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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 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):
– 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
