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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] |
Integrase Inhibitors
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] |
Merck & Co
Merck & Co., Inc. is an American multinational pharmaceutical company headquartered in Rahway, New Jersey, and is named for Merck Group, founded in Germany in 1668, of whom it was once the American arm. The company does business as Merck Sharp & Dohme or MSD outside the United States and Canada. Merck & Co. was originally established as the American affiliate of Merck Group in 1891. Merck develops and produces medicines, vaccines, biologic therapies and animal health products. It has multiple blockbuster drugs or products each with 2020 revenues including cancer immunotherapy, anti-diabetic medication and vaccines against HPV and chickenpox. The company is ranked 71st on the 2022 ''Fortune'' 500 and 87th on the 2022 ''Forbes'' Global 2000, both based on 2021 revenues. Products The company develops medicines, vaccines, biologic therapies and animal health products. In 2020, the company had 6 blockbuster drugs or products, each with over $1 billion in revenue: ''Keytruda' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Discovery And Development Of Integrase Inhibitors
Discovery may refer to: * Discovery (observation), observing or finding something unknown * Discovery (fiction), a character's learning something unknown * Discovery (law), a process in courts of law relating to evidence Discovery, The Discovery or Discoveries may also refer to: Film and television * ''The Discovery'' (film), a 2017 British-American romantic science fiction film * Discovery Channel, an American TV channel owned by Warner Bros. Discovery * ''Discovery'' (Canadian TV series), a 1962–1963 Canadian documentary television program * ''Discovery'' (Irish TV series), an Irish documentary television programme * ''Discovery'' (UK TV programme), a British documentary television programme * ''Discovery'' (U.S. TV series), a 1962–1971 American television news program * '' Star Trek: Discovery'', an American television series ** USS ''Discovery'' (NCC-1031), a fictional space craft on ''Star Trek: Discovery'' Literature * ''The Discovery'' (Frances Sheridan p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Raltegravir
Raltegravir, sold under the brand name Isentress, 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, nausea, high blood sugar, and headaches. Severe side effects may include allergic reactions including Stevens–Johnson syndrome, muscle breakdown, and liver problems. It is unclear if use during pregnancy or breastfeeding is safe. Raltegravir is an HIV integrase strand transfer inhibitor which blocks the functioning of HIV integrase which is needed for viral replication. Raltegravir was approved for medical use in the United States in 2007. It is on the World Health Organization's List of Essential Medicines. Lamivudine/raltegravir, a combination with lamivudine, is also available. Medical uses Raltegravir was initially approved only for use ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 term typically refers to the use of antiviral drugs as a strategy for the prevention of HIV/AIDS. PrEP is one of a number of HIV prevention strategies for people who are HIV negative but who have a higher risk of acquiring HIV, including sexually active adults at increased risk of contracting HIV, people who engage in intravenous drug use (see drug injection), and serodiscordant sexually active couples. When used as directed, PrEP has been shown to be highly effective, reducing the risk of acquiring HIV by up to 99%. , the World Health Organization (WHO) recommends two drug combinations for the use as PrEP for HIV/AIDS: the combination of tenofovir disoproxil and emtricitabine (Truvada), or the combination of tenofovir disoproxil and lamivudine (Cimduo). In October 2019, the US Food and Drug Admi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
