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

Target
Filters Sort results
Reset Apply
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
1 2 3