Terguride
Systematic (IUPAC) name
N,N-diethyl-N'-[(8α)-6-methylergolin-8-yl]urea
Clinical data
AHFS/Drugs.com
Legal status
  • Prescription only
Routes Oral
Identifiers
CAS number
ATC code G02
PubChem
IUPHAR ligand
UNII  YesY
KEGG  YesY
Chemical data
Formula C20H28N4O 
Mol. mass 340.46 g/mol
 YesY   

Terguride (INN) is a serotonin antagonist. It is used for the treatment of hyperprolactinemia. Terguride is an oral, potent antagonist of 5-HT2B and 5-HT2A (serotonin) receptors. Serotonin stimulates the proliferation of pulmonary artery smooth muscle cells, and induces fibrosis in the wall of pulmonary arteries. Together, this causes vascular remodeling and narrowing of the pulmonary arteries. These changes result in increased vascular resistance and PAH. Due to the potential anti-proliferative and anti-fibrotic activity of terguride, this potential medicine could offer the hope of achieving reversal of pulmonary artery vascular remodeling and attenuation of disease progression.

In May 2008, terguride was granted orphan drug status for the treatment of pulmonary arterial hypertension.[1] In May 2010 Pfizer purchased world-wide rights for the drug.[2]


References

  1. ^ Presseportal (Swiss press portal, in German)
  2. ^ TheDay.com 5/10/2010