Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase
AbstractOne 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
Share & Cite This Article
Singh, K.; Sarafianos, S.G.; Sönnerborg, A. Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase. Pharmaceuticals 2019, 12, 62.
Singh K, Sarafianos SG, Sönnerborg A. Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase. Pharmaceuticals. 2019; 12(2):62.Chicago/Turabian Style
Singh, Kamal; Sarafianos, Stefan G.; Sönnerborg, Anders. 2019. "Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase." Pharmaceuticals 12, no. 2: 62.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.