Sampatrilat

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[6-[[2-[[2-(2-amino-3-mercaptopropanoyl)amino]acetyl]amino]-2-methylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoic acid | image = | width = | CAS_number = 120806-61-5 | ATC_prefix = none | PubChem = 6918184 | ChemSpiderID = 5293703 | UNII = 3F0I0G1D5A | KEGG = D05995 | ChEMBL = 2103870 | C=19 | H=34 | N=4 | O=6 | S=1 | molecular_weight = 446.56 }}

Sampatrilat is a pharmaceutical drug that has been investigated for its potential use in treating cardiovascular diseases. It is classified as a vasopeptidase inhibitor, which means it inhibits the activity of enzymes that degrade vasoactive peptides.

Mechanism of Action

Sampatrilat functions by inhibiting two key enzymes: angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). By inhibiting ACE, sampatrilat reduces the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, thereby lowering blood pressure. Inhibition of NEP prevents the breakdown of natriuretic peptides, which are involved in vasodilation and natriuresis, further contributing to its antihypertensive effects.

Clinical Development

Sampatrilat has been studied in various clinical trials to assess its efficacy and safety in patients with hypertension and heart failure. However, as of the latest updates, it has not been approved for clinical use. The development of sampatrilat has provided insights into the potential benefits and challenges of dual enzyme inhibition in cardiovascular therapy.

Potential Benefits

The dual inhibition of ACE and NEP by sampatrilat offers a comprehensive approach to managing cardiovascular conditions. This dual action can lead to more effective blood pressure control and improved cardiac function compared to traditional ACE inhibitors alone.

Challenges and Considerations

Despite its potential, the development of sampatrilat has faced challenges, including adverse effects such as hypotension and renal impairment. The balance between efficacy and safety remains a critical consideration in its clinical development.

Also see

• Angiotensin-converting enzyme inhibitor
• Neutral endopeptidase inhibitor
• Hypertension
• Heart failure
• Vasopeptidase inhibitor