Combination product for the prevention of sexually transmitted infections
Inventors
O'Keefe, Barry R. • Robbiani, Melissa • Romero, José A. Fernández
Assignees
Population Council Inc • US Department of Health and Human Services
Publication Number
US-10143721-B2
Publication Date
2018-12-04
Expiration Date
2035-01-13
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Abstract
Disclosed are compositions for inhibiting transmission of a sexually transmitted infection that contain one or more polyanionic microbicides, such as carrageenans, including lambda carrageenan, as well as water-soluble metal salts and specified lectins. Also disclosed are methods for making and using the compositions.
Core Innovation
The invention discloses antimicrobial compositions for inhibiting transmission of sexually transmitted infections (STIs) that combine one or more lectins, such as Griffithsin, with one or more additional antimicrobial agents including physiologically acceptable water soluble metal salts (notably zinc salts like zinc acetate) and carrageenans, particularly lambda carrageenan. These combinations provide enhanced and synergistic anti-viral activity against pathogens such as HIV, HSV-2, and human papillomavirus (HPV). The compositions may be formulated in various physical forms including gels, solutions, solids, powders, or dried forms suitable for vaginal or rectal administration.
The problem being addressed is the unmet need for effective microbicides that simultaneously protect against HIV and other STIs. Previous single active pharmaceutical ingredient (API) microbicides have failed in clinical trials due to reasons such as low potency, short protection window, reduced activity in biological fluids, or adverse mucosal and microflora changes. There remains a need for more potent and safe APIs, or combinations thereof, capable of broad spectrum prevention of STIs.
Applicant's discovery is that combinations of lectins like Griffithsin with zinc metal salts and/or carrageenans produce compositions with more potent and synergistic antimicrobial effects. The combination of Griffithsin and zinc acetate enhances anti-HIV activity synergistically, while Griffithsin combined with carrageenans shows synergy against HPV. Additionally, combinations of Griffithsin, zinc acetate, and carrageenan show increased anti-HSV-2 activity both in vitro and in vivo. These compositions can also be combined with other agents such as contraceptives for multipurpose prevention technologies.
Claims Coverage
The patent claims describe mainly two independent claims covering antimicrobial compositions combining Griffithsin with a water soluble metal salt and/or carrageenan, and a specific triple combination composition.
Antimicrobial composition comprising Griffithsin and a selected agent
An antimicrobial composition comprising Griffithsin in an amount from about 0.01% to 1% by weight, combined with one or more agents selected from a physiologically acceptable water soluble metal salt (0.03% to 1.5%), carrageenan (1% to 5%), or combinations thereof.
Antimicrobial composition comprising Griffithsin, zinc acetate, and carrageenan
An antimicrobial composition comprising Griffithsin (0.01% to 1.0%), zinc acetate (0.03% to 1.5%), and carrageenan (1% to 5%) by weight of the composition.
The claims cover antimicrobial compositions that integrate Griffithsin with water soluble metal salts and/or carrageenan in specified amounts, including the specific triple combination of Griffithsin, zinc acetate, and carrageenan, formulated for prevention of STIs.
Stated Advantages
The compositions provide broad and extremely potent antimicrobial activity against HIV, HSV-2, HPV, and potentially other STIs through synergistic effects of combined agents.
The compositions avoid the use of antiretroviral drugs (ARVs), reducing the risk of ARV drug resistance and providing an advantageous alternative for HIV prevention.
The compositions can be formulated for vaginal and rectal administration and may be suitable for over-the-counter use, increasing accessibility and affordability and contributing to public health benefits worldwide.
Documented Applications
Use as microbicidal compositions to prevent vaginal or rectal transmission of sexually transmitted infections including HIV, HSV-2, HPV, and other STIs.
Administration as multipurpose prevention technologies combining antimicrobial agents with drugs such as contraceptive agents or hormone replacement therapy for simultaneous prevention of infections and unintended pregnancy.
Treatment or prevention of microbial infections, including viral infections caused by HIV, HSV-2, HPV, and other sexually transmitted pathogens, in subjects at risk or already infected.
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