• Antiviral Activity, Pharmacokinetics, and Safety of BMS-488043, a Novel Oral
  Small-Molecule HIV-1 Attachment Inhibitor, in HIV-1-Infected Subjects.
  Hanna GJ, Lalezari J, Hellinger JA, Wohl DA,  et al Antimicrob Agents Chemother. 2010 Nov 15
• In Vivo Resistance Patterns to the HIV Attachment Inhibitor BMS-488043.
  Zhou N, Nowicka-Sans B, Zhang S, Fan L, et al Antimicrob Agents Chemother. 2010 Nov 15.

• Antiviral Activity, Pharmacokinetics, and Safety of BMS-488043, a Novel Oral
  Small-Molecule HIV-1 Attachment Inhibitor, in HIV-1-Infected Subjects.
  Hanna GJ, Lalezari J, Hellinger JA, Wohl DA,  et al
  Antimicrob Agents Chemother. 2010 Nov 15
  Abstract
• In Vivo Resistance Patterns to the HIV Attachment Inhibitor BMS-488043.
  Zhou N, Nowicka-Sans B, Zhang S, Fan L, et al
  Antimicrob Agents Chemother. 2010 Nov 15.
  Abstract
• Increased sensitivity of HIV variants selected by attachment inhibitors to broadly neutralizing
  antibodies.
  Zhou N, Fan L, Ho HT,  et al
  Virology. 2010 Jul 5;402(2):256-61.
  Abstract
• Utilization of in vitro Caco-2 permeability and liver microsomal half-life screens in discovering
  BMS-488043, a novel HIV-1 attachment inhibitor with improved pharmacokinetic properties.
  Yang Z, Zadjura LM, Marino AM,  et al
  J Pharm Sci. 2010 Apr;99(4):2135-52.
  Abstract
• Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to
  azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo
  [2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activity
  in HIV-1-infected subjects.
  Wang T, Yin Z, Zhang Z, et al
  J Med Chem. 2009 Dec 10;52(23):7778-87.
  Abstract
• Amorphous drug-PVP dispersions: application of theoretical, thermal and spectroscopic analytical
  techniques to the study of a molecule with intermolecular bonds in both the crystalline and pure
  amorphous state.
  Tobyn M, Brown J, Dennis AB,  et al
  J Pharm Sci. 2009 Sep;98(9):3456-68
  Abstract
• Enhancement of oral bioavailability of an HIV-attachment inhibitor by nanosizing and amorphous
  formulation approaches.
  Fakes MG, Vakkalagadda BJ, Qian F, et al
  Int J Pharm. 2009 Mar 31;370(1-2):167-74.
  Abstract
• FULL-TEXT ARTICLE
  Envelope conformational changes induced by human immunodeficiency virus type 1 attachment
  inhibitors prevent CD4 binding and downstream entry events.
  Ho HT, Fan L, Nowicka-Sans B, McAuliffe B,  et al
  J Virol. 2006 Apr;80(8):4017-25.
  Paper

BMS-499043