monomethyl auristatin E

Also Known As:

MMAE peptide; monomethylauristatin E; N-methyl-L-valyl-N-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1-methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-L-valinamide

Networked: 170 relevant articles (21 outcomes, 21 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Amino Acids, Peptides, and Proteins: 1
- Peptides: 82426
  - Oligopeptides: 519
    - monomethyl auristatin E: 170

Experts

1.	Otlewski, Jacek: 6 articles (12/2021 - 01/2016)
2.	Senter, Peter D: 6 articles (08/2007 - 07/2003)
3.	Neri, Dario: 5 articles (01/2021 - 01/2017)
4.	Polakis, Paul: 5 articles (01/2021 - 02/2004)
5.	Firestein, Ron: 5 articles (01/2017 - 03/2011)
6.	Cazzamalli, Samuele: 4 articles (01/2021 - 01/2017)
7.	Fang, Jianmin: 4 articles (01/2021 - 08/2015)
8.	Doronina, Svetlana O: 4 articles (04/2006 - 07/2003)
9.	Meyer, Damon L: 4 articles (04/2006 - 07/2003)
10.	Wahl, Alan F: 4 articles (04/2006 - 07/2003)

Related Diseases

1.	Neoplasms (Cancer) 12/01/2020 - "An anti-MUC1 ADC was synthesized by conjugating GSTA neoantigen-specific 16A with monomethyl auristatin E (MMAE), which displayed potent antitumoral efficacy with an IC50 ranging 0.2-49.4 nM toward various cancer cells. " 10/20/2023 - "Among these ADCs, the use of monomethyl auristatin E (MMAE) as a payload is prevalent in the development of ADC drugs, which has significantly improved overall therapeutic efficacy against various malignancies. " 01/01/2021 - "Similarly, a conjugate of OncoFAP with the monomethyl auristatin E-based Vedotin payload was well tolerated and cured tumor-bearing mice in combination with a clinical-stage antibody-interleukin-2 fusion. " 10/01/2021 - "Conjugation with fluorescence labels and monomethyl auristatin E (MMAE) was used to study their intracellular trafficking and anti-cancer effects, respectively. " 11/01/2020 - "A Phase I Study of DLYE5953A, an Anti-LY6E Antibody Covalently Linked to Monomethyl Auristatin E, in Patients with Refractory Solid Tumors."
2.	Non-Hodgkin Lymphoma (Lymphosarcoma) 01/01/2020 - "A two-analyte integrated population pharmacokinetic (PK) model that simultaneously describes concentrations of antibody-conjugated monomethyl auristatin E (acMMAE) and unconjugated MMAE following repeated administrations of polatuzumab vedotin (pola) was developed based on data from four clinical studies of pola in patients with non-Hodgkin lymphoma. " 10/01/2016 - "In this study, HB22.7, an anti-CD22 monoclonal antibody, was used for specific, targeted delivery of monomethyl auristatin E (MMAE) to non-Hodgkin lymphoma (NHL). " 01/01/2017 - "Polatuzumab vedotin, an antibody-drug conjugate containing monomethyl auristatin E, was associated with an incidence of grade ≥2 peripheral neuropathy (PN) of 55-72% in patients with indolent non-Hodgkin lymphoma in a phase II study, when dosed 1.8-2.4 mg/kg every 3 weeks until progression or for a maximum of 17 cycles. " 01/01/2021 - "We are interested in developing a second generation of antibody-drug conjugates (ADCs) for the treatment of non-Hodgkin lymphoma (NHL) that could provide a longer duration of response and be more effective in indolent NHL than the microtubule-inhibiting ADCs pinatuzumab vedotin [anti-CD22-vc-monomethyl auristatin E (MMAE)] and polatuzumab vedotin (anti-CD79b-vc-MMAE). " 01/01/2018 - "In this study, the ADC, Rituximab-monomethyl auristatin E (MMAE) with a Valine-Citrulline cleavable linker, was designed to investigate its therapeutic efficacy against non-Hodgkin lymphoma (NHL) as well as the underlying mechanisms. "
