The structure of antibody-drug conjugate (ADC)
ADC consists of antibodies and payload, linker connects antibodies and small molecule drugs. After ADC drugs enter the blood, its antibody part will recognize and bind to the surface antigen of target cells. Theninternalizing ADC antigen complex into cells through endocytosis, the complex will be degraded by lysosomes and the payload will be released, so as to destroy DNA or microtubules, or exert the inhibitory effect of topoisomerase / RNA polymerase, resulting in cell death. It has the characteristics of precision and great lethality. It is a new generation of therapeutic drugs.1
Cellular Processing of antibody-drug conjugate (ADC)
ADC is composed of navigator targeting specific tumor cells and small molecules that can enter tumor cells to kill them, so how to maintain activity in blood to achieve good presentation effect is also a problem. Of course, accurate targeting can greatly reduce the sidekill effect. After ADC is swallowed into cells, lysosomal enzymes will hydrolyze the navigation of missiles (antibodies), thus releasing small cytotoxic molecules. Thus, it can block a series of activities in cells, including the transcription and translation of DNA and RNA. It can also block the transport of proteins by affecting tubulin. Finally, it can kill tumor cells. Therefore, here we need to pay attention to the consequences of Miss target and the loading of small molecules, which are potentially harmful to normal tissues and cells. The suspension of many clinical drugs in phase II and phase III is also greatly related to these two key points.
How antibody-drug conjugate (ADC) work? Mechanisms of action (MOA) for ADC
The drugs in ADC can recognize the membrane proteins of tumor cells, then locate the target cells. After endocytosis into cells, lysosomes hydrolyze and release small molecules in ADC. For example, VCMMAE is an anti-mitotic agent in antibody coupled drugs (ADC). It is crosslinked by monomethylalistatin e (MMAE) and dipeptide valine citrulline (VC). VCMMAE is a powerful anti-mitotic agent by blocking tubulin polymerization. VCMMAE effectively resist mitosis and kill cells by blocking tubulin polymerization. Microtubules play an important role in cell function, participate in migration, transportation and recombination, and have many dynamic roles, including the movement of motor proteins and the separation of chromosomes during cell division.
Reference:
1. Su Z , Xiao D , Xie F , et al. Antibodydrug conjugates: Recent advances in linker chemistry[J]. Acta Pharmaceutica Sinica B, 2021.
2. Dean AQ, Luo S, Twomey JD, Zhang B. Targeting cancer with antibody-drug conjugates: Promises and challenges. MAbs. 2021 Jan-Dec;13(1):1951427. doi: 10.1080/19420862.2021.1951427. Erratum in: MAbs. 2021 Jan-Dec;13(1):1966993. PMID: 34291723; PMCID: PMC8300931.
Product List
Cat No. | Products Name (INN Index) | INN Name | Previous Name | Target | Format | Order |
---|---|---|---|---|---|---|
Pre-Made Losatuxizumab Vedotin Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
losatuxizumab vedotin |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Lupartumab Amadotin Biosimilar, Whole Mab Adc, Anti-Lypd3 Antibody: Anti-C4.4A therapeutic antibody Drug Conjugate |
lupartumab amadotin |
NA |
LYPD3 |
Whole mAb ADC |
||
Pre-Made Mipasetamab Uzoptirine Biosimilar, Whole Mab Adc, Anti-Axl Antibody: Anti-ARK/JTK11/Tyro7/UFO therapeutic antibody Drug Conjugate |
mipasetamab uzoptirine |
NA |
AXL |
Whole mAb ADC |
||
Pre-Made Mirvetuximab Soravtansine Biosimilar, Whole Mab Adc, Anti-Folr1 Antibody: Anti-FBP/FOLR/FRalpha/NCFTD therapeutic antibody Drug Conjugate |
mirvetuximab soravtansine |
NA |
FOLR1 |
Whole mAb ADC |
||
Pre-Made Mirzotamab Clezutoclax Biosimilar, Whole Mab Adc, Anti-Cd276 Antibody: Anti-4Ig-B7-H3/B7-H3/B7H3/B7RP-2 therapeutic antibody Drug Conjugate |
mirzotamab clezutoclax |
NA |
CD276 |
Whole mAb ADC |
||
Pre-Made Naratuximab Emtansine Biosimilar, Whole Mab Adc, Anti-Cd37 Antibody: Anti-GP52-40/TSPAN26 therapeutic antibody Drug Conjugate |
