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Islatravir
Islatravir (4′-ethynyl-2-fluoro-2′-deoxyadenosine, EFdA, or MK-8591) is an investigational drug for the treatment of HIV infection. It is classified as a nucleoside reverse transcriptase translocation inhibitor (NRTTI). Merck is developing a subdermal drug-eluting implant to administer islatravir. In 2021, FDA placed a partial clinical hold for several studies under Islatravir. The reason was a decline in CD4 T cells under therapy. Merck announced to restart the study program in 2023 with a decreased dose, however studies of islatravir for pre-exposure prophylaxis (PrEP) will be discontinued. In 2024, results from a phase II study combining islatravir with lenacapavir indicated that the regimen shows promise as a possible weekly oral regimen. Biological activity Islatravir has activity against HIV in animal models, and is being studied clinically for HIV treatment and prophylaxis. Islatravir is a nucleoside Nucleosides are glycosylamines that can be thought of as nu ...
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Reverse-transcriptase Inhibitor
Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replication of HIV and other retroviruses. Mechanism of action When HIV infects a cell, reverse transcriptase copies the viral single stranded RNA genome into a double-stranded viral DNA. The viral DNA is then integrated into the host chromosomal DNA, which then allows host cellular processes, such as transcription and translation, to reproduce the virus. RTIs block reverse transcriptase's enzymatic function and prevent completion of synthesis of the double-stranded viral DNA, thus preventing HIV from multiplying. A similar process occurs with other types of viruses. The hepatitis B virus, for example, carries its genetic material in the form of DNA, and employs an RNA-dependent DNA polymerase to replicate. Some of the same compounds used as RTIs c ...
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Lenacapavir
Lenacapavir, sold under the brand name Sunlenca, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is taken by mouth or by subcutaneous injection. Lenacapavir is a human immunodeficiency virus type 1 (HIV-1) capsid inhibitor. The most common side effects include reactions at the injection site and nausea. Lenacapavir was approved for medical treatment in the European Union in August 2022, in Canada in November 2022, and in the United States in December 2022. It is the first of a class of drugs called capsid inhibitors to be approved by the US Food and Drug Administration (FDA) for treating HIV/AIDS. In June 2025, it received approval in the US for HIV prevention. Medical uses Lenacapavir, as Sunlenca, in combination with other antiretrovirals, is indicated for the treatment of HIV/AIDS. It is used in heavily treatment-experienced adults with multiple drug resistance in whom current antiretroviral therapy is ineffective due to resistance, intolerance o ...
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HIV Infection
The human immunodeficiency virus (HIV) is a retrovirus that attacks the immune system. Without treatment, it can lead to a spectrum of conditions including acquired immunodeficiency syndrome (AIDS). It is a preventable disease. It can be managed with treatment and become a manageable chronic health condition. While there is no cure or vaccine for HIV, antiretroviral treatment can slow the course of the disease, and if used before significant disease progression, can extend the life expectancy of someone living with HIV to a nearly standard level. An HIV-positive person on treatment can expect to live a normal life, and die with the virus, not of it. Effective treatment for HIV-positive people (people living with HIV) involves a life-long regimen of medicine to suppress the virus, making the viral load undetectable. Treatment is recommended as soon as the diagnosis is made. An HIV-positive person who has an undetectable viral load as a result of long-term treatment ...
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Merck & Co
Merck & Co., Inc. is an American Multinational corporation, multinational pharmaceutical company headquartered in Rahway, New Jersey. The company does business as Merck Sharp & Dohme or MSD outside the United States and Canada. It is one of the largest pharmaceutical companies in the world, generally ranking in the global top five by revenue. 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 several blockbuster products, including cancer immunotherapy, anti-diabetic medications, and vaccines for HPV and chickenpox, each generating significant revenue as of 2020. The company is ranked 71st on the 2022 Fortune 500, ''Fortune'' 500 and 87th on the 2022 Forbes Global 2000, ''Forbes'' Global 2000, both based on 2021 revenues. In 2023, the company’s seat in the ''Forbes'' Global 2000 was 73. Products The company develops medicines, vaccines, ...
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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. These h ...
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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 responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C). However, the agency also enforces other laws, notably Section 361 of the Public Health Service Act as well as associated regulations. Much of this regulatory-enforcement work is ...