3.	Melanoma (Melanoma, Malignant) 01/19/2021 - "Monomethyl auristatin E, a cytotoxic part of NECTIN4-targeted antibody-drug conjugate, was effective for BRAF-mutated or BRAFi-resistant melanoma cells. " 03/01/2011 - "When conjugated with monomethyl auristatin E, the antibody-drug conjugate (ADC) showed remarkable efficacy against human melanoma cell lines and xenograft tumor models that was commensurate with levels of receptor expression. " 03/01/2011 - "Second, antibodies were raised to the receptor, conjugated with monomethyl auristatin E, and tested for efficacy against melanoma tumor models generated from cell lines. " 08/01/2007 - "Our prior study characterized a fully human antibody to GPNMB covalently linked to monomethylauristatin E, CR011-vcMMAE, and further demonstrated cell surface staining of melanoma lines susceptible to the immunoconjugate's cytotoxicity (Clin Cancer Res 2005; 12(4): 1373-1382). " 06/01/2010 - "High expression of glycoprotein-NMB (GPNMB) in cutaneous melanomas led to the development of CDX-011 (glembatumumab vedotin), a fully human monoclonal antibody against the extracellular domain of GPNMB conjugated to the cytotoxic microtubule toxin monomethylauristatin E. "
4.	Breast Neoplasms (Breast Cancer) 06/01/2014 - "This platform also significantly improved efficacy of the chemotherapeutic monomethylauristatin E (MMAE) in both MDA-MB-231 orthotopic human and syngeneic Py230 murine breast tumors. " 04/06/2015 - "In this study, we investigate the efficacy of pHLIP to target and deliver the highly potent and clinically validated microtubule inhibitor monomethyl auristatin E (MMAE) to cancer cells and breast tumors. " 04/06/2015 - "Inhibition of cancer cell proliferation and breast tumor targeting of pHLIP-monomethyl auristatin E conjugates." 01/01/2022 - "We previously described PVRL4/nectin-4 as a new therapeutic target in breast cancer and produced an efficient EV-like ADC comprising a human anti-nectin-4 mAb conjugated to monomethyl auristatin-E (MMAE) named N41mab-vcMMAE. " 01/01/2020 - "These ADCs are composed of trastuzumab, an antibody targeting HER2 receptors overexpressed on breast cancer cells, and monomethyl auristatin E (MMAE) as a drug payload. "
5.	Stomach Neoplasms (Stomach Cancer) 01/01/2016 - "An anti-HER2 antibody conjugated with monomethyl auristatin E is highly effective in HER2-positive human gastric cancer." 01/01/2016 - "This study assessed antitumor activity of ADC with an antimitotic agent, monomethyl auristatin E (MMAE) and a humanized monoclonal anti-HER2 antibody, hertuzumab, in gastric cancer. " 11/29/2023 - "The conjugation of B9 with a potent cytotoxic agent, monomethyl auristatin E (MMAE), exhibited superior antitumor efficacy against CEACAM5-expressing human gastric cancer cell line MKN-45, human pancreatic carcinoma cell line BxPC-3 and human colorectal cancer cell line LS174T with IC50 values of 38.14, 25.60, and 101.4 nM, respectively. " 01/01/2019 - "We have developed antibody-drug conjugates (ADCs), comprising IgG1 linked via valine-citrulline to monomethyl auristatin E, with potential to treat HER2-positive gastric cancer in humans. "

Related Drugs and Biologics

1.	Immunoconjugates (Immunoconjugate)
2.	Valine (L-Valine)
3.	Citrulline
4.	Monoclonal Antibodies
5.	Brentuximab Vedotin
6.	polatuzumab vedotin
7.	Antibodies
8.	Rituximab (Mabthera)
9.	Cytotoxins (Cytolysins)
10.	Prodrugs

Related Therapies and Procedures

1.	Drug Therapy (Chemotherapy)
2.	Therapeutics
3.	Chemoradiotherapy
4.	Castration
5.	Stem Cell Transplantation