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Synonyms: 5F9vcMMAE [6] | MLN-0264 | MLN0264 | TAK-264 | TAK264
Compound class:
Antibody
Comment: Indusatumab vedotin was a clinical lead antibody-drug conjugate (ADC). It comprises an anti-guanylate cyclase 2C (GUCY2C) antibody linked to the synthetic antineoplastic toxin monomethyl auristatin E (MMAE, aka vedotin; PubChem CID 11542188).
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. A BLAST search of patented peptide sequences reveals that the heavy and light chain variable regions of indusatumab are identical to SEQ ID NO: 18 and SEQ ID NO: 20 respectively, from patent US8785600 B2 [6]. The patent also describes the toxin conjugation methodology. 
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Almhanna K, Miron ML, Wright D, Gracian AC, Hubner RA, Van Laethem JL, López CM, Alsina M, Muñoz FL, Bendell J et al.. (2017)
Phase II study of the antibody-drug conjugate TAK-264 (MLN0264) in patients with metastatic or recurrent adenocarcinoma of the stomach or gastroesophageal junction expressing guanylyl cyclase C. Invest New Drugs, 35 (2): 235-241. [PMID:28188407] |
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2. Almhanna K, Wright D, Mercade TM, Van Laethem JL, Gracian AC, Guillen-Ponce C, Faris J, Lopez CM, Hubner RA, Bendell J et al.. (2017)
A phase II study of antibody-drug conjugate, TAK-264 (MLN0264) in previously treated patients with advanced or metastatic pancreatic adenocarcinoma expressing guanylyl cyclase C. Invest New Drugs, 35 (5): 634-641. [PMID:28527133] |
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3. Birbe R, Palazzo JP, Walters R, Weinberg D, Schulz S, Waldman SA. (2005)
Guanylyl cyclase C is a marker of intestinal metaplasia, dysplasia, and adenocarcinoma of the gastrointestinal tract. Hum Pathol, 36 (2): 170-9. [PMID:15754294] |
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4. Carrithers SL, Barber MT, Biswas S, Parkinson SJ, Park PK, Goldstein SD, Waldman SA. (1996)
Guanylyl cyclase C is a selective marker for metastatic colorectal tumors in human extraintestinal tissues. Proc Natl Acad Sci USA, 93 (25): 14827-32. [PMID:8962140] |
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5. Lucas KA, Pitari GM, Kazerounian S, Ruiz-Stewart I, Park J, Schulz S, Chepenik KP, Waldman SA. (2000)
Guanylyl cyclases and signaling by cyclic GMP. Pharmacol Rev, 52 (3): 375-414. [PMID:10977868] |
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6. Nam SS, Greenfield EA, O'Keefe TL, Qin S, Babcock J. (2014)
Anti-GCC antibody molecules and related compositions and methods. Patent number: US8785600 B2. Assignee: Millennium Pharmaceuticals, Inc., Amgen British Columbia. Priority date: 23/10/2009. Publication date: 22/07/2014. |
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7. Schulz S, Hyslop T, Haaf J, Bonaccorso C, Nielsen K, Witek ME, Birbe R, Palazzo J, Weinberg D, Waldman SA. (2006)
A validated quantitative assay to detect occult micrometastases by reverse transcriptase-polymerase chain reaction of guanylyl cyclase C in patients with colorectal cancer. Clin Cancer Res, 12 (15): 4545-52. [PMID:16899600] |
