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Main elements of antibody-drug conjugate (ADC): Toxins/Payloads (Classification and function)
Virus-like particles (VLP) Platforms for immunogens, vaccines and drug carriers
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
There are so many payloads, like MMAE, Calicheamicin, MMAF, DM1, SN-38 and Dxd.
Microtubule destroying drug
1. Calendula
Auristatins is an important payload used in ADC. The most famous family member MMAE exists in two listed drugs, adcetris and Polivy. At present, more than 10 kinds of ADCs with calendula (such as MMAE) or methylcalendula f (MMAF) as payload are undergoing clinical trials.
The figure above describes auristatine and its common connection sites. The structure-activity relationship (SAR) of Calendula has been widely studied, mainly focusing on the terminal subunit: P1 (N-terminal) and P5 (C-terminal). The most common method is to introduce carbamate function on P1.
2. Meidengsu derivatives (DM2, DM4)
Metanthin is a very effective inhibitor of microtubule assembly, which can induce the cessation of cell mitosis. However, this structure is difficult to conjugate because it has no reactive functional groups. In order to overcome this problem, a series of very effective derivatives containing SME groups have been created. The first examples of such molecules are DM1 and DM4, which carry methylthiopropionyl rather than natural N-acetyl groups.
3. Microtubule lysin
Tubulysins is an effective inhibitor of microtubule polymerization, which can lead to the rapid disintegration of the cytoskeleton of dividing cells and apoptosis. They are a naturally occurring tetrapeptide family containing Mep, Ile, Tuv and Tut, R3 = OH or Tup, R3 = H.
4. Cryptomyxin
Cryptomyxin (CR) is a family of six membered macrocyclic dipeptides with antitumor activity. The results of existing clinical trials show that the toxicity level is unacceptable at the dose required to achieve the therapeutic effect.
5. Anti-mitotic Eg5 inhibitor
Spindle kinesin (KSP, also known as Eg5 or kif11) is an ATP dependent motor protein involved in the separation of cell cycle centrosomes. Therefore, blocking this important event in mitosis with KSP inhibitors (kspis) can produce antitumor efficacy.
DNA damage drugs
1. Pyrrole benzodiazepines and indole chlorobenzodiazepines
Pyrrolo [2,1-c] [1,4] benzodiazepine (PBD) is a natural product with antitumor activity. Their mode of action is selective alkylation in small grooves of DNA, in which the N2 of guanine forms a covalent bond with the electrophilic N10 / C11 imine on PBD.
2. Ducamycin
Ducamycin is a powerful cytotoxic substance. It binds to the small groove of DNA through its highly active cyclopropane ring and alkylates adenine at N3 position. The non cyclized, halomethyl form of ducamycin significantly reduced its cytotoxic activity. Because the phenol group in the molecule can be used as the racemic activator to form electrophilic cyclopropane, the ligation strategy in the development of ducamycin ADC focuses on the linker ligation of phenol functional groups.
3. Camptothecin
Camptothecin (CPT) and its derivatives are classic examples of topoisomerase I inhibitors. They stabilize DNA single strand breaks induced by topoisomerase, and DNA double strand breaks occur when the ternary dna-top1-inhibitor complex encounters the replication fork. Natural camptothecin is a five ring structure. Its very low solubility prevents its wide application as a cancer therapeutic drug. Irinotecan, its water-soluble prodrug, has been licensed for the marketing of metastatic colorectal cancer. SN-38 is an active metabolite of irinoteptan. It is produced in vivo by the action of human liver carboxylesterase, which can be inactivated by opening the lactone ring.
4. Kajimycin
Kajimycin is a widely studied class of enediyne antibiotics. Its structure and mechanism of action are particularly interesting and complex, making it a class of antibiotics in the field of ADC payload. The strategy of connecting calicheamicin in ADC takes ADC Mylotarg in the market as an example, and besponsa.
Innovative drugs
1. Apoptosis inducer (BCL XL inhibitor)
Overexpression of anti apoptotic Bcl-2 family members (including BCL XL) is one of the mechanisms for cancer cells to obtain apoptosis resistance. Drugs that block the BH3 binding domain on BCL XL can trigger cancer cell apoptosis.
