Endogenous coupling of amino acids and Disulfide re bridging strategy
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Antibody-drug Conjugate (ADC): Pre-made ADC benchmark, MOA, Production and QC
Neutralizing antibodies of virus (SARS2, HIV, HBV, Rabies, RSV, Ebola, Influenza)
Immunoglobulin Fc receptors for Fc&Fc Receptor binding assay
ILIBRA-HuEasy Monoclonal antibody (mab) humanization service (fully humanized ab)
Single domain antibody (Nanobody)
SOCAIL MEDIA
Endogenous coupling of amino acids
One of the most common coupling methods is to use the lysine residue of the antibody, the amino acid nucleophilic NH2 group, to react with the electrophilic N-hydroxysuccinimide (NHS) Group on the lik payload. Although the reaction is simple, the high abundance of available lysine residues leads to the formation of uneven mixtures of many ADCs under random distribution. DAR is controlled by antibody-drug conjugates stoichiometry, which is widely used, including approved ADCs such as Besponsa, Mylotarg, and Kadcyla.
Disulfide re bridging strategy
IgG antibodies contain four disulfide bonds between chains, two connecting light chains and heavy chains, and two are located in the hinge region connecting two heavy chains. They maintain the integrity of monoclonal antibodies. Another classic biological coupling pathway explores the role of these cysteines as payload attachment points. The reduction of four disulfide bonds usually produces eight sulfhydryl groups, which can react with the linker of maleimide to produce ADC with DAR=8.
Dorona and colleagues reported an example of an ADC with a chimeric anti-CD30 monoclonal antibody coupled to MMAE, DAR= 8. Compared with the classical lysine coupling, this payload loading method is better controlled. However, it is reported that the plasma clearance rate will be higher and the risk of plasma aggregation will be reduced.
In 2015, chudasama et al. Introduced a new type of re bridging reagent, dibromopyridazinediones. They proved that it can be effectively inserted into the disulfide bond, and the resulting structure shows excellent hydrolytic stability even at high temperature. However, with the increase of temperature on the reduction step, heterogeneity is also observed, and this structure also allows the selective introduction of different functional groups.
Divinylpyrimidine is another effective re-bridging reagent, which can produce stable ADC with Dar = 4. Spring et al. Studied the effect of vinyl heteroaryl scaffold on cysteine re bridging. They believe that replacing pyridine with pyrimidine can make heteroaryl ring a better electron acceptor, so as to improve the crosslinking efficiency. Their work extends to divinyltriazine, which shows higher efficiency at high temperature.
In order to avoid the disadvantage of in vivo instability associated with classical maleimide coupling, Barbas et al studied methylsulfonylphenyloxadiazole, which has a specific reaction to cysteine. They are more stable than cysteine maleimide conjugates in plasma. Inspired by this, Zeglis designed dipods reagent, which contains two oxadiazole methyl sulfone parts connected by phenyl. Dipods forms covalent bonds with two sulfate radicals in the way of re bridging. Compared with maleimide coupling, coupling in this way has superior stability in vitro and performance in vivo.
