evolocumab   Click here for help

GtoPdb Ligand ID: 7343

Synonyms: AMG-145 | AMG145 | Repatha®
Approved drug
evolocumab is an approved drug (EMA & FDA (2015))
Compound class: Antibody
Comment: Evolocumab is a clinically approved anti-PCSK9 (proprotein convertase subtilisin/kexin type 9) monoclonal antibody. Peptide sequences for this antibody are available from its IMGT/mAb-DB link. The development and discovery of this antibody is described in patent US8030457, where SEQ IDs 23 and 49 comprising clone 21B12 light and heavy chain variable regions respectively, match the peptide sequences in the INN record for evolocumab.
Click here for help

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.

✖

View interactive charts of activity data across species
References
1. Abifadel M, Varret M, Rabès JP, Allard D, Ouguerram K, Devillers M, Cruaud C, Benjannet S, Wickham L, Erlich D et al.. (2003)
Mutations in PCSK9 cause autosomal dominant hypercholesterolemia.
Nat Genet, 34 (2): 154-6. [PMID:12730697]
2. Dubuc G, Chamberland A, Wassef H, Davignon J, Seidah NG, Bernier L, Prat A. (2004)
Statins upregulate PCSK9, the gene encoding the proprotein convertase neural apoptosis-regulated convertase-1 implicated in familial hypercholesterolemia.
Arterioscler Thromb Vasc Biol, 24 (8): 1454-9. [PMID:15178557]
3. Jackson SM, Shan B, Shen W, King CT. 
Antigen binding proteins to proprotein convertase subtilisin kexin type 9 (PCSK9).
Patent number: US8030457. Assignee: Amgen, Inc.. Priority date: 23/08/2007. Publication date: 04/10/2011.
4. Sabatine MS, Giugliano RP, Wiviott SD, Raal FJ, Blom DJ, Robinson J, Ballantyne CM, Somaratne R, Legg J, Wasserman SM et al.. (2015)
Efficacy and safety of evolocumab in reducing lipids and cardiovascular events.
N Engl J Med, 372 (16): 1500-9. [PMID:25773607]
5. Sullivan D, Olsson AG, Scott R, Kim JB, Xue A, Gebski V, Wasserman SM, Stein EA. (2012)
Effect of a monoclonal antibody to PCSK9 on low-density lipoprotein cholesterol levels in statin-intolerant patients: the GAUSS randomized trial.
JAMA, 308 (23): 2497-506. [PMID:23128163]