Clinical data | |
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Trade names | Bronica in Japan, Changnuo, Mai Xu Jia, Quan Kang Nuo in China and as Seradair in India. . [1] |
AHFS/ Drugs.com | International Drug Names |
Routes of administration | By mouth ( tablets, granules) |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Protein binding | >96% |
Elimination half-life | 22 hours |
Identifiers | |
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CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
KEGG | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.220.176 |
Chemical and physical data | |
Formula | C22H26O4 |
Molar mass | 354.446 g·mol−1 |
3D model ( JSmol) | |
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(what is this?) (verify) |
Seratrodast (development name, AA-2414; marketed originally as Bronica) [2] is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. [3] [4] It was the first TP receptor antagonist that was developed as an anti-asthmatic drug and received marketing approval in Japan in 1997. [5] As of 2017 seratrodast was marketed as Bronica in Japan, and as Changnuo, Mai Xu Jia, Quan Kang Nuo in China. [1]
Unlike thromboxane synthase inhibitors such as ozagrel, seratrodast does not affect thrombus formation, time to occlusion and bleeding time. [6] Seratrodast has no effect on prothrombin time and activated partial thromboplastin time, thus ruling out any action on blood coagulation cascade. [7]
Seratrodast is used to treat asthma. [8] [9]
There are no adequate and well-controlled studies of seratrodast in pregnant women. The drug should be used in pregnancy only if the potential benefits justify the risk to the fetus. [9] Seratrodast should not be used during lactation. [9]
The safety and efficacy of seratrodast has not been established in children (<18 years of age). [9]
Seratrodast should not be used in people with liver disease. [9]
Use with paracetamol or with cephem antibiotics increases the risk of liver damage. Use with aspirin increases the bioavailability of seratrodast. [9]
The most frequently observed (0.1 to 5%) adverse reactions include elevated transaminases, nausea, loss of appetite, stomach discomfort, abdominal pain, diarrhea, constipation, dry mouth, taste disturbance, drowsiness, headache, dizziness, palpitations and malaise. [9] Less than 0.1% of patients experienced vomiting, thrombocytopenia, epistaxis, bleeding tendency, insomnia, tremor, numbness, hot flushes and edema. [9] All the adverse reactions reported were of mild to moderate severity, and resolved when the drug was discontinued. [9]
Thromboxane A2 (TXA2) is generated in the lungs of people with asthma, and when it signals through the thromboxane receptor it causes bronchoconstriction, vasoconstriction, mucous secretion, and airway hyper-responsiveness. Seratrodast inhibits the activity of the thromboxane receptor, blocking the effects of TXA2. [10]
The pharmacokinetics of seratrodast have been studied in Japanese and Caucasian, including Indian, healthy volunteers. [11] [12] [13] [14] The plasma concentrations of seratrodast increase with increasing doses. The absorption of seratrodast is relatively rapid with maximum plasma concentrations of 4.6–6 μg/ml obtained in 3 to 4 hours. [11] Steady state plasma concentrations of seratrodast are reached within 4–5 days. [13] Seratrodast is slowly cleared, mainly by hepatic biotransformation. The drug shows biexponential decay in plasma profiles with a mean elimination half-life of 22 hours. [11] [13] Approximately 20% of the administered dose is recovered in the urine, with 60% of the urinary recovery being in the form of conjugates [12]
Seratrodast can be prepared in five steps starting from pimelic acid monoester. [15]
Seratrodast was the first thromboxane receptor antagonist to reach the market as a treatment for asthma; it was approved in Japan in 1997. [8]
As of 2017 seratrodast was marketed as Bronica in Japan, Changnuo, Mai Xu Jia, Quan Kang Nuo in China and as Seretra & Seradair in India. [1]
Seratrodast was studied in perennial allergic rhinitis, chronic bronchitis and chronic pulmonary emphysema but efforts to bring the drug to market in those indications was abandoned around 2000. [2]
