The document discusses antibody-drug conjugates (ADCs), which are monoclonal antibodies coupled to cytotoxic drugs. Effective ADC payloads must be highly cytotoxic, target intracellular components, be small to avoid immunogenicity, and be stable in plasma. Common intracellular targets of ADC payloads include DNA, microtubules, and transcription machinery. The payloads aim to induce DNA damage, disrupt microtubule assembly, or interfere with transcription to promote cancer cell death. Novel payloads also include nano-carriers, protein toxins, and enzymes for antibody-directed prodrug therapy.

1. Antibody-drug Conjugates
Payloads
Reference: https://www.creative-biolabs.com/adc/drug-module.htm

2. Contents
 What is antibody-drug conjugate
 Properties of ADC Payloads
 Major intracellular targets of ADC payloads

3. What is antibody-drug conjugate
01

4. Antibody-drug conjugate
As a key factor in an ADC, the payload drug dictates its efficacy. At this moment, a large variety of
payload drugs have been exploited in ADC and the number is on the rise.
Antibody-drug conjugates (ADCs) are next-generation targeted anti-tumor agents that are constructed by
the covalent coupling of a monoclonal antibody with a cytotoxic payload drug via a small molecular linker.

5. Properties of ADC Payload
02

6. 01
must exert
extremely high
cytotoxic efficacy
02
the targets of the
payloads must be
located inside the
cell
03
small in size to
minimize the risk of
immunogenicity
04
exert adequate
plasma stability
Properties of ADC Payloads

7. Major intracellular targets of ADC payloads
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8. DNA
Toxins
Induce DNA damage and subsequently cell death by various
mechanisms, such as double stranded DNA cleavage, DNA cross-
linking
Microtubul
e
Toxins
Inhibit tumor cell growth and promote apoptosis by disrupting the
assembly and dynamics of microtubules.
Inhibitors Bearing unique chemical and cytotoxicity profiles
Transcription
Toxins
Toxins targeting the DNA transcription machineries have
been demonstrated as good candidates for ADC
development
01
02
03
04

9. Other payloads
With the development of fusion protein expression technology and nanoscience, the warfare against
cancer has expended exponentially and many novel payloads based on these technological platforms,
such as Nano-carriers, protein toxins, and toxic proteins for antibody-directed enzyme prodrug therapy
(ADEPT), have also been exploited for ADC development.

10. THANK YOU
Reference: https://www.creative-biolabs.com/adc/drug-module.htm