New Antiretrovirals on the Block: Pharmacological news from Croi 2017

The Conference on Retrovirus and Opportunistic Infections, CROI, 2017 at Seattle, USA, presented several new substances, therapy strategies and other data about the treatment of HIV/AIDS. The following article discusses a pharmacological selection of these, and shows data of new integrase inhibitors (INSTI), nucleoside (NRTI) and non-nucleoside reverse transcriptase inhibitors (NNRTI) as well as protease inhibitors (PI), CCR5-inhibitors and several long-acting antibodies or new formulations of already widely used drugs, such as Nano particle PI and NNRTI (NANO-NNRTI, NANO-PI).

New Antiretrovirals on the Block
New Antiretrovirals on the Block

Karen White and colleagues presented the new NRTI GS-9131, which reveals strong activity against NRTI-resistant HIV-1.At a very low EC50 of only 0.16 μM (± 0.02) GS-9131 is still active against most of NRTI-resistant HIV-1, showing mutations of K65R, M184V, L74V/I, 6TAMs+184V or Q151M+M184V.Unlike TAF, GS-3131 is an adenosine-analogue. But alike TAF it is a prodrug, which is modified by cathepsin A into its intracellular form of GS-9148 and then phosphorylated by intracellular kinases into its antiretroviral active diphosphate.


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