Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3 times per day, have been demonstrated to improve clinical end points in diseases responsive to prostacyclin. Oral beraprost therapy improved the survival and pulmonary hemodynamics of patients with primary pulmonary hypertension.1 Beraprost inhibits platelet aggregation in healthy subjects and in diabetic patients at similar doses.2,3
1
Nagaya, N., Uematsu, M., Okano, Y., et al. Effect of orally active prostacyclin analogue on survival of outpatients with primary pulmonary hypertension. J Am Coll Cardiol341188-1192(1999).
2
Nony, P., Ffrench, P., Girard, P., et al. Platelet-aggregation inhibition and hemodynamic effects of beraprost sodium, a new oral prostacyclin derivative: A study in healthy male subjects. Can J Physiol Pharmacol74887-893(1996).
3
Kato, H., Takashima, T., Kishikawa, H., et al. Effect of beraprost sodium, a stable prostaglandin I2 analogue, on platelet aggregation in diabetes mellitus. Int J Clin Pharmacol Res1699-102(1996).
Synonyms
TRK 100
Procyclin
ML 1129
Formal Name
2,3,3a,8b-tetrahydro-2-hydroxy-1-(3-hydroxy-4-methyl-1-octen-6-ynyl)-1H-cyclopenta[b]benzofuran-5-butanoic acid, monosodium salt
Nagaya, N., Uematsu, M., Okano, Y., et al. Effect of orally active prostacyclin analogue on survival of outpatients with primary pulmonary hypertension. J Am Coll Cardiol341188-1192(1999).
Nony, P., Ffrench, P., Girard, P., et al. Platelet-aggregation inhibition and hemodynamic effects of beraprost sodium, a new oral prostacyclin derivative: A study in healthy male subjects. Can J Physiol Pharmacol74887-893(1996).
Kato, H., Takashima, T., Kishikawa, H., et al. Effect of beraprost sodium, a stable prostaglandin I2 analogue, on platelet aggregation in diabetes mellitus. Int J Clin Pharmacol Res1699-102(1996).
Beraprost (sodium salt) is available in the following screening
library: