BVM: A Promising Agent for Future HIV-1 Treatment

Autori

  • Alex Joseph Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104
  • Suthar Sharad Kumar Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104
  • Sandeep Lohan Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104
  • Abhishek Mathur Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104
  • Srinivasan K.K Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104
  • Angel Treasa Thomas Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104

Parole chiave:

BVM, HIV-1, Maturation inhibitors, Glucuronidation, CA-SP1 cleavage

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.

Biografia autore

  • Suthar Sharad Kumar, Manipal College of Pharmaceutical Sciences Manipal University Manipal-576104
    Assistant Professor, Department of Pharmaceutical Chemistry,

Dowloads

Pubblicato

2011-08-18

Fascicolo

V. 2 N. 1 (2011)

Sezione

Review Articles

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