The Use of alpha-4 beta-7 integrin Inhibitors to Inhibit HIV Transmission and Infection

This invention involves the use of inhibitors of alpha-4 beta-7 (a4b7) integrin to inhibit HIV transmission/infection, as a prophylactic to inhibit onset of the acute stage of HIV infection or to treat HIV infection. The a4b7 integrin inhibitors were previously developed for use in other diseases, such as multiple sclerosis or inflammatory bowel disease.

a4b7 integrin is a multifaceted target for HIV infection and recent studies indicate that it is important for establishing HIV infection through multiple paths. Studies indicate that: 1) CD4 T-cells present in vaginal and anal mucosa have high levels of a4b7 integrin, making CD4 T-cells permissive to HIV infection; 2) a4b7 integrin is important for cell to cell transmission of HIV; 3) a4b7 integrin is used to dysregulate the host humoral response to HIV; and 4) HIV acts on a4b7 integrin through an epitope in V2 loop of GP120, identified as important for HIV vaccine protection. Additionally, primate studies indicate that a4b7 integrin inhibition of HIV infection preserves gut-associated lymphoid tissue (GALT) generally destroyed during the acute phase of HIV infection.

Potential Commercial Applications: Competitive Advantages:
  • Prevention and treatment of HIV infection
  • a4b7 integrin is a multifaceted target for HIV infection
  • Previously developed a4b7 integrin inhibitors can be used for a new purpose

James Arthos (NIAID)
Diana Goode (NIAID)
Claudia Cicala (NIAID)
Anthony Fauci (NIAID)

Intellectual Property:
PCT Application No. PCT/US2007/086663
US Application No. 60/957,140
US Application No. 60/920,880
US Application No. 60/873,884
US Application No. 12/518,035

Martinelli E, et al. PMID 23797688
Nawaz F, PMID 21383973
Cicala C, et al. PMID 19933330
Arthos J, et al. PMID 18264102

Collaboration Opportunity:

The National Institute of Allergy and Infectious Diseases is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize alpha-4 beta-7 integrin inhibitors. For collaboration opportunities, please contact Bill Ronnenberg, JD/MIP, MS at 301-451-3522 or

Licensing Contact:
Cristina Thalhammer-Reyero , Ph.D., M.B.A.
NIH Office of Technology Transfer
Phone: 301-435-4507

OTT Reference No: E-055-2007/0

Updated: Feb-28-2014