Modified dolutegravir
Scientists have created a drug that suppresses HIV for a month
American virologists have developed a drug, a single dose of which suppresses the reproduction of the immunodeficiency virus for a month and prevents HIV infection for two weeks, according to an article published in the journal Nature Communications (Sillman et al., Creation of a long-acting nanoformulated dolutegravir).
"Modern antiretroviral therapies allow HIV carriers to lead a full life, but they do not get this life for free. Such drugs are expensive, toxic, they gradually lose their effectiveness and violations of the regime have a hard effect on patients. Many of these problems could be solved by creating a drug that would act on the body for a very long time," Howard Gendelman from the University of Nebraska in Omaha (USA) and his colleagues write (in a press release, Chemically modified drug shows promise for HIV treatment, elimination – VM).
As scientists explain, today HIV patients can live for decades thanks to the use of antiretroviral drugs – substances that suppress various stages of virus replication in the cells of the body. Since they often have strong side effects, doctors are often forced to stop taking them for several weeks.
When they stop taking them, HIV "gets out of the trenches" and begins to intensively copy itself, often returning to the initial scale of infection in three or two weeks. In recent years, scientists have been actively trying to find drugs or antibodies that would help avoid such a "counterattack" of the virus, or would allow the virus to be "kicked out" of cells.
Gendelman and his colleagues developed a kind of intermediate solution – they managed to modify one of the already existing drugs, dolutegravir, in such a way that its molecules continued to suppress the reproduction of the virus in animals for a very long time.
To do this, as doctors note, they had to make only minimal changes to the structure of the drug molecule. In particular, they added a long hydrocarbon tail to it, which prevents the body from decomposing them quickly, and embedded them in the strands of a polymer that gradually decomposes when it enters the bloodstream.
Experiments on mice have shown that a small dose of nanoparticles made from such a polymer suppresses the reproduction of the virus in already infected rodents for a month, and protects healthy animals from HIV infection for at least two weeks.
Interestingly, such a "package" of dolutegravir, according to scientists, increased its activity by several dozen times and extended the lifetime of its molecules in the bloodstream by about 5 times, which allowed doctors to significantly reduce the dose of the drug that they injected into the body of mice.
This almost completely eliminated all the side effects of taking this medicine, and reduced its toxicity level to almost zero, which, according to the authors of the article, gives their nanoparticles a great chance of passing clinical trials and getting into medical practice faster.
According to Handelman, his team has already started preliminary experiments on monkeys and so far they show that their drug does not interfere with the normal functioning of the immune system and does not cause other side effects.
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