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Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase

1
Department of Molecular Microbiology and Immunology, University of Missouri, Columbia, MO 65211, USA
2
Bond Life Sciences Center, University of Missouri, Columbia, MO 65211, USA
3
Division of Clinical Microbiology, Department of Laboratory Medicine, Karolinska Institute, Huddinge 14186, Stockholm, Sweden
4
Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA
5
Division of Infectious Diseases, Department of Medicine Huddinge, Karolinska Institute, Huddinge 14186, Stockholm, Sweden
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2019, 12(2), 62; https://doi.org/10.3390/ph12020062
Received: 17 March 2019 / Revised: 16 April 2019 / Accepted: 18 April 2019 / Published: 20 April 2019
(This article belongs to the Special Issue The Story of Successful Drugs and Recent FDA-Approved Molecules)
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Abstract

One of the major factors contributing to HIV-1 drug resistance is suboptimal adherence to combination antiretroviral therapy (cART). Currently, recommended cART for HIV-1 treatment is a three-drug combination, whereas the pre-exposure prophylaxis (PrEP) regimens consist of one or two antivirals. Treatment regimens require adherence to a once or twice (in a subset of patients) daily dose. Long-acting formulations such as injections administered monthly could improve adherence and convenience, and thereby have potential to enhance the chances of expected outcomes, although long-lasting drug concentrations can also contribute to clinical issues like adverse events and development of drug resistance. Globally, two long-acting antivirals have been approved, and fifteen are in clinical trials. More than half of investigational long-acting antivirals target HIV-1 reverse transcriptase (HIV-1 RT) and/or integrase (HIV-1 IN). Here, we discuss the status and potential of long-acting inhibitors, including rilpivirine (RPV), dapivirine (DPV), and 4-ethynyl-2-fluoro-2-deoxyadenosine (EFdA; also known as MK-8591), which target RT, and cabotegravir (CAB), which targets IN. The outcomes of various clinical trials appear quite satisfactory, and the future of long-acting HIV-1 regimens appears bright. View Full-Text
Keywords: HIV-1; long-acting formulation; reverse transcriptase; integrase; antivirals HIV-1; long-acting formulation; reverse transcriptase; integrase; antivirals
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Singh, K.; Sarafianos, S.G.; Sönnerborg, A. Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase. Pharmaceuticals 2019, 12, 62.

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