Synonyms: CSL-312 | CSL312
Compound class:
Antibody
Comment: Garadacimab (CSL312) is a fully-human monoclonal antibody that inhibits activated factor XII (FXIIa) [3]. Peptide sequence alignments suggest that CSL312 may be the antibody referred to as VR115 in CSL Behring patent US9856325B2 [2]. Activation of FXII initiates the kallikrein-kinin cascade that drives hereditary angioedema (HAE) attacks. FXIIa also induces IL-6 and migration of fibroblasts in lung interstitium, promotes inflammation and represents a novel pathological pathway to fibrotic disease progression in idiopathic pulmonary fibrosis (IPF) [1].
![]() 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 |
1. Jaffar J, McMillan L, Wilson N, Panousis C, Hardy C, Cho HJ, Symons K, Glaspole I, Westall G, Wong M. (2022)
Coagulation factor-XII induces interleukin-6 by primary lung fibroblasts: a role in idiopathic pulmonary fibrosis?. Am J Physiol Lung Cell Mol Physiol, 322 (2): L258-L272. [PMID:34873957] |
2. Panousis C, Rayznam V, Nash A, Wilson M, Schmidbauer S, Nolte M. (2018)
Nucleic acids encoding inhibitory anti-factor XII/XIIa monoclonal antibodies. Patent number: US9856325B2. Assignee: CSL Ltd, CSL Behring GmbH Deutschland. Priority date: 04/11/2016. Publication date: 04/06/2024. |
3. Pawaskar D, Chen X, Glassman F, May F, Roberts A, Biondo M, McKenzie A, Nolte MW, Jusko WJ, Tortorici M. (2022)
Pharmacokinetic/pharmacodynamic modeling for dose selection for the first-in-human trial of the activated Factor XII inhibitor garadacimab (CSL312). Clin Transl Sci, 15 (3): 709-720. [PMID:34811931] |
4. (2023)
Department of Error. Lancet, 401 (10384): 1266. [PMID:37061268] |