2. Telanstadine and its analogues
Targeted spliceosome is a large ribonucleoprotein complex involved in mRNA processing, which provides a promising treatment option for targeted cancer therapy. Several natural products can inhibit RNA splicing by binding to different splice subunits. The most representative is thailanstatin A, which can bind to the SF3B subunit of spliceosome to prevent RNA splicing.
3. Amanita toxin
In the field of ADC technology, the use of transcription inhibitors similar to Amatoxins is a relatively new method. Nine naturally occurring amatoxin derivatives have the same skeleton structure. A macrocycle composed of eight L-configuration amino acids is partially connected between tryptophan and cysteine residues by sulfoxide. The three side chains of Amatoxins are hydroxylated, and the OH group has good water solubility and binds to the target molecule. Two peptides, α- Amanita glycoprotein and β- Amanita toxin accounts for 90% of all toxins.
4. Nicotinamide phosphoribosyltransferase
Nicotinamide phosphoribosyltransferase (Nampt) is an enzyme responsible for converting nicotinamide to nicotinamide mononucleotide. Its inhibitor has shown effectiveness in various preclinical and clinical studies, but its clinical application is limited by targeted toxicity and dose limiting toxicity, such as thrombocytopenia and gastrointestinal adverse reactions.
5. Camamycin
Two new protease inhibitors, camamycin A and camamycin B, were isolated from Curacao bacteria.
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Cat No. | Products Name (INN Index) | INN Name | Previous Name | Target | Format | Order |
|---|---|---|---|---|---|---|
Pre-Made Telimomab Aritox Biosimilar, Whole Mab Adc, Anti-Cd5 Antibody: Anti-LEU1/T1 therapeutic antibody |
telimomab aritox |
NA |
CD5 |
ADC |
||
Pre-Made Telisotuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Met Antibody: Anti-AUTS9/DFNB97/HGFR/RCCP2/c-Met therapeutic antibody Drug Conjugate |
telisotuzumab vedotin |
NA |
MET |
Whole mAb ADC |
||
Pre-Made Tisotumab Vedotin Biosimilar, Whole Mab Adc, Anti-F3 Antibody: Anti-CD142/TF/TFA therapeutic antibody Drug Conjugate |
tisotumab vedotin |
NA |
F3 |
Whole mAb ADC |
||
Pre-Made Trastuzumab Deruxtecan Biosimilar, Whole Mab Adc, Anti-ERBB2/HER2 Antibody: Anti-CD340/neu/MLN 19/NEU/NGL/TKR1/VSCN2/c-ERB-2/c-ERB2 therapeutic antibody Drug Conjugate |
trastuzumab deruxtecan |
NA |
ERBB2 |
Whole mAb ADC |
||
Pre-Made Trastuzumab Duocarmazine Biosimilar, Whole Mab Adc, Anti-ERBB2/HER2 Antibody: Anti-CD340/neu/MLN 19/NEU/NGL/TKR1/VSCN2/c-ERB-2/c-ERB2 therapeutic antibody Drug Conjugate |
trastuzumab duocarmazine |
NA |
ERBB2 |
Whole mAb ADC |
||
Pre-Made Trastuzumab Emtansine Biosimilar, Whole Mab Adc, Anti-ERBB2/HER2 Antibody: Anti-CD340/neu/MLN 19/NEU/NGL/TKR1/VSCN2/c-ERB-2/c-ERB2 therapeutic antibody Drug Conjugate |
trastuzumab emtansine |
NA |
ERBB2 |
Whole mAb ADC |
||
