Sebetralstat (Sebetralstat)-Ekterly instruction manual Chinese introduction

1. Common names:Sebetralstat, Ekterly

Drug aliases: sebetrastat, sebetrastat, sebetrastat, sebetrastat (transliteration)

2. Who can use sebetrostat? Indications?

Sebetralstat - Ekterly is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adults and children 12 years of age and older.

3. What are the side effects of sebetrostat?

In clinical studies of sebetrostat, the most common side effect was headache.

4. How should Sabetrostat be used?

Once an acute attack of HAE is diagnosed, the recommended dose is 600 mg (2 tablets) orally; if the patient responds poorly or the symptoms continue to worsen or relapse 3 hours after taking the first dose, a second dose of 600 mg (2 tablets) can be taken orally; within 24 hours, the maximum dose of this product is 1200 mg orally.

5. How to store sebetrostat?

Sebetrostat is available as an oral 300 mg film-coated tablet. Each tablet contains the active ingredient sebetralstat. Store at 20°C to 25°C (68°F to 77°F). Excursions allowed between 15°C and 30°C (59°F to 86°F).

6. How does Sebetrostat work?

Sebetralstat is a competitive, reversible inhibitor of plasma kallikrein. Plasma kallikrein is a serine protease that cleaves high molecular weight kininogen (HK) to release bradykinin, which increases vascular permeability by activating bradykinin receptors that cause edema. Sebetralstat inhibits the cleavage of HK and reduces the production of bradykinin, thereby treating the clinical symptoms of acute HAE attacks. Sebetralstat also inhibits the positive feedback mechanism of the kallikrein system through plasma kallikrein, thereby reducing factor XIIa and additional plasma kallikrein production.

Pharmacodynamics: Concentration-dependent inhibition of plasma kallikrein, measured as a decrease in specific enzyme activity from baseline, was observed in exploratory trials. Following a single oral dose of 600 mg sebetralstat to healthy subjects, a mean inhibition of plasma kallikrein activity of greater than 90% was observed beginning 30 minutes post-dose and maintained for approximately 6 hours post-dose.

Reference materials:https://www.ekterly.com/