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Synonyms: AB0024 | GS 6624 | GS-6624
Compound class:
Antibody
Comment: Simtuzumab is an investigational monoclonal antibody targeting lysyl oxidase-like 2 (LOXL2). The antibody is reported to be an allosteric modulator of LOXL2 enzymatic activity [6-7].
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. Peptide sequence matches reveal that US8461303 is the covering patent [7]. The heavy chain variable domain sequence of simtuzumab (from IMGT) matches the sequence for the AB0023 M20 variant 3 clone in US8461303. 
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. ✖ |
| No information available. |
Summary of Clinical Use  |
| Simtuzumab is being evaluated in Phase 2 clinical trials for the fibrotic diseases nonalcoholic steatohepatitis (NASH), primary sclerosing cholangitis and idiopathic pulmonary fibrosis (IPF) [1]. |
| Mechanism Of Action and Pharmacodynamic Effects |
| Simtuzumab reduces the development of fibrotic lesions by inhibiting the enzyme responsible for the final enzymatic step in the formation of crosslinks in collagens and elastin required for biogenesis of connective tissue. Up-regulation of this enzyme, LOXL2, is associated with poorer prognosis in some types of cancer [2,4-5,8], and is involved in fibrosis [3,9]. |