Pre-Made Tusamitamab Ravtansine Biosimilar, Whole Mab Adc, Anti-CEACAM5/CD66e Antibody: Anti-CEA therapeutic antibody Drug Conjugate |
tusamitamab ravtansine |
NA |
CEACAM5 |
Whole mAb ADC |
||
Pre-Made Upifitamab Rilsodotin Biosimilar, Whole Mab Adc, Anti-Slc34A2 Antibody: Anti-NAPI-3B/NAPI-IIb/NPTIIb/PULAM therapeutic antibody Drug Conjugate |
upifitamab rilsodotin |
NA |
SLC34A2 |
Whole mAb ADC |
||
Pre-Made Vadastuximab Talirine Biosimilar, Whole Mab Adc, Anti-Cd33 Antibody: Anti-SIGLEC-3/SIGLEC3/p67 therapeutic antibody Drug Conjugate |
vadastuximab talirine |
NA |
CD33 |
Whole mAb ADC |
||
Pre-Made Vandortuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Steap1 Antibody: Anti-PRSS24/STEAP therapeutic antibody Drug Conjugate |
vandortuzumab vedotin |
NA |
STEAP1 |
Whole mAb ADC |
||
Pre-Made Vorsetuzumab Mafodotin Biosimilar, Whole Mab Adc, Anti-CD70/CD27-L Antibody: Anti-CD27LG/LPFS3/TNFSF7/TNLG8A therapeutic antibody Drug Conjugate |
vorsetuzumab mafodotin |
NA |
CD70 |
Whole mAb ADC |
||
Pre-Made Zilovertamab Vedotin Biosimilar, Whole Mab Adc, Anti-Ror1 Antibody: Anti-NTRKR1/dJ537F10.1 therapeutic antibody Drug Conjugate |
zilovertamab vedotin |
NA |
ROR1 |
Whole mAb ADC |
||
Pre-Made Zolimomab Aritox Biosimilar, Whole Mab Adc, Anti-Cd5 Antibody: Anti-LEU1/T1 therapeutic antibody |
zolimomab aritox |
NA |
CD5 |
ADC |
||
Pre-Made Actinium (225Ac) Lintuzumab Satetraxetan Biosimilar, Whole Mab Adc, Anti-Cd33 Antibody: Anti-SIGLEC-3/SIGLEC3/p67 therapeutic antibody Drug Conjugate |
actinium (225Ac) lintuzumab satetraxetan |
NA |
CD33 |
Whole mAb ADC |
||
Pre-Made Anetumab Corixetan Biosimilar, Whole Mab Adc, Anti-Msln Antibody: Anti-MPF/SMRP therapeutic antibody Drug Conjugate |
anetumab corixetan |
NA |
MSLN |
Whole mAb ADC |
||
Pre-Made Anetumab Ravtansine Biosimilar, Whole Mab Adc, Anti-Msln Antibody: Anti-MPF/SMRP therapeutic antibody Drug Conjugate |
anetumab ravtansine |
NA |
MSLN |
Whole mAb ADC |
||
Pre-Made Aprutumab Ixadotin Biosimilar, Whole Mab Adc, Anti-Fgfr2 Antibody: Anti-BBDS/BEK/BFR-1/CD332/CEK3/CFD1/ECT1/JWS/K-SAM/KGFR/TK14/TK25 therapeutic antibody Drug Conjugate |
aprutumab ixadotin |
NA |
FGFR2 |
Whole mAb ADC |
||
Pre-Made Azintuxizumab Vedotin Biosimilar, Whole Mab Adc, Anti-SLAMF7/CS1 Antibody: Anti-19A/CD319/CRACC therapeutic antibody Drug Conjugate |
azintuxizumab vedotin |
NA |
SLAMF7 |
Whole mAb ADC |
||
Pre-Made Belantamab Mafodotin Biosimilar, Whole Mab Adc, Anti-Tnfrsf17 Antibody: Anti-BCM/BCMA/CD269/TNFRSF13A therapeutic antibody Drug Conjugate |
belantamab mafodotin |
NA |
TNFRSF17 |
Whole mAb ADC |
||
Pre-Made Brentuximab Vedotin Biosimilar, Whole Mab Adc, Anti-Tnfrsf8 Antibody: Anti-CD30/D1S166E/Ki-1 therapeutic antibody Drug Conjugate |
brentuximab vedotin |
NA |
TNFRSF8 |
Whole mAb ADC |
||
Pre-Made Camidanlumab Tesirine Biosimilar, Whole Mab Adc, Anti-Il2Ra Antibody: Anti-CD25/IDDM10/IL2R/IMD41/TCGFR/p55 therapeutic antibody Drug Conjugate |
