galegenimab   Click here for help

GtoPdb Ligand ID: 11759

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 [6]. The antibody and its use are claimed in patent WO2017075212A1 [3]. HTRA1 is a serine protease whose substrates include transforming growth factor β [1,5], fibronectin, amyloid precursor protein [2] and Dickkop-related protein 3 (DKK3) [4]. 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.
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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]