The Chemistry Behind ADCs

Area of Science:

• Medicinal Chemistry
• Oncology
• Drug Development

Background:

• Antibody-drug conjugates (ADCs) are an effective cancer therapy, leveraging targeted cell recognition and potent cytotoxic payloads.
• Numerous ADCs are approved or in clinical development, highlighting their therapeutic significance.

Purpose of the Study:

• To review the chemistry of ADCs from a medicinal chemistry perspective.
• To focus on chemical methods for ADC assembly and controlled drug payload release.

Main Methods:

• Review of chemical methodologies for ADC construction.
• Analysis of linker chemistry and its impact on drug release.

Main Results:

• Discussion of strategies for selecting antibodies and drug payloads based on disease pharmacology.
• Emphasis on the choice of chemical linkers for efficient ADC assembly.

Conclusions:

• The chemical assembly and controlled release of drug payloads are critical for ADC efficacy.
• Medicinal chemistry plays a vital role in advancing ADC-based cancer therapeutics.