ADC Conjugation

Antibody–drug conjugate (ADC) is typically composed of an antibody covalently attached to a payload via a chemical linker. It has lower toxicity and higher anticancer activity, as well as higher stability, allowing patients to receive better anticancer therapeutics. There have been 16 ADCs received market approval so far worldwide. The global market size is estimated to reach USD 32.1 billion by 2028. The success of ADC drug development is largely determined by the conjugation technology. Typical conjugation approaches include non-site specific conjugation and site-specific conjugation techniques.

Non-site specific conjugation processes produce heterogeneous mixtures of conjugated species with variable DARs. Adding to the complexity, the site of conjugation could be different for each ADC species containing even only one drug. Site-specific methods to modify antibodies produce homogeneous and well-defined conjugates without compromising the conjugate’s biological activity, representing a significant trend in recent years. Site-specific conjugation techniques currently include the incorporation of cysteine (Cys), glutamine (Gln), unnatural amino acids (such as p-acetylphenylalanine or pAcF and p-azidomethyl-L-phenylalanine or pAMF), or short peptide tags. At ChemExpress, our expert team offers free consultations to help you choose the optimal conjugation strategy that aligns with your project goals. We work closely with you to understand your specific needs and accelerate your path to discovery.

How to choose the right conjugation strategy for your Antibody Drug Conjugation development?

Fig.1 The characteristics of various conjugation methods applied for ADC
	Conjugation methods	Advantages
Non-site specific conjugation	Lysine sites	• Rapid and convenient
Non-site specific conjugation	Reduced cysteine sites	• A relatively homogeneous product
Site-specific conjugation	Engineered reactive cysteine residues	• High homogeneity; •Tunable reactivity and stability
	Disulfide re-bridging	• High homogeneity; •No influence on spatial structure of antibody; •National amino acid sequence and glycosylation
	Unnatural amino acids	•High homogeneity; •Tunable reactivity and stability; •High efficiency of conjugation
	Enzyme-assisted ligation	•High homogeneity; •High efficiency of conjugation •DAR alteration possible
	Glycan remodeling and glycoconjugation	•High homogeneity; •No alteration of amino acid sequence
	pClick technology	•Without antibody engineering or chemical / enzymatic treatments •Simple, efficient, and convenient

ChemExpress ADC Conjugation Services

Choose proper chemistry conjugation methods according to your unique needs, ChemExpress's ADC conjugation technology services are available in various formats, including FFS, FTE, and CMC, providing services such as conjugate drug screening, conjugation process development and optimization, and conjugate sample preparation. ChemExpress R&D team employs multiple methods for the synthesis of bioconjugates between payloads and macromolecules. Our bioconjugation experience includes various carriers, and we offer an extensive library of linkers and payloads for your R&D purposes, as demonstrated below. Contact us for more information and a detailed quote.

Drug carrier

Monoclonal antibody
Bispecific antibody ThioMab
Antibody Fragments Aptamer
Conjugation methods

Lysine sites Cysteine sites
Unnatural amino acids
Transglutaminase
ThioBridge-like
Payloads

MMAE, Exatecan, Eribulin,
DXd PBD, Tublysin
Doxorubicin Etc.

ChemExpress ADC Analytical Platform

Biomolecules like ADCs are complex and require thorough analytical assessment to ensure safety and quality. At ChemExpress, we leverage our in-house expertise and advanced analytical equipment to characterize key intermediates, including proteins/mAbs, payloads, and linkers. To streamline your project and ensure scalability, our experienced R&D and analytical teams work closely together to develop processes that meet your specific quality attributes. The methods used to assess and characterize these complex bioconjugate molecules include:

Next-generation bioconjugates and the future of ADCs

With the continuous progress of chemical conjugation, protein genetic engineering and other technologies, the field of targeted delivery of drug conjugates is not limited to ADCs, and various types of drug conjugates have been generated. For example, a peptide‒drug conjugate (PDC) comprises a homing peptide, payload and linker. Degrader-antibody conjugates (DACs) that combine a proteolysis targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical linker. In radionuclide drug conjugates (RDCs), another innovative form of medical imaging and treatment, tumor antigen-specific targeting antibodies or Payload-Linkers are connected by linkers to radioisotopes (both imaging and radiokilling), which enables accurately guided radionuclide delivery to tumors for diagnosis or treatment. Other examples include peptide-oligonucleotide conjugates (POCs), Payload-Linker–drug conjugates (SMDCs), virus-like drug conjugates (VDCs), antibody–oligonucleotide conjugates (AOCs), antibody–cell conjugates (ACCs), immune-stimulating antibody conjugates (ISACs), antibody fragment–drug conjugates (FDCs), antibody–degrader conjugates (ADeCs), and aptamer–drug conjugates (ApDCs).

Such novel approaches to bioconjugates opens doors to new mechanisms of action, therapies, and indications. With expertise and dedication, advanced ADC bioconjugation platform and services from ChemExpress will be your best companion in creating customized ADCs.

Partner with ChemExpress

ChemExpress maintains a substantial inventory of over 80 payloads and 400 linkers and can customize the synthesis of payload-linkers to meet client needs. With extensive experience in linker compound synthesis, having successfully completed over 1,000 syntheses, our experienced technical team is dedicated to providing end-to-end, one-stop solutions for Antibodies and ADCs, providing antibodies, payload linkers, conjugates and drug products to biotech & pharma from R&D to commercialization. Contact a ChemExpress representative for more information.

80+ Payloads

400+ Linkers

1000+ Linker Syntheses
Large-scale payloads and
linkers GMP manufacturing
Advanced technologies
and methodologies
50+ CMC Projects,

1 Commercial Project
12 sec-DMFs,
offering High-quality and cost-effective products
Passed US FDA inspection
with zero 483 observations
Integrated ADC DS & DP CDMO
platform for commercialization

References

[1] Sig Transduct Target Ther. 2022
[2] Angew Chem Int Ed Engl. 2021
[3] Antibody Therapeutics. 2020
[4] Zhou et al.Experimental Hematology & Oncology. 2024

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