ofetinin

Ofetinin is a non-peptide, orally active, selective inhibitor of the neprilysin enzyme. Neprilysin is a zinc metalloprotease that degrades various bioactive peptides, including angiotensin II, bradykinin, and neuropeptides. By inhibiting neprilysin, ofetinin increases the levels of these peptides, which can have various physiological effects, including vasodilation, anti-inflammatory actions, and neuroprotective properties.

Ofetinin was discovered through high-throughput screening of a chemical library and has shown promise in preclinical studies for the treatment of conditions associated with neprilysin activity, such as hypertension, heart failure, and neurodegenerative diseases. It has been demonstrated to lower blood pressure in animal models and to improve cognitive function and reduce inflammation in models of neurodegenerative diseases.

Ofetinin is currently in clinical development for the treatment of hypertension and heart failure. Phase II clinical trials have shown that ofetinin can reduce blood pressure and improve left ventricular ejection fraction in patients with heart failure. Additionally, ofetinin has been shown to have a favorable safety profile, with no significant adverse effects observed in clinical trials.

The mechanism of action of ofetinin is distinct from other neprilysin inhibitors, such as sacubitril, which is a peptide-based inhibitor. Ofetinin is a non-peptide, orally active compound, which may offer advantages in terms of stability, bioavailability, and ease of administration. However, further clinical trials are needed to fully evaluate the safety and efficacy of ofetinin in the treatment of hypertension and heart failure.