Development of potent monoclonal antibody auristatin conjugates for cancer therapy

SO Doronina, BE Toki, MY Torgov… - Nature …, 2003 - nature.com
We describe the in vitro and in vivo properties of monoclonal antibody (mAb)-drug
conjugates consisting of the potent synthetic dolastatin 10 analogs auristatin E (AE) and …

Highly potent monomethyl auristatin E prodrug activated by caspase-3 for the chemoradiotherapy of triple-negative breast cancer

SW Chung, YS Cho, JU Choi, HR Kim, TH Won… - Biomaterials, 2019 - Elsevier
Despite the emergence of advanced therapeutics such as targeted therapy and
immunotherapy in the modern oncology, cytotoxic chemotherapy still remains as the first-line …

[HTML][HTML] Whole-body pharmacokinetics and physiologically based pharmacokinetic model for monomethyl auristatin E (MMAE)

HP Chang, YK Cheung, DK Shah - Journal of Clinical Medicine, 2021 - mdpi.com
Monomethyl auristatin E (MMAE) is one of the most commonly used payloads for developing
antibody–drug conjugates (ADC). However, limited studies have comprehensively …

Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin αvβ6 Binding Peptide–Drug Conjugate for Tumor Targeted Drug Delivery

RA Davis, T Ganguly, R Harris… - Journal of Medicinal …, 2023 - ACS Publications
Many anticancer drugs exhibit high systemic off-target toxicities causing severe side effects.
Peptide–drug conjugates (PDCs) that target tumor-specific receptors such as integrin αvβ6 …

Synthesis, characterization, and preclinical evaluation of a small-molecule prostate-specific membrane antigen-targeted monomethyl auristatin E conjugate

AE Machulkin, AA Uspenskaya, NU Zyk… - Journal of Medicinal …, 2021 - ACS Publications
Prostate cancer is the second most common type of cancer among men. Its main method of
treatment is chemotherapy, which has a wide range of side effects. One of the solutions to …

Non-clinical pharmacokinetics of XMT-1522, a HER2 targeting auristatin-based antibody drug conjugate

A Yurkovetskiy, D Gumerov, E Ter-Ovanesyan… - Cancer Research, 2017 - AACR
The ADC XMT-1522 consists of a novel human IgG1 anti-HER2 monoclonal antibody and a
novel, auristatin-based cytotoxic payload (Auristatin F-hydroxypropylamide, AF-HPA). An …

Site-specific conjugation of monomethyl auristatin E to anti-CD30 antibodies improves their pharmacokinetics and therapeutic index in rodent models

F Lhospice, D Brégeon, C Belmant… - Molecular …, 2015 - ACS Publications
Antibody–drug conjugates (ADCs) have demonstrated clinical benefits that have led to the
recent FDA approval of KADCYLA and ADCETRIS. Most ADCs that are currently in clinical …

[HTML][HTML] Pharmacokinetic and metabolism studies of monomethyl auristatin F via liquid chromatography-quadrupole-time-of-flight mass spectrometry

MH Park, BI Lee, JJ Byeon, SH Shin, J Choi, Y Park… - Molecules, 2019 - mdpi.com
A simple liquid chromatography–quadrupole-time-of-flight–mass spectrometric assay (LC-
TOF-MS/MS) has been developed for the evaluation of metabolism and pharmacokinetic …

[HTML][HTML] Structural basis of microtubule destabilization by potent auristatin anti-mitotics

AB Waight, K Bargsten, S Doronina, MO Steinmetz… - PloS one, 2016 - journals.plos.org
The auristatin class of microtubule destabilizers are highly potent cytotoxic agents against
several cancer cell types when delivered as antibody drug conjugates. Here we describe the …

Dual intra-and extracellular release of monomethyl auristatin E from a neutrophil elastase-sensitive antibody-drug conjugate

IAM Amar, S Huvelle, E Douez, S Letast… - European Journal of …, 2022 - Elsevier
Antibody-drug conjugates (ADCs) are targeted therapies, mainly used in oncology,
consisting in a three-component molecular architecture combining a highly potent drug …