ADC Payloads

1
ADC Payloads

• https//www.creative-biolabs.com/adc

2
ADC Payloads

• 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. 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.

3
To facilitate the unique needs for different ADC
antibody development projects, Creative Biolabs
has established an advanced DrugLnk organic
synthesis platform with a large collection of
payload drugs and linkers in the drug module
and the linker module, respectively. Our
scientists are highly experienced in full
chemical synthesis, chemical modification, as
well as bio-conjugation. We are dedicated to help
our clients prepare innovated payload-linker
complexes for novel ADC developments.
4
ADC Payloads
02
DNA Toxins
03
Transcription Toxins
04
Inhibitors
05
Other Payloads
5

• Microtubule toxins are a successful group of
  anticancer drugs that inhibit tumor cell growth
  and promote apoptosis by disrupting the assembly
  and dynamics of microtubules. They are generally
  applied in combination with other treatments
  against malignancies.

• In the form of an ADC, serious adverse effects of
  these microtubule toxins are greatly reduced,
  allowing the usage of these extremely potent
  agents for therapeutic applications.

6

• DNA toxins induce DNA damage and subsequently
  cell death by various mechanisms, such as double
  stranded DNA cleavage, DNA cross-linking They
  are highly toxic agents with in vitro potency
  down to the picomolar level against tumor cell
  lines.

• With optimized linkers and conjugation
  strategies, DNA toxins are incorporated into ADCs
  for accurate drug delivery and an expanded
  therapeutic window.

7

• Toxins targeting the DNA transcription
  machineries have been demonstrated as good
  candidates for ADC development.

• Currently, toxins against RNA polymerase II (the
  initial step in DNA transcription) and
  spliceosome (for correct mRNA maturation and
  processing) are being actively exploited.

8

• Various small molecule inhibitors, bearing unique
  chemical and cytotoxicity profiles, have also
  been exploited as ADC payloads.

• The process inhibited include oxidative
  phosphorylation (oligomycins), ATP biosynthesis
  (ipatasertib), and other important enzymes such
  as dihydrofolate reductase (DHFR, methotrexate)

9

• 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 antibody), have also been
  exploited for ADC development.

10
With our well-established DrugLnk organic
synthesis platform, the experienced scientists
here at Creative Biolabs is dedicated to help you
prepare various customized payload-linker
complexes using toxins in the Drug Module for ADC
development in a timely and cost-effective
manner.
11
45-1 Ramsey Road, Shirley, NY 11967, USA
Email marketing_at_creative-biolabs.com
Contact us
12
Thank You