Elvitegravir is a drug that belongs to the active substances of integrase inhibitors. In human medicine, elvitegravir is used primarily as a drug for the treatment of infections with the HIV-1 virus. Physicians always use the active ingredient together with other drugs that have an antiretroviral effect. Doctors particularly often combine elvitegravir with the substance cobicistat, which is a so-called booster.
What is elvitegravir?
Elvitegravir inhibits integrase (a retroviral enzyme) to a high degree, making it well suited for treating infections with the HIV-1 virus. The pharmaceutical manufacturer Gilead Sciences developed the drug Elvitegravir, which received approval as a drug from the Food and Drug Administration in 2012. In this context, Elvitegravir is mainly used for drug therapy of adult patients. Elvitegravir represents a derivative of dihydroquinoline and appears as a powder of white to yellowish color at room temperature. In addition, elvitegravir is characterized by relatively poor solubility in water. The active ingredient is particularly well suited for people whose HIV drug therapy is just beginning. Thus, in many cases, elvitegravir represents an initial medication. Pharmaceutical manufacturers sometimes combine elvitegravir with the active ingredient tenofovir. This combination of two drugs improves efficacy, while disadvantages decrease in some cases. People infected with HIV often receive elvitegravir as a single drug under the trade name Vitekta. In addition, physicians often combine the active ingredient with ritonavir. Ritonavir is a pharmacological substance that is used in numerous HIV medications. Here, ritonavir usually acts as a booster that increases the effectiveness of the actual drug.
Pharmacologic effects on the body and organs
The effect of elvitegravir is mainly due to the inhibition of integrase. This results in the good suitability of elvitegravir as an HIV drug. This is because elvitegravir inhibits the enzyme integrase of viruses, particularly HIV-1 viruses. Elvitegravir is somewhat less effective on HIV-2 viruses. The viruses need this enzyme to transfer their genetic information into the host’s DNA. In this way, elvitegravir has a strong antiviral effect. Elvitegravir is usually used in combination with CYP inhibitors, which slow down the metabolism of elvitegravir and thus increase its effectiveness in the organism. Elvitegravir is mainly degraded by CYP3A. Therefore, concomitant use with inducers of the enzyme should be refrained from. These include, for example, phenytoin or St. John’s wort. Elvitegravir has little effect on renal function. Patients take elvitegravir in tablet form. If taken at the same time as ritonavir and a meal, the active ingredient reaches its highest concentrations in the blood plasma after about four hours. Studies have shown that high-fat meals increase the bioavailability of elvitegravir. In the bloodstream, the majority of elvitegravir binds to plasma proteins. Nearly 95 percent of the active ingredient is excreted by the body in the stool. The remainder exits the body in the urine. The plasma half-life of elvitegravir in combination with ritonavir is between 9 and 13 hours.
Medicinal use and use for treatment and prevention.
Elvitegravir is an HIV-1 medication that is commonly used as a fixed-dose combination with pharmacologic boosters. Patients take elvitegravir orally as a film-coated tablet. It is sufficient to consume a single tablet of the active ingredient elvitegravir per day. It is recommended that elvitegravir be taken during a meal to increase efficacy. Mandatory is the co-administration of the active ingredient Elvitegravir with a booster that inhibits protease. For this reason, elvitegravir is usually available in a fixed combination with an appropriate booster. The dose depends primarily on the protease inhibitor administered at the same time. Currently, however, physicians still use elvitegravir as a reserve drug.
Risks and side effects
Taking elvitegravir sometimes results in adverse side effects similar to those of many other HIV medications.Most commonly, elvitegravir administration results in digestive tract symptoms such as nausea, vomiting, and diarrhea. In addition, some patients report headaches and fatigue. In addition, some individuals develop rashes on the skin. The pharmaceutical manufacturers generally describe elvitegravir as a well-tolerated drug. Therapy with the active ingredient is generally ruled out if patients suffer from intolerance to the active ingredient. Even in the case of resistance to elvitegravir, it does not make medical sense to take the drug. For pregnant and breastfeeding women, special guidelines sometimes apply for therapy with elvitegravir. Before taking elvitegravir, certain interactions with other pharmaceutical substances must be considered. Elvitegravir is metabolized primarily in the liver by the enzyme CYP3A. For this reason, concomitant use of elvitegravir and phenytoin, rifampicin, and carbamazepine should be urgently avoided. Combination with St. John’s wort should also be avoided. Elvitegravir is characterized by cross-resistance to the active ingredient raltegravir. In general, elvitegravir is considered a reserve preparation for the drug therapy of infections with the HIV-1 virus. Clinical experience to date is comparatively limited. However, the advantage of elvitegravir is that one dose per day is sufficient for therapy.
