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Cobicistat
Cobicistat, sold under the brand name Tybost, is a medication for use in the treatment of human immunodeficiency virus infection (HIV/AIDS). Its major mechanism of action is through the inhibition of human CYP3A proteins. Like ritonavir (Norvir), cobicistat is of interest for its ability to inhibit liver enzymes that metabolize other medications used to treat HIV, notably elvitegravir, an HIV integrase inhibitor. By combining cobicistat with elvitegravir, higher concentrations of the latter are achieved in the body with lower dosing, theoretically enhancing elvitegravir's viral suppression while diminishing its adverse side-effects. In contrast with ritonavir, the only other booster approved for use as a part of HAART, cobicistat has no anti-HIV activity of its own.Highleyman, L.Elvitegravir "Quad" Single-tablet Regimen Shows Continued HIV Suppression at 48 Weeks HIV and Hepatitis.com Cobicistat is a component of three four-drug, fixed-dose combination HIV treatments. The first, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tenofovir Alafenamide
Tenofovir alafenamide, sold under the brand name Vemlidy, is a hepatitis B virus (HBV) nucleotide reverse transcriptase inhibitor medication for the treatment of chronic hepatitis B virus (HBV) infection in adults with compensated liver disease. It is taken by mouth. Tenofovir alafenamide is a prodrug of tenofovir. It was developed by Gilead Sciences based on the protide technology of Chris McGuigan for use in the treatment of HIV/AIDS and chronic hepatitis B, and is applied in the form of tenofovir alafenamide fumarate (TAF). Closely related to the commonly used reverse-transcriptase inhibitor tenofovir disoproxil fumarate (TDF), TAF has greater antiviral activity and better distribution into lymphoid tissues than that agent. Vemlidy was approved by the U.S. Food and Drug Administration (FDA) in November 2016. Fixed-dose combinations containing tenofovir alafenamide * Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (Genvoya) — approved both in the United Sta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atazanavir/cobicistat
Atazanavir/cobicistat, sold under the brand name Evotaz, is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS. It contains atazanavir and cobicistat. Atazanavir is an HIV protease inhibitor and cobicistat is an inhibitor of cytochrome P450 (CYP) enzymes of the CYP3A family. Atazanavir/cobicistat was approved by the Food and Drug Administration (FDA) for medical use in United States in January 2015. It was approved for medical use in the European Union in July 2015. Medical uses Atazanavir/cobicistat is indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ... for use in combination with other antiretroviral agents for the treatment of HIV‑1 infection in people weighing at least . References External links * Antiretroviral drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Darunavir/cobicistat
Darunavir/cobicistat, sold under the brand names Prezcobix (US) and Rezolsta (EU), is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS. It contains darunavir and cobicistat. Darunavir is an HIV protease inhibitor and cobicistat increases the effectiveness of darunavir by blocking its metabolism by the enzyme CYP3A Cytochrome P450, family 3, subfamily A, also known as CYP3A, is a human gene locus. A homologous locus is found in mice. The CYP3A locus includes all the known members of the 3A subfamily of the cytochrome P450 superfamily of genes. These genes .... Darunavir/cobicistat was approved for use in the European Union in November 2014, and for use in the United States in January 2015. References External links * * * Antiretroviral drugs CYP3A4 inhibitors Fixed dose combination (antiretroviral) {{antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elvitegravir/cobicistat/emtricitabine/tenofovir Disoproxil
Elvitegravir/cobicistat/emtricitabine/tenofovir, sold under the brand name Stribild, also known as the Quad pill, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. Elvitegravir, emtricitabine and tenofovir disoproxil directly suppress viral reproduction. Cobicistat increases the effectiveness of the combination by inhibiting the liver and gut wall enzymes that metabolize elvitegravir. It is taken by mouth. The drug is manufactured by Gilead Sciences. An increase in the serum creatinine level (a marker of kidney function) may increase with use of Elvitegravir/cobicistat/emtricitabine/tenofovir. This is caused by inhibition of tubular secretion of creatinine in the nephron by cobicistat. An increase of up to 0.3 mg/dL is expected; if serum creatinine level increases by 0.4 mg/dL or more, further evaluation for other causes of acute kidney injury is recommended. Society and culture Legal status Elvitegravir/cobicistat/emtricitabine/ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Integrase 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, blocking it can halt further spread of the virus. Integrase inhibitors were initially developed for the treatment of HIV infection but have been applied to other retroviruses. The class of integrase inhibitors called integrase strand transfer inhibitors (INSTIs) are in established medical use. Other classes, such as integrase binding inhibitors (INBIs), are still experimental. The development of integrase inhibitors led to a first approval for the class by the U.S. Food and Drug Administration (FDA) on October 12, 2007, for raltegravir (brand name Isentress). Research published at the time supported the conclusion that "raltegravir plus optimized background therapy provided better viral suppression than optimized background therapy alone for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Darunavir
