Key result
Amphiphilic monoconjugates of human brain-type natriuretic peptide designed for oral delivery retained in vitro activity comparable to the native peptide.
Amphiphilic conjugates of hBNP designed for oral delivery retain in vitro activity comparable to the native peptide, suggesting potential for chronic heart failure treatment.
Supports oral BNP development for HF; leaves open in vivo efficacy and human translation.
Congestive heart failure (CHF) is a complex syndrome involving altered neurohormonal levels and impaired cardiac and renal function. In recent years, intravenous administration of exogenous human brain-type natriuretic peptide (hBNP) has become an important therapy in treating patients with acutely decompensated CHF. However, reports during the past year suggest that hBNP could play a prominent role in the chronic treatment of CHF patients as well. We are currently developing conjugates of hBNP suitable for oral delivery to provide a patient-friendly treatment option for chronic heart failure patients. In this report, we present in vitro activity results obtained from hBNP conjugates featuring a variety of rationally designed amphiphilic oligomers. Mapping studies revealed that the hydrophobic/hydrophilic balance of the oligomer impacted the regioselectivity of conjugation. Additionally, the regiochemistry and extent of conjugation had a significant impact on activity. Many monoconjugates retained activity comparable to native peptide and are currently under evaluation in subsequent in vivo screens.
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Miller et al. (2006) studied Congestive heart failure. Amphiphilic conjugates of human brain-type natriuretic peptide (hBNP) vs. Native peptide was evaluated on In vitro activity. Amphiphilic monoconjugates of human brain-type natriuretic peptide designed for oral delivery retained in vitro activity comparable to the native peptide.
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