BVM: A Promising Agent for Future HIV-1 Treatment

Suthar, Sharad Kumar and Joseph, Alex and Lohan, Sandeep and Mathur, Abhishek S and Srinivasan, KK and Thomas, Angel Treasa (2011) BVM: A Promising Agent for Future HIV-1 Treatment. Research & Reviews: A Journal of Pharmaceutical Science, 2 (1). pp. 11-21.

[img] PDF
BVM_Treatment_Joseph_Aug_2011.pdf - Published Version
Restricted to Registered users only

Download (241kB) | Request a copy

Abstract

More than 20 individual and fixed-dose combinations of anti-HIV drugs are available for the treatment of human immunodeficiency virus (HIV) infection. However, owing to the development of viral-drug resistance and adverse effects associated with currently available drug therapy regimen there is a continuous need to explore new drug candidates. BVM is the first in class of maturation inhibitors, which inhibits HIV-1 maturation by blocking a late step in the Gag processing pathway specifically the cleavage of SP1 from the C terminus of capsid (CA). BVM has a side chain at position 3 of betulinic acid. It is well absorbed after oral administration and a long half-life indicating once daily dosing. Metabolism of BVM takes place predominantly by glucuronidation via uridine diphosphate glucuronosyltransferases (UGTs). Elimination of bevirimat is primarily by hepatic glucuronidation and hepatobiliary excretion. Single amino acid substitution at or near the CA-SP1 cleavage site confers resistance to BVM, which is not a known target for resistance to existing antiretroviral drugs. Encouraging results obtained in preclinical and limited clinical trials indicates that BVM is promising agent for the future HIV-1 treatment, henceforth needs further investigations in humans.

Item Type: Article
Uncontrolled Keywords: BVM, HIV-1, Maturation inhibitors, Glucuronidation, CA-SP1 cleavage
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Biotechnology
Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Depositing User: KMC Manipal
Date Deposited: 18 Oct 2012 10:53
Last Modified: 18 Oct 2012 10:53
URI: http://eprints.manipal.edu/id/eprint/77464

Actions (login required)

View Item View Item