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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. Vaccination is the most commonly used form of pre-exposure prophylaxis; other forms of pre-exposure prophylaxis generally involve drug treatment, known as chemoprophylaxis. Examples include taking medication to prevent infection by malaria or HIV. In particular, the term ''PrEP'' is now synonymous in popular usage with the use of pre-exposure prophylaxis for HIV prevention. In general, the use of pre-exposure prophylaxis requires balancing the risks of the treatment (e.g., side effects from a drug) to healthy individuals with the risk of the disease. It should be contrasted with post-exposure prophylaxis, which is used once the patient has already been exposed to the infectious agent. Use of pre-exposure medication against specific diseases Malaria The use of pre-exposure drug treatment to prevent malaria usin ...
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Animal Model
An animal model (short for animal disease model) is a living, non-human, often genetic-engineered animal used during the research and investigation of human disease, for the purpose of better understanding the disease process without the risk of harming a human. Although biological activity in an animal model does not ensure an effect in humans, many drugs, treatments and cures for human diseases are developed in part with the guidance of animal models. Animal models representing specific taxonomic groups in the research and study of developmental processes are also referred to as model organisms. There are three main types of animal models: Homologous, Isomorphic and Predictive. Homologous animals have the same causes, symptoms and treatment options as would humans who have the same disease. Isomorphic animals share the same symptoms and treatments, only. Predictive models are similar to a particular human disease in only a couple of aspects. However, these are useful in isolating ...
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Nucleoside
Nucleosides are glycosylamines that can be thought of as nucleotides without a phosphate group. A nucleoside consists simply of a nucleobase (also termed a nitrogenous base) and a five-carbon sugar (ribose or 2'-deoxyribose) whereas a nucleotide is composed of a nucleobase, a five-carbon sugar, and one or more phosphate groups. In a nucleoside, the anomeric carbon is linked through a glycosidic bond to the N9 of a purine or the N1 of a pyrimidine. Nucleotides are the molecular building blocks of DNA and RNA. List of nucleosides and corresponding nucleobases ''This list does not include modified nucleobases and the corresponding nucleosides'' Each chemical has a short symbol, useful when the chemical family is clear from the context, and a longer symbol, if further disambiguation is needed. For example, long nucleobase sequences in genomes are usually described by CATG symbols, not Cyt-Ade-Thy-Gua (see '' Nucleic acid sequence § Notation''). Sources Nucleosides can ...
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Nucleoside Analog Reverse Transcriptase Inhibitors
Nucleosides are glycosylamines that can be thought of as nucleotides without a phosphate group. A nucleoside consists simply of a nucleobase (also termed a nitrogenous base) and a five-carbon sugar (ribose or 2'-deoxyribose) whereas a nucleotide is composed of a nucleobase, a five-carbon sugar, and one or more phosphate groups. In a nucleoside, the anomeric carbon is linked through a glycosidic bond to the N9 of a purine or the N1 of a pyrimidine. Nucleotides are the molecular building blocks of DNA and RNA. List of nucleosides and corresponding nucleobases ''This list does not include modified nucleobases and the corresponding nucleosides'' Each chemical has a short symbol, useful when the chemical family is clear from the context, and a longer symbol, if further disambiguation is needed. For example, long nucleobase sequences in genomes are usually described by CATG symbols, not Cyt-Ade-Thy-Gua (see '' Nucleic acid sequence § Notation''). Sources Nucleosides can b ...
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Ethynyl Compounds
In organic chemistry, an ethynyl group is a functional group with the formula −C≡CH, representing an acetylene molecule with one fewer hydrogen atom. * Ethynyl group (HC≡C–), also designated as an acetylenic group (from acetylene), is referred to in IUPAC chemical nomenclature with the -yne suffix. It is sometimes designated as ''ethinyl'' in compounds such as ethinylestradiol and ethisterone (ethinyltestosterone). See main page alkynes. See also * Ethynylation * Ethynyl radical * Propynyl (H3C–C≡C–R, 1-propynyl group; or HC≡C–CH2–R, 2-propynyl group, Propargyl In organic chemistry, the propargyl group is a functional group of 2- propynyl with the structure . It is an alkyl group derived from propyne (). The term propargylic refers to a saturated position ( ''sp''3-hybridized) on a molecular framework ...) Alkynyl groups {{hydrocarbon-stub ...
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Fluoroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ...
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