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).
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.(Read more)
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