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The study authors note in their paper that daily oral oral antiviral "cocktail" therapy provides a life-saving treatment for millions of people living with HIV, but some people are resistant to multiple drugs, reducing the effectiveness of the treatment.
if a patient is unable to keep taking daily medication for some reason, not only may the virus return in the body, but the risk of drug resistance will increase, not conducive to treatment.
that's why researchers are working to develop new long-acting drugs that give patients with HIV-resistant strains more treatment options, and can significantly reduce the frequency of medication, helping patients stick to treatment options.
introduce the drugs in this paper, let's briefly introduce HIV.
in virus particles, there is a unique cone protein shell called hiv shell.
the genome of the virus, hidden in this shell with reverse transcriptase and integration enzymes.
shell is formed by a shell protein self-assembled, not only to protect the genetic material of the virus, but also in all stages of HIV infection to help the virus genes and enzymes perfectly match, thus continuously producing the virus.
the authors of the study, most small molecule antiviral drugs for HIV work by interfering with the virus's reverse transcriptase or integrated enzymes, and the new drug, called GS-6207, is unusually targeted.
designed, this small molecule can be tightly bound to HIV shell protein, interfere with the shell assembly, destroy its function.
in cell experiments, scientists found that the small molecule had a wide range of activity against more than 20 HIV strains tested, effectively inhibited replication of the virus, and ec50 was 105 pM in MT-4 cells infected with HIV-1, making them more potent than other approved antiretroviral drugs.
, GS-6207 and other antiretroviral drugs can produce synergies when combined, and researchers believe it could be an ideal complement to "cocktail therapy."
The Structure of the GS-6207 (Photo Source: References) Follows the researchers' preliminary clinical trial studies.
in a single-dose study of randomized, double-blind and placebo-controlled treatments for 40 healthy individuals, researchers showed overall safety and good tolerance by injecting the drug with subcutaneous injections.
, GS-6207 showed slow, sustained drug release, with only one injection, and the drug remained active in the body more than six months later.
later, the researchers conducted phase 1 clinical trials in 32 patients infected with HIV-1 but not treated.
results showed that after 9 days of single-dose administration, the viral load in the patient's body decreased, although it was not completely removed.
in healthy people and HIV-1 infected people, the activity of this small molecule drug can be maintained for 24 weeks, and reduce the viral load in the infected person (Picture source: References 1)) At the end of the paper, the researchers concluded that as a first-in-class HIV-1 shell inhibitor, GS-6207 showed good safety, prolonged pharmacokinetic exposure and the observation of antiviral efficacy in the human body can continue to develop long-term hiv infection.
study authors also say that because it does n'etre that doesn't require frequent administration, the small molecule drug could become a candidate for HIV prevention in at-risk groups, but that needs to be tested in follow-up studies.
We look forward to positive results from subsequent clinical studies that will ultimately benefit more people living with HIV-1.
reference s1 clinical targeting of HIV capsid protein with a long-acting small. Nature DOI: 10.1038/s41586-020-2443-1.