Clinical data | |
---|---|
Trade names | Bronica in Japan, Changnuo, Mai Xu Jia, Quan Kang Nuo in China and as Seradair in India. . [1] |
AHFS/ Drugs.com | International Drug Names |
Routes of administration | By mouth ( tablets, granules) |
ATC code | |
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Protein binding | >96% |
Elimination half-life | 22 hours |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
KEGG | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.220.176 |
Chemical and physical data | |
Formula | C22H26O4 |
Molar mass | 354.446 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(what is this?) (verify) |
Seratrodast (development name, AA-2414; marketed originally as Bronica) [2] is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. [3] [4] It was the first TP receptor antagonist that was developed as an anti-asthmatic drug and received marketing approval in Japan in 1997. [5] As of 2017 seratrodast was marketed as Bronica in Japan, and as Changnuo, Mai Xu Jia, Quan Kang Nuo in China. [1]
Unlike thromboxane synthase inhibitors such as ozagrel, seratrodast does not affect thrombus formation, time to occlusion and bleeding time. [6] Seratrodast has no effect on prothrombin time and activated partial thromboplastin time, thus ruling out any action on blood coagulation cascade. [7]
Seratrodast is used to treat asthma. [8] [9]
There are no adequate and well-controlled studies of seratrodast in pregnant women. The drug should be used in pregnancy only if the potential benefits justify the risk to the fetus. [9] Seratrodast should not be used during lactation. [9]
The safety and efficacy of seratrodast has not been established in children (<18 years of age). [9]
Seratrodast should not be used in people with liver disease. [9]
Use with paracetamol or with cephem antibiotics increases the risk of liver damage. Use with aspirin increases the bioavailability of seratrodast. [9]
The most frequently observed (0.1 to 5%) adverse reactions include elevated transaminases, nausea, loss of appetite, stomach discomfort, abdominal pain, diarrhea, constipation, dry mouth, taste disturbance, drowsiness, headache, dizziness, palpitations and malaise. [9] Less than 0.1% of patients experienced vomiting, thrombocytopenia, epistaxis, bleeding tendency, insomnia, tremor, numbness, hot flushes and edema. [9] All the adverse reactions reported were of mild to moderate severity, and resolved when the drug was discontinued. [9]
Thromboxane A2 (TXA2) is generated in the lungs of people with asthma, and when it signals through the thromboxane receptor it causes bronchoconstriction, vasoconstriction, mucous secretion, and airway hyper-responsiveness. Seratrodast inhibits the activity of the thromboxane receptor, blocking the effects of TXA2. [10]
The pharmacokinetics of seratrodast have been studied in Japanese and Caucasian, including Indian, healthy volunteers. [11] [12] [13] [14] The plasma concentrations of seratrodast increase with increasing doses. The absorption of seratrodast is relatively rapid with maximum plasma concentrations of 4.6–6 μg/ml obtained in 3 to 4 hours. [11] Steady state plasma concentrations of seratrodast are reached within 4–5 days. [13] Seratrodast is slowly cleared, mainly by hepatic biotransformation. The drug shows biexponential decay in plasma profiles with a mean elimination half-life of 22 hours. [11] [13] Approximately 20% of the administered dose is recovered in the urine, with 60% of the urinary recovery being in the form of conjugates [12]
Seratrodast can be prepared in five steps starting from pimelic acid monoester. [15]
Seratrodast was the first thromboxane receptor antagonist to reach the market as a treatment for asthma; it was approved in Japan in 1997. [8]
As of 2017 seratrodast was marketed as Bronica in Japan, Changnuo, Mai Xu Jia, Quan Kang Nuo in China and as Seretra & Seradair in India. [1]
Seratrodast was studied in perennial allergic rhinitis, chronic bronchitis and chronic pulmonary emphysema but efforts to bring the drug to market in those indications was abandoned around 2000. [2]