camidanlumab tesirine |
NA |
IL2RA |
Whole mAb ADC |
||
Pre-Made Cantuzumab Mertansine 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 anti |
cantuzumab mertansine |
NA |
MUC1 |
Whole mAb ADC |
||
Pre-Made Cantuzumab Ravtansine 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 anti |
cantuzumab ravtansine |
NA |
MUC1 |
Whole mAb ADC |
||
Pre-Made Cetuximab Sarotalocan Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
cetuximab sarotalocan |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Clivatuzumab Tetraxetan 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 an |
clivatuzumab tetraxetan |
NA |
MUC1 |
Whole mAb ADC |
||
Pre-Made Cofetuzumab Pelidotin Biosimilar, Whole Mab Adc, Anti-Ptk7 Antibody: Anti-CCK-4/CCK4 therapeutic antibody Drug Conjugate |
cofetuzumab pelidotin |
NA |
PTK7 |
Whole mAb ADC |
||
Pre-Made Coltuximab Ravtansine Biosimilar, Whole Mab Adc, Anti-Cd19 Antibody: Anti-B4/CVID3 therapeutic antibody Drug Conjugate |
coltuximab ravtansine |
NA |
CD19 |
Whole mAb ADC |
||
Pre-Made Dafsolimab Setaritox Biosimilar, Whole Mab Adc, Anti-Cd3E Antibody: Anti-CD3epsilon/IMD18/T3E/TCRE therapeutic antibody Drug Conjugate |
dafsolimab setaritox |
NA |
CD3E |
Whole mAb ADC |
||
Pre-Made Datopotamab Deruxtecan Biosimilar, Whole Mab Adc, Anti-Tacstd2 Antibody: Anti-EGP-1/EGP1/GA733-1/GA7331/GP50/M1S1/TROP2 therapeutic antibody Drug Conjugate |
datopotamab deruxtecan |
NA |
TACSTD2 |
Whole mAb ADC |
||
Pre-Made Denintuzumab Mafodotin Biosimilar, Whole Mab Adc, Anti-Cd19 Antibody: Anti-B4/CVID3 therapeutic antibody Drug Conjugate |
denintuzumab mafodotin |
NA |
CD19 |
Whole mAb ADC |
||
Pre-Made Depatuxizumab Mafodotin Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
depatuxizumab mafodotin |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Disitamab Vedotin Biosimilar, Whole Mab Adc, Anti-ERBB2/HER2 Antibody: Anti-CD340/neu/MLN 19/NEU/NGL/TKR1/VSCN2/c-ERB-2/c-ERB2 therapeutic antibody Drug Conjugate |
disitamab vedotin |
NA |
ERBB2 |
Whole mAb ADC |
||
Pre-Made Dorlimomab Aritox Biosimilar, Whole Mab Adc: Anti-40S Ribosomal Protein S18 therapeutic antibody |
dorlimomab aritox |
NA |
40S ribosomal protein S18 |
ADC |
||
Pre-Made Enapotamab Vedotin Biosimilar, Whole Mab Adc, Anti-Axl Antibody: Anti-ARK/JTK11/Tyro7/UFO therapeutic antibody Drug Conjugate |
enapotamab vedotin |
NA |
AXL |
Whole mAb ADC |
||
Pre-Made Enfortumab Vedotin Biosimilar, Whole Mab Adc, Anti-PVRL4/NECTIN4 Antibody: Anti-EDSS1/LNIR/PRR4/nectin-4 therapeutic antibody Drug Conjugate |
enfortumab vedotin |
NA |
PVRL4 |
Whole mAb ADC |
||
Pre-Made Farletuzumab Ecteribulin Biosimilar, Whole Mab Adc, Anti-Folr1 Antibody: Anti-FBP/FOLR/FRalpha/NCFTD therapeutic antibody Drug Conjugate |
farletuzumab ecteribulin |
NA |
FOLR1 |
Whole mAb ADC |
||
Pre-Made Gemtuzumab Ozogamicin Biosimilar, Whole Mab Adc, Anti-Cd33 Antibody: Anti-SIGLEC-3/SIGLEC3/p67 therapeutic antibody Drug Conjugate |
