Current interest in the novel anti-HIV drug development emphasizes in the development of non-peptide protease inhibitors (e.g., Tipranavir). What are the therapeutic benefits of a non-peptide protease inhibitor over a peptide protease inhibitor in the context of the treatment of HIV infected patients?
Kindly provide references if possible.
Regards,
In general peptidic drugs have very poor pharmacological profiles, they have poor oral bioavailability, are rapidly excreted and susceptible to hydrolysis. As a result they have short half lives in the bloodstream often requiring high doses or the use of boosters to inhibit metabolism. The chemical nature of peptidic inhibitors can also contribute to unpleasant side effects due to cross reactivity with endogenous proteases.
Existing peptidic drugs also show significant cross resistance, whereby a viral strain that is resistant to one peptidic drug is commonly resistant to another. Non-peptidic drugs may have orthogonal resistance profiles and the diverse range of structural features make cross resistance less likely.
As such, from a clinical perspective non-peptidic protease inhibitors may help patients with easier dosing regimens, potentially fewer side effects, and better options in the event of treatment failure due to drug resistance.
Here is a review:
Bhat M A, Siddiqui N, Khan S A, Ahmad M. Non-peptide protease inhibitors as novel anti-HIV agents. Indian J Pharm Sci 2006;68:549-55
- Badges
- Science topic
- Similar topics
- Biological Science
- Anatomy
- Tissue