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Synonyms: BCX-7353 | BCX7353 | Orladeyo®
berotralstat is an approved drug (FDA (2020), EMA (2021))
Compound class: Synthetic organic
Comment: Berotralstat (BCX7353) is an orally bioavailable inhibitor of plasma kallikrein, a proteinase that is encoded by the KLKB1 gene in humans . Plasma kallikrein cleaves Lys-Arg and Arg-Ser bonds in (human) kininogen to release bradykinin. Inhibition of this activity is exploited to reduce bradykinin levels in human disease where abnormally elevated bradykinin induces pathologic vascular permeability and swelling, as seen in patients with hereditary angioedema (HAE; caused by loss of C1 inhibitor SERPING1 expression).
The 'flat' structure of berotralstat with no specified stereochemistry is claimed as compound 52h in Biocryst Pharmaceuticals' patent WO2015134998A1 .
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.✖
|No information available.
|Summary of Clinical Use
|Berotralstat (BCX7353) was the first oral, once-daily drug to be approved as a prophylactic to prevent hereditary angioedema (HAE) attacks . EMA orphan designation for HAE was granted in June 2018 . In November 2020 the UK's MHRA authorised early access to berotralstat, to allow HAE patients to receive the drug prior to full regulatory approval. Full EMA approval was issued in April 2021.
|Clinical Trial ID
|Study to Evaluate the Efficacy and Safety of BCX7353 as an Oral Treatment for the Prevention of HAE Attacks in Japan
|Phase 3 Interventional
|Efficacy and Safety Study of BCX7353 as an Oral Treatment for the Prevention of Attacks in HAE
|Phase 3 Interventional
|Efficacy and Safety of BCX7353 to Prevent Angioedema Attacks in Subjects With Hereditary Angioedema
|Phase 2 Interventional