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berotralstat
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Status:
Possibly Marketed Outside US
Source:
NCT00915733: Phase 4 Interventional Completed Myocardial Infarction
(2009)
Source URL:
Class:
PROTEIN
Status:
Possibly Marketed Outside US
Source:
NCT01595516: Phase 4 Interventional Completed Prehypertension
(2012)
Source URL:
Class:
PROTEIN
Bradykinin, a pro-inflammatory mediator is also a neuromediator and regulator of several vascular and renal functions. Bradykinin can act as a vasoactive substance along with histamine in inflammation and swelling as it is a potent vasodilator. In addition, it triggers the release of other mediators such as nitric oxide in inflammatory and cancer tissues. Bradykinin acts via specific cell surface receptors: bradykinin receptor, B1 and B2 that are G-protein coupled receptors of the seven-transmembrane domain family. It was shown that increased plasma levels of bradykinin lead to the angioedema as the common major clinical manifestation. Bradykinin was also studied in heart transplant recipients and in obesity patients, but these studies were terminated or withdrawn for different reasons. Bradykinin is also an important growth factor for many cancers. Bradykinin antagonists showed higher potency than standard anti-cancer drugs, without evident toxicity to the hosts, that is why they have great promise for the development of new anti-cancer drugs.
Status:
US Approved Rx
(2020)
Source:
NDA214094
(2020)
Source URL:
First approved in 2020
Source:
NDA214094
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Berotralstat (ORLADEYO™; BCX7353) is an orally administered kallikrein inhibitor, which has been developed by BioCryst Pharmaceuticals for hereditary angioedema (HAE). The inhibition of kallikrein by berotralstat decreases the production of bradykinin, which prevents the localised tissue oedema that occurs during attacks of HAE. Berotralstat has been approved in the USA, and subsequently in Japan, for prophylaxis to prevent attacks of HAE in adults and paediatric patients aged 12 years or older.
Status:
US Approved Rx
(2020)
Source:
NDA214094
(2020)
Source URL:
First approved in 2020
Source:
NDA214094
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Berotralstat (ORLADEYO™; BCX7353) is an orally administered kallikrein inhibitor, which has been developed by BioCryst Pharmaceuticals for hereditary angioedema (HAE). The inhibition of kallikrein by berotralstat decreases the production of bradykinin, which prevents the localised tissue oedema that occurs during attacks of HAE. Berotralstat has been approved in the USA, and subsequently in Japan, for prophylaxis to prevent attacks of HAE in adults and paediatric patients aged 12 years or older.