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Synonyms: 15H6v4.D221 | FHTR2163 | RG-6147 | RG6147 | RO-7171009 | RO7171009
Compound class: Antibody
Comment: Galegenimab is the INN that has been assigned to Genentech's anti-HTRA1 (HtrA serine peptidase 1) Fab antibody . The antibody and its use are claimed in patent WO2017075212A1 . HTRA1 is a serine protease whose substrates include transforming growth factor β [1,5], fibronectin, amyloid precursor protein  and Dickkop-related protein 3 (DKK3) . Genetic polymorphisms in the HTRA1 gene are associated with an increased risk of developing neovascular age-related macular degeneration (and geographic atrophy) and with disease progression. Thus inhibition of HTRA1 proteolytic activity is being investigated for this ocular indication.
Ligand Activity Visualisation Charts
These 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.✖
1. Beaufort N, Scharrer E, Kremmer E, Lux V, Ehrmann M, Huber R, Houlden H, Werring D, Haffner C, Dichgans M. (2014)
Cerebral small vessel disease-related protease HtrA1 processes latent TGF-β binding protein 1 and facilitates TGF-β signaling.
Proc Natl Acad Sci U S A, 111 (46): 16496-501. [PMID:25369932]
2. Grau S, Baldi A, Bussani R, Tian X, Stefanescu R, Przybylski M, Richards P, Jones SA, Shridhar V, Clausen T et al.. (2005)
Implications of the serine protease HtrA1 in amyloid precursor protein processing.
Proc Natl Acad Sci U S A, 102 (17): 6021-6. [PMID:15855271]
3. Kelley RF, Kirchhofer DK, Lai J, Lee CV, Liang X-C, Lipari MT, Loyet KM, Sai T, Van Lookeren Campagne M, Wu Y et al.. (2017)
Anti-htra1 antibodies and methods of use thereof.
Patent number: WO2017075212A1. Assignee: Genentech, Hoffmann-La Roche. Priority date: 30/10/2015. Publication date: 04/05/2017.
4. Khanani AM, Hershberger VS, Pieramici DJ, Khurana RN, Brunstein F, Ma L, Maass KF, Honigberg LA, Tom I, Chen H et al.. (2021)
Phase 1 Study of the Anti-HtrA1 Antibody-binding Fragment FHTR2163 in Geographic Atrophy Secondary to Age-related Macular Degeneration.
Am J Ophthalmol, 232: 49-57 [Epub ahead of print]. [PMID:34214452]
5. Oka C, Tsujimoto R, Kajikawa M, Koshiba-Takeuchi K, Ina J, Yano M, Tsuchiya A, Ueta Y, Soma A, Kanda H et al.. (2004)
HtrA1 serine protease inhibits signaling mediated by Tgfbeta family proteins.
Development, 131 (5): 1041-53. [PMID:14973287]
6. Tom I, Pham VC, Katschke Jr KJ, Li W, Liang WC, Gutierrez J, Ah Young A, Figueroa I, Eshghi ST, Lee CV et al.. (2020)
Development of a therapeutic anti-HtrA1 antibody and the identification of DKK3 as a pharmacodynamic biomarker in geographic atrophy.
Proc Natl Acad Sci U S A, 117 (18): 9952-9963. [PMID:32345717]