC Technology: Innovations from Five Key Elements

History of ADC Drug Development Phase 1 (1906-1982), the concept of targeted therapy was proposed, and the technology took shape. Phase 2 (1983-2011), transition from clinical trials to commercialization, Mylotarg® was approved for market. Phase 3 (2012-present), explosive growth of ADC products. The five key elements of ADC drugs are target, antibody, linker, cytotoxic agent, … Read more

The Competitive Landscape Behind Coupling in Drug Development

The Competitive Landscape Behind Coupling in Drug Development

To improve the DMPK characteristics, many studies have explored the coupling of PROTAC payloads with monoclonal antibodies to create a new molecule known as “Antibody-Drug Conjugates (DAC).” This allows for more effective delivery of PROTAC degraders in vivo. â–˛ Structure of DAC (Image Source: Reference 1) Compared to PROTAC molecules, DAC has several potential advantages: … Read more

Degrader-Antibody Conjugates: The Risky Path from Concept to Reality

Degrader-Antibody Conjugates: The Risky Path from Concept to Reality

The Emergence and Advantages of DAC Cancer therapeutics need to achieve a balance between efficacy and safety, even targeted chemotherapy does not always only kill abnormal cancer cells, non-specific toxicity can lead to a low therapeutic index and side effects. The technology of proteolysis-targeting chimeras (PROTACs), which achieves therapeutic effects by promoting the degradation of … Read more

Understanding ADC Drug Resistance Mechanisms

Understanding ADC Drug Resistance Mechanisms

1. Mechanism of ADC Action Antibody-drug conjugates (ADC) (Click to enter the database to search for global ADC drug information) enter the body, the antibody part binds to the targeted antigen on the surface of tumor cells, tumor cells will endocytose the ADC molecule. Among them, some can bind to Fc receptors in the endosome, … Read more

What Magic Do ADCs and RDCs Hold?

What Magic Do ADCs and RDCs Hold?

ADCs (Antibody-Drug Conjugates) and RDCs (Radionuclide Conjugates) are innovative drugs that have gained significant attention in recent years, demonstrating enormous potential in the field of oncology. They are referred to as the “magic bullets” of tumor-targeted therapy because they enable precise treatment while avoiding damage to normal cells. ADC drugs link antibodies with known effective … Read more

Understanding ADC: Overview, Antibody and Linker Selection

Understanding ADC: Overview, Antibody and Linker Selection

The development of ADC drugs has not been smooth sailing, with nearly 100 years of history since the concept of the “magic bullet” was proposed, but ultimately, the clouds have parted to reveal the moon. DS8201 has redefined ADC, but it is not the end of ADC drugs, rather a new beginning. A comprehensive understanding … Read more

Analyzing Successful Payloads and Linkers of Approved ADCs

Analyzing Successful Payloads and Linkers of Approved ADCs

ADC Field Blooms, new technologies evolve like a rolling tide, propelling biomedicine into high-speed mode. This is the best of times. As early as the early 20th century, Paul Ehrlich first proposed the concept of “magic bullets”; however, the first ADC drug, Mylotarg® (gemtuzumab ozogamicin), was not approved until nearly a century later. Every cloud … Read more