Toxins/Payloads (Classification and function) of DNA damage drugs

SOCAIL MEDIA

There are so many payloads, like MMAE, Calicheamicin, MMAF, DM1, SN-38 and Dxd.

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.

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.

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.

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.

Product List

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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
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