Cytotoxic Agents and Antibody-drug Conjugates

Drug name Target Mode of Action Example
Auristatinsα-TubulinPrevent tubulin polymerization
Maytansinoidsα-TubulinPrevent tubulin polymerization
CalicheamicinsSequence-specific minor groove of DNACauses double-strand DNA breaks
Duocarmycin analoguesBind to specific minor groove of DNABreak down adenine-specific molecules in the DNA structure
Doxorubicin and Doxorubicin derivativesTopoisomerase II
DNA complexes
Inhibit DNA religation, leading to DNA double-strand breaks
  • BR96-DOX
CC-1065Sequence-specific minor groove of DNAInduces adenine alkylation
AnthracyclinesDNA, RNA complexesInhibit DNA and RNA synthesis by intercalating between base pairs, preventing replications
PyrrolobenzodiazepineSequence-selective. Bind to the minor groove of DNA and covalently attach to guanine residues

Interfere with the action of endonuclease enzymes on DNA and block transcription by inhibiting DNA polymerase in a sequence specific manner

Other cytotoxic agents used in the development of antibody-drug conjugates include:

  • Streptonigtin (anti CD30 and anti CD70)
  • Geldanamycin (HSP90 inhibitor)
  • Centanamycin (ML-970; indolecarboxamide);
  • SN38 is the active metabolite of irinotecan (an analog of Camptothecin, a topoisomerase I inhibitor)

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ADC Review
ADC Review, Journal of Antibody-drug Conjugates (ISSN 2327-0152) launched in 2013, is designed to serve the needs of a diverse community of individuals including academia, life sciences, pharma, (basic, translational and clinical) research, clinicians/physicians, along with regulatory affairs, government authorities and representatives from payers, and policy makers. The Journal’s content includes peer reviewed research, commentaries, news features, discussions, editorials and blogs on topics relevant to a broad international readership. The Journal also offers a knowledge center (called ADC University) offering the latest and most relevant information about Antibody-drug Conjugates (ADCs), BiSpecific Antibodies, Site Specific Antibody Drug Conjugates, Small Molecule Drug Conjugates (SMDC), and Engineered Antibody Fragments. The purpose of the Journal is to present this information in an understandable and a useful format for all stakeholders.