naratuximab emtansine |
NA |
CD37 |
Whole mAb ADC |
||
Pre-Made Patritumab Deruxtecan Biosimilar, Whole Mab Adc, Anti-ERBB3/Erbb-3 Antibody: Anti-ErbB-3/FERLK/HER3/LCCS2/MDA-BF-1/VSCN1/c-erbB-3/c-erbB3/erbB3-S/p180-ErbB3/p45-sErbB3/p85-sErbB3 therapeutic |
patritumab deruxtecan |
NA |
ERBB3 |
Whole mAb ADC |
||
Pre-Made Pelgifatamab Corixetan Biosimilar, Whole Mab Adc, Anti-FOLH1/GCPII Antibody: Anti-FGCP/FOLH/GCP2/NAALAD1/PSM/PSMA/mGCP therapeutic antibody Drug Conjugate |
pelgifatamab corixetan |
NA |
FOLH1 |
Whole mAb ADC |
||
Pre-Made Pinatuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Cd22 Antibody: Anti-SIGLEC-2/SIGLEC2 therapeutic antibody Drug Conjugate |
pinatuzumab vedotin |
NA |
CD22 |
Whole mAb ADC |
||
Pre-Made Pivekimab Sunirine Biosimilar, Whole Mab Adc, Anti-Il3Ra Antibody: Anti-CD123/IL3R/IL3RX/IL3RY/hIL-3Ra therapeutic antibody Drug Conjugate |
pivekimab sunirine |
NA |
IL3RA |
Whole mAb ADC |
||
Pre-Made Polatuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Cd79B Antibody: Anti-AGM6/B29/IGB therapeutic antibody Drug Conjugate |
polatuzumab vedotin |
NA |
CD79B |
Whole mAb ADC |
||
Pre-Made Praluzatamab Ravtansine Biosimilar, Whole Mab Adc, Anti-Alcam Antibody: Anti-CD166/MEMD therapeutic antibody Drug Conjugate |
praluzatamab ravtansine |
NA |
ALCAM |
Whole mAb ADC |
||
Pre-Made Rolinsatamab Talirine Biosimilar, Whole Mab Adc, Anti-Prlr Antibody: Anti-HPRL/MFAB/RI-PRLR/hPRLrI therapeutic antibody Drug Conjugate |
rolinsatamab talirine |
NA |
PRLR |
Whole mAb ADC |
||
Pre-Made Rosopatamab Tetraxetan Biosimilar, Whole Mab Adc, Anti-FOLH1/GCPII Antibody: Anti-FGCP/FOLH/GCP2/NAALAD1/PSM/PSMA/mGCP therapeutic antibody Drug Conjugate |
rosopatamab tetraxetan |
NA |
FOLH1 |
Whole mAb ADC |
||
Pre-Made Rovalpituzumab Tesirine Biosimilar, Whole Mab Adc, Anti-Dll3 Antibody: Anti-SCDO1 therapeutic antibody Drug Conjugate |
rovalpituzumab tesirine |
NA |
DLL3 |
Whole mAb ADC |
||
Pre-Made Sacituzumab Govitecan Biosimilar, Whole Mab Adc, Anti-Tacstd2 Antibody: Anti-EGP-1/EGP1/GA733-1/GA7331/GP50/M1S1/TROP2 therapeutic antibody Drug Conjugate |
sacituzumab govitecan |
NA |
TACSTD2 |
Whole mAb ADC |
||
Pre-Made Samrotamab Vedotin Biosimilar, Whole Mab Adc, Anti-Lrrc15 Antibody: Anti-LIB therapeutic antibody Drug Conjugate |
samrotamab vedotin |
NA |
LRRC15 |
Whole mAb ADC |
||
Pre-Made Serclutamab Talirine Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
serclutamab talirine |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Sirtratumab Vedotin Biosimilar, Whole Mab Adc, Anti-Slitrk6 Antibody: Anti-DFNMYP therapeutic antibody Drug Conjugate |
sirtratumab vedotin |
NA |
SLITRK6 |
Whole mAb ADC |
||
Pre-Made Sofituzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Muc16 Antibody: Anti-CA125 therapeutic antibody Drug Conjugate |
sofituzumab vedotin |
NA |
MUC16 |
Whole mAb ADC |
View the Knowledge base of Antibody-drug Conjugate (ADC):
– What is antibody-drug conjugate (ADC)?
– Antibody-drug conjugate (ADC) in clinical application (Approved/BLA, phaseI/II/III)
– Main elements of antibody-drug conjugate (ADC): Antibodies and their targets
– Main elements of antibody-drug conjugate (ADC):Linker (cleavable/non-cleavable, structure and mechanism)
– Main elements of antibody-drug conjugate (ADC):Toxins/Payloads (Classification and function)
– Toxins/Payloads (Classification and function) of Microtubule destroying drug
– Toxins/Payloads (Classification and function) of DNA damage drugs
– Toxins/Payloads (Classification and function) of Innovative drugs
– Biological coupling technology Chemical based specific in situ antibody modification
– Endogenous coupling of amino acids and Disulfide re bridging strategy
– Glycan coupling
– Site specific biological coupling of engineered antibodies and Enzymatic method
– Biological coupling with engineered unnatural amino acids
– Review for ADC production, quality control and functional assay
– Product data of ADC