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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, 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 discovery and development of integrase inhibitors, development of integrase inhibitors led to a first approval for the class by the Food and Drug Administration (United States), 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 bac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiretroviral Drug
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 s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tenofovir Disoproxil
Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention of HIV/AIDS among those at high risk before exposure, and after a needlestick injury or other potential exposure. It is sold both by itself and together in combinations such as emtricitabine/tenofovir, efavirenz/emtricitabine/tenofovir, and elvitegravir/cobicistat/emtricitabine/tenofovir. It does not cure HIV/AIDS or hepatitis B. It is available by mouth as a tablet or powder. Common side effects include nausea, rash, diarrhea, headache, pain, depression, and weakness. Severe side effects include high blood lactate and an enlarged liver. There are no absolute contraindications. It is often recommended during pregnancy and appears to be safe. It is a nucleotide reverse transcriptase inhibitor and works by decreasing the ability o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MK-2048
MK-2048 is the Merck & Co. designation for a molecule in its pre-clinical drug discovery that is an integrase inhibitor-class of agent intended to be used against HIV infection. It is a second generation integrase design thought to be superior to the first available integrase inhibitor, raltegravir, in that "MK-2048 has a dissociation half-life of 32 hours on wild-type integrase—more than four times that of raltegravir", and its dissociation half-life against the important HIV integrase mutant N155H was on the same order of magnitude as that of raltegravir against wild-type virus, leading the Merck presenter to suggest the possibility of "reduced susceptibility to resistance mutations" for the second generation drug. MK-2048 is being investigated for use as part of a pre-exposure prophylaxis Pre-exposure prophylaxis (PrEP) is the use of medications to prevent the spread of disease in people who have not yet been exposed to a disease-causing agent, usually a virus. The ter ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BI 224436
BI 224436 was an investigational new drug under development for the treatment of HIV infection. BI 224436 is the first non-catalytic site integrase inhibitor (NCINI). It inhibits HIV replication via binding to a conserved allosteric pocket of the HIV integrase enzyme. This makes the drug distinct in its mechanism of action compared to raltegravir and elvitegravir, which bind at the catalytic site. In October 2011, Gilead Sciences purchased exclusive rights to develop BI 224436 and several related compounds under investigation in Boehringer Ingelheim C.H. Boehringer Sohn AG & Co. is the parent company of the Boehringer Ingelheim group, which was founded in 1885 by Albert Boehringer in Ingelheim am Rhein, Germany. As of 2018, Boehringer Ingelheim is one of the world's largest pharmaceutical ...’s noncatalytic site integrase inhibitor program. Clinical trials were abandoned in advance of Phase 1. References Integrase inhibitors Experimental drugs Tert-butyl com ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cabotegravir/rilpivirine
Cabotegravir/rilpivirine, sold under the brand name Cabenuva, is a co-packaged antiretroviral medication for the treatment of HIV/AIDS. It contains cabotegravir and rilpivirine in a package with two separate injection vials. The most common adverse reactions include injection site reactions, fever or feeling hot (pyrexia), fatigue, headache, musculoskeletal pain, nausea, sleep disorders, dizziness and rash. The co-packaged medication was approved for medical use in the United States in January 2021. It is the first FDA-approved injectable, complete regimen for HIV-infected adults that is administered once a month. It is also approved for use in Canada. In the European Union, the two medications are approved separately. Medical uses Cabotegravir/rilpivirine is indicated as a complete regimen for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults to replace a current antiretroviral regimen in those who are virologically suppressed on a stable a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rilpivirine
Rilpivirine, sold under the brand names Edurant and Rekambys, is a medication, developed by Tibotec, used for the treatment of HIV/AIDS. It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs such as efavirenz. Medical uses In the US, rilpivirine is approved for treatment-naive patients with a viral load of 100,000 copies/mL or less at therapy initiation. It has to be combined with other drugs against HIV.Rilpivirine . Accessed 2021-02-23. In the European Union, rilpivirine is approved in combination with cabotegravir for maintenance treatment of adults who have undetectable HIV levels in the blood (viral load less than 50 copies/ml) with their current antiretroviral treatment, and when the virus has not developed resistance to certain class of anti-HIV medicines called non-nucleoside reverse transcriptase inhibitors (NNRTIs) and integrase strand transfe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cabotegravir
