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 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
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