Product List
Cat No. | Products Name (INN Index) | INN Name | Previous Name | Target | Format | Order |
|---|---|---|---|---|---|---|
Pre-Made Anetumab biosimilar, Whole mAb ADC, Anti-MSLN Antibody: Anti-MPF/SMRP therapeutic antibody |
Anetumab |
NA |
MSLN |
Whole mAb ADC |
||
Pre-Made Aprutumab biosimilar, Whole mAb ADC, Anti-FGFR2 Antibody: Anti-BBDS/BEK/BFR-1/CD332/CEK3/CFD1/ECT1/JWS/K-SAM/KGFR/TK14/TK25 therapeutic antibody |
Aprutumab |
NA |
FGFR2 |
Whole mAb ADC |
||
Pre-Made Azintuxizumab biosimilar, Whole mAb ADC, Anti-SLAMF7/CS1 Antibody: Anti-19A/CD319/CRACC therapeutic antibody |
Azintuxizumab |
NA |
SLAMF7/CS1 |
Whole mAb ADC |
||
Pre-Made Belantamab biosimilar, Whole mAb ADC, Anti-TNFRSF17 Antibody: Anti-BCM/BCMA/CD269/TNFRSF13A therapeutic antibody |
Belantamab |
NA |
TNFRSF17 |
Whole mAb ADC |
||
Pre-Made Brentuximab biosimilar, Whole mAb ADC, Anti-TNFRSF8 Antibody: Anti-CD30/Ki-1/D1S166E therapeutic antibody |
Brentuximab |
NA |
TNFRSF8 |
Whole mAb ADC |
||
Pre-Made Camidanlumab biosimilar, Whole mAb ADC, Anti-IL2RA Antibody: Anti-CD25/IDDM10/IL2R/IMD41/TCGFR/p55 therapeutic antibody |
Camidanlumab |
NA |
IL2RA |
Whole mAb ADC |
||
Pre-Made Cantuzumab biosimilar, Whole mAb ADC, Anti-MUC1 Antibody: Anti-ADMCKD/ADMCKD1/ADTKD2/CA 15-3/CD227/Ca15-3/EMA/H23AG/KL-6/MAM6/MCD/MCKD/MCKD1/SEC/X/ZD/PEM/PEMT/PUM therapeutic antibody |
Cantuzumab |
NA |
MUC1 |
Whole mAb ADC |
||
Pre-Made Cofetuzumab biosimilar, Whole mAb ADC, Anti-PTK7 Antibody: Anti-CCK-4/CCK4 therapeutic antibody |
Cofetuzumab |
NA |
PTK7 |
Whole mAb ADC |
||
Pre-Made Coltuximab biosimilar, Whole mAb ADC, Anti-CD19 Antibody: Anti-B4/CVID3 therapeutic antibody |
Coltuximab |
NA |
CD19 |
Whole mAb ADC |
||
Pre-Made Denintuzumab biosimilar, Whole mAb ADC, Anti-CD19 Antibody: Anti-B4/CVID3 therapeutic antibody |
Denintuzumab |
NA |
CD19 |
Whole mAb ADC |
||
Pre-Made Depatuxizumab biosimilar, Whole mAb ADC, Anti-EGFR Antibody: Anti-ERBB/ERRP/HER1/mENA/ERBB1/PIG61/NISBD2 therapeutic antibody |
Depatuxizumab |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Disitamab biosimilar, Whole mAb ADC, Anti-ERBB2/HER2 Antibody: Anti-CD340/neu/MLN 19/NEU/NGL/TKR1/VSCN2 therapeutic antibody |
Disitamab |
NA |
ERBB2 |
Whole mAb ADC |
||
Pre-Made Enapotamab biosimilar, Whole mAb ADC, Anti-AXL Antibody: Anti-ARK/UFO/JTK11/Tyro7 therapeutic antibody |
Enapotamab |
NA |
AXL |
Whole mAb ADC |
||
Pre-Made Enfortumab biosimilar, Whole mAb ADC, Anti-PVRL4/NECTIN4 Antibody: Anti-EDSS1/LNIR/PRR4/nectin-4 therapeutic antibody |
Enfortumab |
NA |
PVRL4 |
Whole mAb ADC |
||
Pre-Made Gemtuzumab biosimilar, Whole mAb ADC, Anti-CD33 Antibody: Anti-p67/SIGLEC3/SIGLEC-3 therapeutic antibody |
Gemtuzumab |
NA |
CD33 |
Whole mAb ADC |
||
Pre-Made Glembatumumab biosimilar, Whole mAb ADC, Anti-GPNMB Antibody: Anti-HGFIN/NMB/PLCA3 therapeutic antibody |
Glembatumumab |
NA |
GPNMB |
