Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention
HIV/AIDS remains a global public health issue, and products available for the prevention of HIV infections are limited, especially those for short-acting, on-demand, user-controlled applications. Topical inserts are products that can be applied vaginally or rectally and have been explored as drug de...
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| Format: | Article |
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MDPI AG
2024-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/16/3/348 |
| _version_ | 1827305328894541824 |
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| author | M. Melissa Peet Vivek Agrahari Meredith R. Clark Gustavo F. Doncel |
| author_facet | M. Melissa Peet Vivek Agrahari Meredith R. Clark Gustavo F. Doncel |
| author_sort | M. Melissa Peet |
| collection | DOAJ |
| description | HIV/AIDS remains a global public health issue, and products available for the prevention of HIV infections are limited, especially those for short-acting, on-demand, user-controlled applications. Topical inserts are products that can be applied vaginally or rectally and have been explored as drug delivery systems. To fill the gap in the HIV prevention product pipeline, CONRAD has developed a topical insert containing tenofovir alafenamide fumarate (TAF) and elvitegravir (EVG), two potent and synergistic antiretrovirals, as a simple, low-cost, and discreet option that can be self-administered vaginally and/or rectally, before and after coitus. In this review, we have described the development path of the TAF/EVG insert up to its current point in clinical testing, highlighting findings from acceptability, preclinical safety, pharmacokinetics, and efficacy evaluations and early clinical studies. In summary, the TAF/EVG inserts are stable, easy to manufacture, low-cost, acceptable, and show highly promising preclinical and clinical results for on-demand topical pre- or post-exposure HIV prevention. |
| first_indexed | 2024-04-24T17:55:20Z |
| format | Article |
| id | doaj.art-b08ca4d6ac9d4393a2f9bc79632e7082 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-24T17:55:20Z |
| publishDate | 2024-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-b08ca4d6ac9d4393a2f9bc79632e70822024-03-27T13:59:41ZengMDPI AGPharmaceutics1999-49232024-03-0116334810.3390/pharmaceutics16030348Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV PreventionM. Melissa Peet0Vivek Agrahari1Meredith R. Clark2Gustavo F. Doncel3CONRAD, Eastern Virginia Medical School, Norfolk, VA 23507, USACONRAD, Eastern Virginia Medical School, Norfolk, VA 23507, USACONRAD, Eastern Virginia Medical School, Norfolk, VA 23507, USACONRAD, Eastern Virginia Medical School, Norfolk, VA 23507, USAHIV/AIDS remains a global public health issue, and products available for the prevention of HIV infections are limited, especially those for short-acting, on-demand, user-controlled applications. Topical inserts are products that can be applied vaginally or rectally and have been explored as drug delivery systems. To fill the gap in the HIV prevention product pipeline, CONRAD has developed a topical insert containing tenofovir alafenamide fumarate (TAF) and elvitegravir (EVG), two potent and synergistic antiretrovirals, as a simple, low-cost, and discreet option that can be self-administered vaginally and/or rectally, before and after coitus. In this review, we have described the development path of the TAF/EVG insert up to its current point in clinical testing, highlighting findings from acceptability, preclinical safety, pharmacokinetics, and efficacy evaluations and early clinical studies. In summary, the TAF/EVG inserts are stable, easy to manufacture, low-cost, acceptable, and show highly promising preclinical and clinical results for on-demand topical pre- or post-exposure HIV prevention.https://www.mdpi.com/1999-4923/16/3/348HIV pre-exposure and post-exposure prophylaxistopical PrEP and PEPantiretroviralsacceptabilitysafety |
| spellingShingle | M. Melissa Peet Vivek Agrahari Meredith R. Clark Gustavo F. Doncel Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention Pharmaceutics HIV pre-exposure and post-exposure prophylaxis topical PrEP and PEP antiretrovirals acceptability safety |
| title | Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention |
| title_full | Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention |
| title_fullStr | Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention |
| title_full_unstemmed | Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention |
| title_short | Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention |
| title_sort | preclinical and early clinical development of tenofovir alafenamide elvitegravir topical inserts for effective on demand vaginal and rectal hiv prevention |
| topic | HIV pre-exposure and post-exposure prophylaxis topical PrEP and PEP antiretrovirals acceptability safety |
| url | https://www.mdpi.com/1999-4923/16/3/348 |
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