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BMS-955176
BMS-955176 is an experimental second generation HIV maturation inhibitor under development by Bristol-Myers Squibb for use in the treatment of HIV infection. By blocking the maturation of the virus, it prevents viral reproduction in host CD4+ T cells. First generation maturation inhibitors such as bevirimat were ineffective against some naturally occurring changes (polymorphisms) in the Gag protease HIV-1 protease (PR) is a retroviral aspartyl protease (retropepsin), an enzyme involved with peptide bond hydrolysis in retroviruses, that is essential for the life-cycle of HIV, the retrovirus that causes AIDS. HIV protease cleaves newly synthe ... polyprotein; BMS-955176 has been selected to better tolerate gag polymorphisms. __TOC__ Studies Results of a phase 2a trial of BMS-955176 was reported at the 2015 Conference on Retroviruses and Opportunistic Infections (CROI). Investigators concluded that the drug was well tolerated and effective against HIV, including strains w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Maturation Inhibitor
The maturation inhibitors are a class of antiviral drugs for the treatment of infection with HIV. They act by interfering with the maturation of the virus. Specifically, drugs in this class disrupt the final step in the processing of the HIV-1 ''gag'' protein, the cleavage of its immediate precursor by the enzyme HIV-1 protease HIV-1 protease (PR) is a retroviral aspartyl protease (retropepsin), an enzyme involved with peptide bond hydrolysis in retroviruses, that is essential for the life-cycle of HIV, the retrovirus that causes AIDS. HIV protease cleaves newly synthesi .... Unlike the class of drugs known as protease inhibitors, maturation inhibitors bind the ''gag'' protein, not the protease. This leads to the formation of noninfectious, immature virus particles, incapable of infecting other cells. No other class of drugs shares this mechanism of action, thus maturation inhibitors retain inhibitory activity against HIV infections with resistance. There are no currently availa ... [...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 pre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bevirimat
Bevirimat (research code MPC-4326) is an anti-HIV drug derived from a betulinic acid-like compound, first isolated from ''Syzygium claviflorum,'' a Chinese herb. It is believed to inhibit HIV by a novel mechanism, so-called maturation inhibition. It is not currently U.S. Food and Drug Administration (FDA) approved. It was originally developed by the pharmaceutical company Panacos and reached Phase IIb clinical trials. Myriad Genetics announced on January 21, 2009 the acquisition of all rights to bevirimat for $7M USD. On June 8, 2010 Myriad Genetics announced that it was halting the development of maturation inhibitors, including bevirimat, to focus more on their oncology portfolio. Pharmacokinetics According to the only currently available study, "the mean terminal elimination half-life of bevirimat ranged from 56.3 to 69.5 hours, and the mean clearance ranged from 173.9 to 185.8 mL/hour." Mechanism of action Like protease inhibitors, bevirimat and other maturation inhibito ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fipravirimat
Fipravirimat is an experimental drug for the treatment of 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 belongs to a class of drugs known as maturation inhibitors. Fipravirimat is being developed by ViiV Healthcare and as of 2023 is in Phase II clinical trials. See also * BMS-955176 References {{antiinfective-drug-stub Antiviral drugs Carboxylic acids Organofluorides Pentacyclic compounds Sulfones ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Development
Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regulatory status, such as via the United States Food and Drug Administration for an investigational new drug to initiate clinical trials on humans, and may include the step of obtaining regulatory approval with a new drug application to market the drug. The entire process – from concept through preclinical testing in the laboratory to clinical trial development, including Phase I–III trials – to approved vaccine or drug typically takes more than a decade. New chemical entity development Broadly, the process of drug development can be divided into preclinical and clinical work. Pre-clinical New chemical entities (NCEs, also known as new molecular entities or NMEs) are compounds that emerge from the process of drug discovery. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gag Protease
HIV-1 protease (PR) is a retroviral aspartyl protease (retropepsin), an enzyme involved with peptide bond hydrolysis in retroviruses, that is essential for the life-cycle of HIV, the retrovirus that causes AIDS. HIV protease cleaves newly synthesized polyproteins (namely, Gag and Gag- Pol) at nine cleavage sites to create the mature protein components of an HIV virion, the infectious form of a virus outside of the host cell. Without effective HIV protease, HIV virions remain uninfectious. Structure Mature HIV protease exists as a 22 kDa homodimer, with each subunit made up of 99 amino acids. A single active site lies between the identical subunits and has the characteristic Asp- Thr-Gly (Asp25, Thr26 and Gly27) catalytic triad sequence common to aspartic proteases. As HIV-1 PR can only function as a dimer, the mature protease contains two Asp25 amino acids, one from each monomer, that act in conjunction with each other as the catalytic residues. Additionally, HIV pro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Polymorphism (biology)
In biology, polymorphism is the occurrence of two or more clearly different morphs or forms, also referred to as alternative ''phenotypes'', in the population of a species. To be classified as such, morphs must occupy the same habitat at the same time and belong to a panmictic population (one with random mating). Ford E.B. 1965. ''Genetic polymorphism''. Faber & Faber, London. Put simply, polymorphism is when there are two or more possibilities of a trait on a gene. For example, there is more than one possible trait in terms of a jaguar's skin colouring; they can be light morph or dark morph. Due to having more than one possible variation for this gene, it is termed 'polymorphism'. However, if the jaguar has only one possible trait for that gene, it would be termed "monomorphic". For example, if there was only one possible skin colour that a jaguar could have, it would be termed monomorphic. The term polyphenism can be used to clarify that the different forms arise from the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, pharmaceutical drug, drugs, medical nutrition therapy, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received institutional review board, health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small Pilot experiment, pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Conference On Retroviruses And Opportunistic Infections
The Conference on Retroviruses and Opportunistic Infections (CROI) is an annual scientific meeting devoted to the understanding, prevention and treatment of HIV/ AIDS and the opportunistic infection An opportunistic infection is an infection caused by pathogens (bacteria, fungi, parasites or viruses) that take advantage of an opportunity not normally available. These opportunities can stem from a variety of sources, such as a weakened immun ...s associated with AIDS. Thousands of leading researchers and clinicians from around the world convene in a different location in North America each year for the Conference. List of conferences Below is the list of conferences and their venue: External links * {{Official website, http://www.croiconference.org/ Webcasts of past conferencesConference Manager, IAS-USA International AIDS Conferences Recurring events established in 1993 Annual events in the United States ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiretroviral Drugs
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 stea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Maturation Inhibitors
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Maturation is the process of becoming mature; the emergence of individual and behavioral characteristics through growth processes over time. Maturation may refer to: Science * Developmental psychology * Foetal development * Maturity (geology), in petroleum geology * Maturation, as a threat to internal validity of an experiment * Tissue maturation, an aspect of developmental biology ** The final stages of cellular differentiation of cells, tissues, or organs See also * Expiration (other) * Maturity (other) * Mature (other) Mature is the adjectival form of maturity, as immature is the adjectival form of immaturity, which have several meanings. Mature or immature may also refer to: * Mature, a character from ''The King of Fighters'' series *"Mature 17+", a rating in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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