Whole mAb ADC |
||
Pre-Made Iladatuzumab biosimilar, Whole mAb ADC, Anti-CD79B Antibody: Anti-AGM6/B29/IGB therapeutic antibody |
Iladatuzumab |
NA |
CD79B |
Whole mAb ADC |
||
Pre-Made Indatuximab biosimilar, Whole mAb ADC, Anti-SDC1 Antibody: Anti-SDC/CD138/SYND1/syndecan therapeutic antibody |
Indatuximab |
NA |
SDC1 |
Whole mAb ADC |
||
Pre-Made Indusatumab biosimilar, Whole mAb ADC, Anti-GUCY2C Antibody: Anti-DIAR6/GC-C/GUC2C/MECILIL/STAR therapeutic antibody |
Indusatumab |
NA |
GUCY2C |
Whole mAb ADC |
||
Pre-Made Inotuzumab biosimilar, Whole mAb ADC, Anti-CD22 Antibody: Anti-SIGLEC2/SIGLEC-2 therapeutic antibody |
Inotuzumab |
NA |
CD22 |
Whole mAb ADC |
||
Pre-Made Labetuzumab biosimilar, Whole mAb ADC, Anti-CEACAM5/CD66e Antibody: Anti-CEA therapeutic antibody |
Labetuzumab |
NA |
CEACAM5 |
Whole mAb ADC |
||
Pre-Made Ladiratuzumab biosimilar, Whole mAb ADC, Anti-SLC39A6 Antibody: Anti-LIV-1/LIV1/ZIP6 therapeutic antibody |
Ladiratuzumab |
NA |
SLC39A6 |
Whole mAb ADC |
||
Pre-Made Laprituximab biosimilar, Whole mAb ADC, Anti-EGFR Antibody: Anti-ERBB/ERRP/HER1/mENA/ERBB1/PIG61/NISBD2 therapeutic antibody |
Laprituximab |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Lifastuzumab biosimilar, Whole mAb ADC, Anti-SLC34A2 Antibody: Anti-NAPI-3B/NAPI-IIb/NPTIIb/PULAM therapeutic antibody |
Lifastuzumab |
NA |
SLC34A2 |
Whole mAb ADC |
||
Pre-Made Lilotomab biosimilar, Whole mAb ADC, Anti-CD37 Antibody: Anti-GP52-40/TSPAN26 therapeutic antibody |
Lilotomab |
NA |
CD37 |
Whole mAb ADC |
||
Pre-Made Loncastuximab biosimilar, Whole mAb ADC, Anti-CD19 Antibody: Anti-B4/CVID3 therapeutic antibody |
Loncastuximab |
NA |
CD19 |
Whole mAb ADC |
||
Pre-Made Lorvotuzumab biosimilar, Whole mAb ADC, Anti-NCAM1 Antibody: Anti-CD56/NCAM/MSK39 therapeutic antibody |
Lorvotuzumab |
NA |
NCAM1 |
Whole mAb ADC |
||
Pre-Made Losatuxizumab biosimilar, Whole mAb ADC, Anti-EGFR Antibody: Anti-ERBB/ERRP/HER1/mENA/ERBB1/PIG61/NISBD2 therapeutic antibody |
Losatuxizumab |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Lupartumab biosimilar, Whole mAb ADC, Anti-LYPD3 Antibody: Anti-C4.4A therapeutic antibody |
Lupartumab |
NA |
LYPD3 |
Whole mAb ADC |
||
Pre-Made Milatuzumab biosimilar, Whole mAb, Anti-CD74 Antibody: Anti-CLIP/DHLAG/HLADG/II/Ia-GAMMA/p33 therapeutic antibody |
Milatuzumab |
NA |
CD74 |
Whole mAb ADC |
||
Pre-Made Mirvetuximab biosimilar, Whole mAb ADC, Anti-FOLR1 Antibody: Anti-FBP/FOLR/FRalpha/NCFTD therapeutic antibody |
Mirvetuximab |
NA |
FOLR1 |
Whole mAb ADC |
||
Pre-Made Naratuximab biosimilar, Whole mAb ADC, Anti-CD37 Antibody: Anti-GP52-40/TSPAN26 therapeutic antibody |
Naratuximab |
NA |
CD37 |
Whole mAb ADC |
||
Pre-Made Pelgifatamab biosimilar, Whole mAb ADC, Anti-FOLH1/GCPII Antibody: Anti-FGCP/FOLH/GCP2/NAALAD1/PSM/PSMA/mGCP therapeutic antibody |
Pelgifatamab |
NA |
FOLH1 |
Whole mAb ADC |
||
