Dolutegravir (DTG), sold under the brand name Tivicay, is an

antiretroviral medication Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Unlike most antibiotics, antiviral drugs do n ...

used, together with other medication, to treat

HIV/AIDS Human immunodeficiency virus infection and acquired immunodeficiency syndrome (HIV/AIDS) is a spectrum of conditions caused by infection with the human immunodeficiency virus (HIV), a retrovirus. Following initial infection an individual ...

. It may also be used, as part of

post exposure prophylaxis Post-exposure prophylaxis, also known as post-exposure prevention (PEP), is any preventive medical treatment started after exposure to a pathogen in order to prevent the infection from occurring. COVID-19 In 2021, the FDA has approved bamlanivim ...

, to prevent HIV infection following potential exposure. It is taken by mouth. Common side effects include trouble sleeping, feeling tired,

diarrhea Diarrhea, also spelled diarrhoea, is the condition of having at least three loose, liquid, or watery bowel movements each day. It often lasts for a few days and can result in dehydration due to fluid loss. Signs of dehydration often begin wi ...

high blood sugar Hyperglycemia is a condition in which an excessive amount of glucose circulates in the blood plasma. This is generally a blood sugar level higher than 11.1 mmol/L (200 mg/dL), but symptoms may not start to become noticeable until even ...

, and headache. Severe side effects may include

allergic reactions Allergies, also known as allergic diseases, refer a number of conditions caused by the hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include hay fever, food allergies, atopic derma ...

and

liver problems Liver disease, or hepatic disease, is any of many diseases of the liver. If long-lasting it is termed chronic liver disease. Although the diseases differ in detail, liver diseases often have features in common. Signs and symptoms Some of the sig ...

. There are tentative concerns that use during

pregnancy Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ca ...

can result in harm to the baby. It is unclear if use during

breastfeeding Breastfeeding, or nursing, is the process by which human breast milk is fed to a child. Breast milk may be from the breast, or may be expressed by hand or pumped and fed to the infant. The World Health Organization (WHO) recommends that br ...

is safe. Dolutegravir is an

HIV integrase strand transfer inhibitor Integrase inhibitors (INIs) are a class of antiretroviral drug designed to block the action of integrase, a viral enzyme that inserts the viral genome into the DNA of the host cell. Since integration is a vital step in retroviral replication, block ...

which blocks the functioning of

HIV integrase Retroviral integrase (IN) is an enzyme produced by a retrovirus (such as HIV) that integrates—forms covalent links between—its genetic information into that of the host cell it infects. Retroviral INs are not to be confused with phage inte ...

which is needed for

viral replication Viral replication is the formation of biological viruses during the infection process in the target host cells. Viruses must first get into the cell before viral replication can occur. Through the generation of abundant copies of its genome an ...

. Dolutegravir was approved for medical use in the United States in 2013. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health ...

Abacavir/dolutegravir/lamivudine Abacavir/dolutegravir/lamivudine, sold under the brand name Triumeq among others, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. It is a combination of three medications with different and complementary mech ...

, a combination with

abacavir Abacavir, sold under the brand name Ziagen among others, is a medication used to treat HIV/AIDS. Similar to other nucleoside analog reverse-transcriptase inhibitors (NRTIs), abacavir is used together with other HIV medications, and is not recom ...

and

lamivudine Lamivudine, commonly called 3TC, is an antiretroviral medication used to prevent and treat HIV/AIDS. It is also used to treat chronic hepatitis B when other options are not possible. It is effective against both HIV-1 and HIV-2. It is typically ...

is also available. As of 2019, the

World Health Organization The World Health Organization (WHO) is a specialized agency of the United Nations responsible for international public health. The WHO Constitution states its main objective as "the attainment by all peoples of the highest possible level of h ...

(WHO) recommends DTG as the first- and second-line treatment for all persons with HIV.

Medical use

Dolutegravir is approved for use in a broad population of HIV-infected patients. It can be used to treat HIV-infected adults who have never taken HIV therapy (treatment-naïve) and HIV-infected adults who have previously taken HIV therapy (treatment-experienced), including those who have been treated with other integrase strand transfer inhibitors. Tivicay is also approved for children ages 12 years and older weighing at least 40 kilograms (kg) who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors. In the European Union it is indicated, in combination with other anti-retroviral medicinal products, for the treatment of Human Immunodeficiency Virus (HIV) infected adults, adolescents and children above six years of age. In June 2020, the indication for dolutegravir in the US was updated to include children at least four weeks old and weighing at least 3 kg (6.61 pounds).

Adverse effects

Common side effects of dolutegravir in clinical trials included insomnia and headache. Serious side effects included allergic reactions and abnormal liver function in patients who were also infected with hepatitis B or C. The package insert warns against a mean rise in serum creatinine of 0.11 mg/dL due to inhibition of tubular secretion of creatinine and does not affect

GFR GFR may refer to: * Gas-cooled fast reactor * Gefreiter * General fertility rate * Glomerular filtration rate * Government Flight Representative * Grand Forks Railway, a Canadian railway * Grand Funk Railroad, an American rock band * Grup Ferovi ...

Pregnancy

There are tentative concerns that use during

can result in harm to the baby. Effective

birth control Birth control, also known as contraception, anticonception, and fertility control, is the use of methods or devices to prevent unwanted pregnancy. Birth control has been used since ancient times, but effective and safe methods of birth contr ...

is thus recommended while on dolutegravir, with pregnancy testing before starting treatment. Use during the first trimester should only occur if there is no alternative.

History

In February 2013, the U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) announced that it would fast track dolutegravir's approval process. On August 13, 2013, dolutegravir was approved for medical use in the United States. On November 4, 2013, dolutegravir was approved by Health Canada. On January 16, 2014, it was approved by the European Commission for use throughout the European Union. In 2019, a triple-combination therapy, with dolutegravir replacing

efavirenz Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention after a needlest ...

, was introduced as the first-line treatment for all people (pregnant excluded) with HIV by the

South African Government The Republic of South Africa is a parliamentary republic with three-tier system of government and an independent judiciary, operating in a parliamentary system. Legislative authority is held by the Parliament of South Africa. Executive authority ...

(public) sector. In June 2020, dolutegravir was approved in the US with an indication to treat HIV-1 infection in children at least four weeks old and weighing at least 3 kg (6.61 pounds) in combination with other antiretroviral treatments. It is intended to treat children at least 4 weeks old and 3 kg who have never been treated for HIV or who have been treated, but not with an integrase strand transferase inhibitor (INSTI) class drug. The U.S.

(FDA) granted the approval of Tivicay and Tivicay PD to ViiV Healthcare.

References

External links

* {{Portal bar , Medicine , Viruses GSK plc brands Hepatotoxins Integrase inhibitors Organofluorides World Health Organization essential medicines Wikipedia medicine articles ready to translate