Toxins/Payloads (Classification and function) of Microtubule destroying drug

SOCAIL MEDIA

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

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.

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.

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.

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.

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.

Product List

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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
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