Darunavir (DRV), sold under the brand name Prezista among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It is often used with low doses of ritonavir or cobicistat to increase darunavir levels. It may be used for prevention after a needlestick injury or other potential exposure. It is taken by mouth once to twice a day. Common side effects include diarrhea, nausea, abdominal pain, headache, rash and vomiting. Severe side effects include allergic reactions, liver problems, and skin rashes such as toxic epidermal necrolysis. While poorly studied in pregnancy it appears to be safe for the baby. It is of the protease inhibitor (PI) class and works by blocking HIV protease. Developed by pharmaceutical company Tibotec, darunavir is named after Arun K. Ghosh, the chemistry professor who discovered the molecule at the University of Illinois at Chicago. It was approved by the Food and Drug Adm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bristol-Myers Squibb
The Bristol Myers Squibb Company (BMS) is an American multinational pharmaceutical company. Headquartered in New York City, BMS is one of the world's largest pharmaceutical companies and consistently ranks on the ''Fortune'' 500 list of the largest U.S. corporations. For fiscal 2021, it had a total revenue of $46.4 billion. Bristol Myers Squibb manufactures prescription pharmaceuticals and biologics in several therapeutic areas, including cancer, HIV/AIDS, cardiovascular disease, diabetes, hepatitis, rheumatoid arthritis, and psychiatric disorders. BMS's primary research and development (R&D) sites are located in Lawrence, New Jersey (formerly Squibb, near Princeton), Summit, New Jersey, formerly HQ of Celgene, New Brunswick, New Jersey, Redwood City, California, and Seville in Spain, with other sites in Devens and Cambridge, Massachusetts, East Syracuse, New York, Braine-l'Alleud, Belgium, Tokyo, Japan, Bangalore, India, and Wirral, United Kingdom. BMS previously had ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP3A4
Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body. It is highly homologous to CYP3A5, another important CYP3A enzyme. While many drugs are deactivated by CYP3A4, there are also some drugs which are ''activated'' by the enzyme. Some substances, such as some drugs and furanocoumarins present in grapefruit juice, interfere with the action of CYP3A4. These substances will therefore either amplify or weaken the action of those drugs that are modified by CYP3A4. CYP3A4 is a member of the cytochrome P450 family of oxidizing enzymes. Several other members of this family are also involved in drug metabolism, but CYP3A4 is the most common and the most versatile one. Like all members of this family, it is a hemoprotein, i.e. a protein containing a heme group with an iron atom. In humans, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 may not notice any symptoms, or may experience a brief period of influenza-like illness. Typically, this is followed by a prolonged incubation period with no symptoms. If the infection progresses, it interferes more with the immune system, increasing the risk of developing common infections such as tuberculosis, as well as other opportunistic infections, and tumors which are rare in people who have normal immune function. These late symptoms of infection are referred to as acquired immunodeficiency syndrome (AIDS). This stage is often also associated with unintended weight loss. HIV is spread primarily by unprotected sex (including anal and vaginal sex), contaminated blood transfusions, hypodermic needles, and from mother to ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elvitegravir
Elvitegravir (EVG) is an integrase inhibitor used to treat HIV infection. It was developed by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008. The drug gained approval by the U.S. Food and Drug Administration on August 27, 2012 for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild. On September 24, 2014 the FDA approved Elvitegravir as a single pill formulation under the trade name Vitekta. On November 5, 2015 the FDA approved the drug for use in patients affected with HIV-1 as a part of a second fixed dose combination pill known as Genvoya. According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor. Medical uses In the United States, elvitegravir can be obtained eithe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Management Of HIV/AIDS
The management of HIV/AIDS normally includes the use of multiple antiretroviral drugs as a strategy to control HIV infection. There are several classes of antiretroviral agents that act on different stages of the HIV life-cycle. The use of multiple drugs that act on different viral targets is known as highly active antiretroviral therapy (HAART). HAART decreases the patient's total burden of HIV, maintains function of the immune system, and prevents opportunistic infections that often lead to death. HAART also prevents the transmission of HIV between serodiscordant same sex and opposite sex partners so long as the HIV-positive partner maintains an undetectable viral load. Treatment has been so successful that in many parts of the world, HIV has become a chronic condition in which progression to AIDS is increasingly rare. Anthony Fauci, head of the United States National Institute of Allergy and Infectious Diseases, has written, "With collective and resolute action now and a steadfa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxy Group
In chemistry, a hydroxy or hydroxyl group is a functional group with the chemical formula and composed of one oxygen atom covalently bonded to one hydrogen atom. In organic chemistry, alcohols and carboxylic acids contain one or more hydroxy groups. Both the negatively charged anion , called hydroxide, and the neutral radical , known as the hydroxyl radical, consist of an unbonded hydroxy group. According to IUPAC definitions, the term ''hydroxyl'' refers to the hydroxyl radical () only, while the functional group is called a ''hydroxy group''. Properties Water, alcohols, carboxylic acids, and many other hydroxy-containing compounds can be readily deprotonated due to a large difference between the electronegativity of oxygen (3.5) and that of hydrogen (2.1). Hydroxy-containing compounds engage in intermolecular hydrogen bonding increasing the electrostatic attraction between molecules and thus to higher boiling and melting points than found for compounds that lack this ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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