BMS-955176

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BMS-955176
BMS-955176.svg
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
  • 1392312-45-6
ChemSpider
UNII
Chemical and physical data
FormulaC42H62N2O4S
Molar mass691.03 g·mol−1
3D model (JSmol)
  • CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]3CC[C@H]4[C@]([C@@]3(CC2)C)(CC[C@@H]5[C@@]4(CC=C(C5(C)C)c6ccc(cc6)C(=O)O)C)C)NCCN7CCS(=O)(=O)CC7
  • InChI=1S/C42H62N2O4S/c1-28(2)31-14-19-42(43-22-23-44-24-26-49(47,48)27-25-44)21-20-40(6)33(36(31)42)12-13-35-39(5)17-15-32(29-8-10-30(11-9-29)37(45)46)38(3,4)34(39)16-18-41(35,40)7/h8-11,15,31,33-36,43H,1,12-14,16-27H2,2-7H3,(H,45,46)/t31-,33+,34-,35+,36+,39-,40+,41+,42-/m0/s1
  • Key:XDMUFNNPLXHNKA-ZTESCHFWSA-N

BMS-955176 is an experimental second generation HIV maturation inhibitor under development by Bristol-Myers Squibb for use in the treatment of HIV infection. By blocking the maturation of the virus, it prevents viral reproduction in host CD4+ T cells.[1] First generation maturation inhibitors such as bevirimat were ineffective against some naturally occurring changes (polymorphisms) in the Gag protease polyprotein; BMS-955176 has been selected to better tolerate gag polymorphisms.[2][3]

Studies

Results of a phase 2a trial of BMS-955176 was reported at the 2015 Conference on Retroviruses and Opportunistic Infections (CROI).[4] Investigators concluded that the drug was well tolerated and effective against HIV, including strains with gag polymorphisms.[4][5] Phase 2b studies are currently ongoing in early 2016.[6][7] It appears that development of BMS-955176 has been terminated.[8]

References

  1. ^ "BMS Maturation Inhibitor Is Potent Against HIV in Early Trial". 25 February 2015. Archived from the original on 23 July 2015. Retrieved 22 July 2015.
  2. ^ "CROI2015: New HIV maturation inhibitor BMS-955176 appears more potent than earlier beviramat - Project Inform".
  3. ^ Wang D, Lu W, Li F (November 2015). "Pharmacological intervention of HIV-1 maturation". Acta Pharmaceutica Sinica B. 5 (6): 493–9. doi:10.1016/j.apsb.2015.05.004. PMC 4675807. PMID 26713265.
  4. ^ a b "Antiviral Activity/Safety of a Second-Generation HIV-1 Maturation Inhibitor | CROI Conference". www.croiconference.org. Retrieved 2016-01-01.
  5. ^ "HIV maturation inhibitor BMS-955176 looks promising in early study". www.aidsmap.com. Retrieved 2016-01-01.
  6. ^ "Dose-finding Study of BMS-955176 to Treat HIV-1 Infected Treatment-naive Adults - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2016-01-01.
  7. ^ Clinical trial number NCT02386098 for "Strategy-confirming Study of BMS-955176 to Treat HIV-1 Infected Treatment-experienced Adults" at ClinicalTrials.gov
  8. ^ "GSK Discontinues Development of Maturation Inhibitor BMS-955176".