Pre-Made Pinatuzumab biosimilar, Whole mAb ADC, Anti-CD22 Antibody: Anti-SIGLEC2/SIGLEC-2 therapeutic antibody |
Pinatuzumab |
NA |
CD22 |
Whole mAb ADC |
||
Pre-Made Polatuzumab biosimilar, Whole mAb ADC, Anti-CD79B Antibody: Anti-AGM6/B29/IGB therapeutic antibody |
Polatuzumab |
NA |
CD79B |
Whole mAb ADC |
||
Pre-Made Rolinsatamab biosimilar, Whole mAb ADC, Anti-PRLR Antibody: Anti-HPRL/MFAB/RI-PRLR/hPRLrI therapeutic antibody |
Rolinsatamab |
NA |
PRLR |
Whole mAb ADC |
||
Pre-Made Rovalpituzumab biosimilar, Whole mAb ADC, Anti-DLL3 Antibody: Anti-SCDO1 therapeutic antibody |
Rovalpituzumab |
NA |
DLL3 |
Whole mAb ADC |
||
Pre-Made Sacituzumab biosimilar, Whole mAb ADC, Anti-TACSTD2 Antibody: Anti-EGP-1/EGP1/GA733-1/GA7331/GP50/M1S1/TROP2 therapeutic antibody |
Sacituzumab |
NA |
TACSTD2 |
Whole mAb ADC |
||
Pre-Made Samrotamab biosimilar, Whole mAb ADC, Anti-LRRC15 Antibody: Anti-LIB therapeutic antibody |
Samrotamab |
NA |
LRRC15 |
Whole mAb ADC |
||
Pre-Made Serclutamab biosimilar, Whole mAb ADC, Anti-EGFR Antibody: Anti-ERBB/ERRP/HER1/mENA/ERBB1/PIG61/NISBD2 therapeutic antibody |
Serclutamab |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Sirtratumab biosimilar, Whole mAb ADC, Anti-SLITRK6 Antibody: Anti-DFNMYP therapeutic antibody |
Sirtratumab |
NA |
SLITRK6 |
Whole mAb ADC |
||
Pre-Made Sofituzumab biosimilar, Whole mAb ADC, Anti-MUC16 Antibody: Anti-CA125 therapeutic antibody |
Sofituzumab |
NA |
MUC16 |
Whole mAb ADC |
||
Pre-Made Tabituximab biosimilar, Whole mAb ADC, Anti-FZD10 Antibody: Anti-CD350/FZ-10/Fz10/FzE7/hFz10 therapeutic antibody |
Tabituximab |
NA |
FZD10 |
Whole mAb ADC |
||
Pre-Made Tamrintamab biosimilar, Whole mAb ADC, Anti-DPEP3 Antibody: Anti-MBD3 therapeutic antibody |
Tamrintamab |
NA |
DPEP3 |
Whole mAb ADC |
||
Pre-Made Telisotuzumab biosimilar, Whole mAb ADC, Anti-MET Antibody: Anti-AUTS9/DFNB97/HGFR/RCCP2/c-Met therapeutic antibody |
Telisotuzumab |
NA |
MET |
Whole mAb ADC |
||
Pre-Made Vadastuximab biosimilar, Whole mAb ADC, Anti-CD33 Antibody: Anti-p67/SIGLEC3/SIGLEC-3 therapeutic antibody |
Vadastuximab |
NA |
CD33 |
Whole mAb ADC |
||
Pre-Made Vandortuzumab biosimilar, Whole mAb ADC, Anti-STEAP1 Antibody: Anti-PRSS24/STEAP therapeutic antibody |
Vandortuzumab |
NA |
STEAP1 |
Whole mAb ADC |
||
Pre-Made Vorsetuzumab biosimilar, Whole mAb ADC, Anti-CD70/CD27-L Antibody: Anti-CD27L/LPFS3/CD27LG/TNFSF7/TNLG8A therapeutic antibody |
Vorsetuzumab |
NA |
CD70 |
Whole mAb ADC |
||
Pre-Made Tabituximab Barzuxetan Biosimilar, Whole Mab Adc, Anti-Fzd10 Antibody: Anti-CD350/FZ-10/Fz10/FzE7/hFz10 therapeutic antibody Drug Conjugate |
tabituximab barzuxetan |
NA |
FZD10 |
Whole mAb ADC |
||
Pre-Made Tamrintamab Pamozirine Biosimilar, Whole Mab Adc, Anti-Dpep3 Antibody: Anti-MBD3 therapeutic antibody Drug Conjugate |
tamrintamab pamozirine |
NA |
DPEP3 |
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