Cabotegravir, sold under the brand name Vocabria among others, is a antiretroviral medication used for the treatment of HIV/AIDS. It is available in the form of tablets and as an intramuscular injection, as well as in an injectable combination with rilpivirine under the brand name Cabenuva. It is an integrase inhibitor with a carbamoyl pyridone structure similar to that of dolutegravir. In December 2021, the U.S. Food and Drug Administration approved cabotegravir for pre-exposure prophylaxis (PrEP) in at-risk people under the brand name Apretude. Medical uses Cabotegravir in combination with rilpivirine is indicated for the treatment of human immunodeficiency virus type-1 (HIV-1) in adults. The combination injection is intended for maintenance treatment of adults who have undetectable HIV levels in the blood (viral load less than 50 copies/mL) with their current antiretroviral treatment, and when the virus has not developed resistance to non-nucleoside reverse transcriptas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bictegravir/emtricitabine/tenofovir Alafenamide
Bictegravir/emtricitabine/tenofovir alafenamide, sold under the brand name Biktarvy, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. One tablet, taken orally once daily, contains 50mg bictegravir, 200mg emtricitabine, and 25mg tenofovir alafenamide. It was approved for use in the United States in February 2018, and for use in the European Union in June 2018. Combination therapy Bictegravir/emtricitabine/tenofovir alafenamide is an example of a combination drug that can be taken as a complete regimen for treatment of the human immunodeficiency virus. Combination therapy for HIV, often called highly active antiretroviral therapy (HAART), is composed of two or more types of antiretroviral drugs. Combination therapy decreases the likelihood that drug resistance will occur, because it is unlikely that the HIV-1 strains will be able to mutate enough to become resistant to all drugs being used in the combination. Combination therapy increase ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ViiV Healthcare
ViiV Healthcare ( ) is a pharmaceutical company specializing in the development of therapies for HIV infection that was created as a joint venture by Pfizer and GlaxoSmithKline in November 2009 with both companies transferring their HIV assets to the new company.Jacks, Andre"GSK and Pfizer to Merge HIV PortfoliosFinancial Times. 16 April 2010 In 2012 Shionogi joined the company. 76.5% of the company is now owned by GlaxoSmithKline, 13.5% by Pfizer and 10% by Shionogi. This ownership structure may change depending upon the achievement of certain milestones. ViiV Healthcare's products have a market share of approximately 19% of the global HIV market, making it the second-largest healthcare company, after Gilead Sciences, which is working on the treatment of HIV. ViiV Healthcare's headquarters are in Brentford in the United Kingdom and it has sites in a number of other countries including; the United States, Australia, Belgium, Canada, France, Germany, Italy, Japan, Mexico, the N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dolutegravir
Dolutegravir (DTG), sold under the brand name Tivicay, is an antiretroviral medication used, together with other medication, to treat HIV/AIDS. It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential exposure. It is taken by mouth. Common side effects include trouble sleeping, feeling tired, diarrhea, high blood sugar, and headache. Severe side effects may include allergic reactions and liver problems. There are tentative concerns that use during pregnancy can result in harm to the baby. It is unclear if use during breastfeeding is safe. Dolutegravir is an HIV integrase strand transfer inhibitor which blocks the functioning of HIV integrase which is needed for viral replication. Dolutegravir was approved for medical use in the United States in 2013. It is on the World Health Organization's List of Essential Medicines. Abacavir/dolutegravir/lamivudine, a combination with abacavir and lamivudine is also available. As of 2019, the Wo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elvitegravir/cobicistat/emtricitabine/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 St ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinolone Antibiotic
A quinolone antibiotic is a member of a large group of broad-spectrum bacteriocidals that share a bicyclic core structure related to the substance 4-quinolone. They are used in human and veterinary medicine to treat bacterial infections, as well as in animal husbandry, specifically poultry production. Nearly all quinolone antibiotics in use are fluoroquinolones, which contain a fluorine atom in their chemical structure and are effective against both Gram-negative and Gram-positive bacteria. One example is ciprofloxacin, one of the most widely used antibiotics worldwide. Medical uses Fluoroquinolones are often used for genitourinary infections and are widely used in the treatment of hospital-acquired infections associated with urinary catheters. In community-acquired infections, they are recommended only when risk factors for multidrug resistance are present or after other antibiotic regimens have failed. However, for serious acute cases of pyelonephritis or bacterial pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