gemtuzumab ozogamicin |
NA |
CD33 |
Whole mAb ADC |
||
Pre-Made Glembatumumab Vedotin Biosimilar, Whole Mab Adc, Anti-Gpnmb Antibody: Anti-HGFIN/NMB/PLCA3 therapeutic antibody Drug Conjugate |
glembatumumab vedotin |
NA |
GPNMB |
Whole mAb ADC |
||
Pre-Made Grisnilimab Setaritox Biosimilar, Whole Mab Adc, Anti-Cd7 Antibody: Anti-GP40/LEU-9/TP41/Tp40 therapeutic antibody Drug Conjugate |
grisnilimab setaritox |
NA |
CD7 |
Whole mAb ADC |
||
Pre-Made Iladatuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Cd79B Antibody: Anti-AGM6/B29/IGB therapeutic antibody Drug Conjugate |
iladatuzumab vedotin |
NA |
CD79B |
Whole mAb ADC |
||
Pre-Made Indatuximab Ravtansine Biosimilar, Whole Mab Adc, Anti-Sdc1 Antibody: Anti-CD138/SDC/SYND1/syndecan therapeutic antibody Drug Conjugate |
indatuximab ravtansine |
NA |
SDC1 |
Whole mAb ADC |
||
Pre-Made Indusatumab Vedotin Biosimilar, Whole Mab Adc, Anti-Gucy2C Antibody: Anti-DIAR6/GC-C/GUC2C/MECILIL/STAR therapeutic antibody Drug Conjugate |
indusatumab vedotin |
NA |
GUCY2C |
Whole mAb ADC |
||
Pre-Made Inotuzumab Ozogamicin Biosimilar, Whole Mab Adc, Anti-Cd22 Antibody: Anti-SIGLEC-2/SIGLEC2 therapeutic antibody Drug Conjugate |
inotuzumab ozogamicin |
NA |
CD22 |
Whole mAb ADC |
||
Pre-Made Labetuzumab Govitecan Biosimilar, Whole Mab Adc, Anti-CEACAM5/CD66e Antibody: Anti-CEA therapeutic antibody Drug Conjugate |
labetuzumab govitecan |
NA |
CEACAM5 |
Whole mAb ADC |
||
Pre-Made Ladiratuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Slc39A6 Antibody: Anti-LIV-1/LIV1/ZIP6 therapeutic antibody Drug Conjugate |
ladiratuzumab vedotin |
NA |
SLC39A6 |
Whole mAb ADC |
||
Pre-Made Laprituximab Emtansine Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
laprituximab emtansine |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Lifastuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Slc34A2 Antibody: Anti-NAPI-3B/NAPI-IIb/NPTIIb/PULAM therapeutic antibody Drug Conjugate |
lifastuzumab vedotin |
NA |
SLC34A2 |
Whole mAb ADC |
||
Pre-Made Loncastuximab Tesirine Biosimilar, Whole Mab Adc, Anti-Cd19 Antibody: Anti-B4/CVID3 therapeutic antibody Drug Conjugate |
loncastuximab tesirine |
NA |
CD19 |
Whole mAb ADC |
||
Pre-Made Lonigutamab Ugodotin Biosimilar, Whole Mab Adc, Anti-Igf1R Antibody: Anti-CD221/IGFIR/IGFR/JTK13 therapeutic antibody Drug Conjugate |
lonigutamab ugodotin |
NA |
IGF1R |
Whole mAb ADC |
||
Pre-Made Lorvotuzumab Mertansine Biosimilar, Whole Mab Adc, Anti-Ncam1 Antibody: Anti-CD56/MSK39/NCAM therapeutic antibody Drug Conjugate |
lorvotuzumab mertansine |
NA |
NCAM1 |
Whole mAb ADC |
View the Knowledge base of Antibody-drug Conjugate (ADC):
– The Landscape of Antibody-drug Conjugate (ADC): Production, Mechanisms of Action (MOA), FDA approved-antibodies, and Functional assay
– 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
– 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
