Scientists from Gilead Sciences have developed and tested an antiretroviral drug in a new class of small molecule that disrupts the capsid protein of HIV and inhibits the replication of the virus at different stages. The researchers conducted the first phase of clinical trials with a single injection of the drug he was safe, effective and remained in the blood for six months. The authors of an article published in the journal Nature, believe that the drug is useful for patients who have developed multidrug resistance, and for prevention for people at risk.
Modern antiretroviral drugs are saving the lives of millions of people with human immunodeficiency virus (HIV) and protect those who are at risk, but the virus actively mutates and can acquire resistance to the drugs. People, the virus which are resistant to multiple classes of antiretroviral drugs, it is difficult and sometimes impossible to find treatment. In addition, medications in pill form must be taken daily and absences increase the probability of reproduction and mutation of HIV. It is therefore necessary to look for drugs in new classes, which will operate for a long time and suppress the virus by a different mechanism.
Scientists from the U.S. biopharmaceutical company Gilead Sciences under the leadership of Steven Yanta (Stephen Yant) investigated the action of a small molecule GS-6207 — inhibitor protein of the viral capsid. First tested its effect on speed of Assembly of the capsid and on the reproduction of HIV in cultures of various immune cells.
GS-6207 accelerated the Assembly of capsid proteins, which viral envelope is deformed. The drug was more effective than all of the approved antiretroviral drugs: it premaxillae effective concentration for the cells infected with HIV, amounted to 105 per litre in picomoles culture T-helper cells, 32 and 56 picomole per liter in the culture of primary T cells and macrophages. GS-6207 was effective against the two major forms of HIV — 1 and HIV-2, including against the types of virus that are resistant to modern medicines. In addition, the drug almost had no cytotoxic effect on human cells.