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NITD609
Cipargamin (NITD609, KAE609) is an experimental synthetic antimalarial drug belonging to the spiroindolone class.{{cite journal, title=Spiroindolones, a potent compound class for the treatment of malaria , journal=Science , year=2010 , volume=329 , issue=5996 , pages=1175–80 , pmid=20813948 , doi=10.1126/science.1193225, vauthors=Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J, Cohen SB, Spencer KR, González-Páez GE, Lakshminarayana SB, Goh A, Suwanarusk R, Jegla T, Schmitt EK, Beck HP, Brun R, Nosten F, Renia L, Dartois V, Keller TH, Fidock DA, Winzeler EA, Diagana TT, author25-link=David A. Fidock , pmc=3050001, bibcode=2010Sci...329.1175R The compound was developed at the Novartis Institute for Tropical Diseases in Singapore, through a collaboration with the Genomics Institute of the Novartis Research Foundation (GNF), the Biomedical Primate Research Centre and the Swiss Tropical Institute. Cipargamin is a synthetic antim ...
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Spiroindolone
The spiroindolones are a class of compounds in which an indolone ring is substituted with another ring in a spiro arrangement. Alkaloids in this class include horsfiline, rhynchophylline, gelsemine, carapanaubine, and maremycin E. Spiroindolones are also an emerging class of antimalarial drugs whose mode of action is to inhibit protein synthesis in the target parasite. The most advanced compound in this class in terms of 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 re ... is cipargamin (NITD609). References Antimalarial agents Spiro compounds {{antiinfective-drug-stub ...
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Antimalarial Medication
Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria, in the latter case, most often aiming at two susceptible target groups, young children and pregnant women. As of 2018, modern treatments, including for severe malaria, continued to depend on therapies deriving historically from quinine and artesunate, both parenteral (injectable) drugs, expanding from there into the many classes of available modern drugs. Incidence and distribution of the disease ("malaria burden") is expected to remain high, globally, for many years to come; moreover, known antimalarial drugs have repeatedly been observed to elicit resistance in the malaria parasite—including for combination therapies featuring artemisinin, a drug of last resort, where resistance has now been observed in Southeast Asia. As such, the needs for new antimalarial agents and new strategies of treatment (e.g., new combin ...
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Novartis Institute For Tropical Diseases
The Novartis Institute for Tropical Disease (NITD) was a Singapore-based tropical disease research institute created through a public-private partnership between Novartis and the Singapore Economic Development Board. Research at NITD focuses primarily on developing novel small molecule therapies for tropical infectious diseases that are endemic to the developing world, particularly dengue fever, malaria and tuberculosis. History and mission NITD was founded in 2002 as a public-private partnership between Swiss-based pharmaceutical company Novartis and the Singapore Economic Development Board. NITD states its goals are "to discover novel treatments and prevention methods for major tropical diseases." Their website states they hope to have at least two drug candidates going through clinical trials in patients by the year 2012. Novartis has also stated that the NITD will seek to make treatments developed by the NITD available without profit to the poor in developing nations in ...
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Genomics Institute Of The Novartis Research Foundation
Novartis AG is a Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and Cambridge, Massachusetts, United States (global research).name="novartis.com">https://www.novartis.com/research-development/research-locations It is one of the largest pharmaceutical companies in the world. Novartis manufactures the drugs clozapine (Clozaril), diclofenac (Voltaren; sold to GlaxoSmithKline in 2015 deal), carbamazepine (Tegretol), valsartan (Diovan), imatinib mesylate (Gleevec/Glivec), cyclosporine (Neoral/Sandimmune), letrozole (Femara), methylphenidate (Ritalin; production ceased 2020), terbinafine (Lamisil), deferasirox (Exjade), and others. In March 1996, the companies Ciba-Geigy and Sandoz merged to form Novartis; the pharmaceutical and agrochemical divisions of both companies formed Novartis as an independent entity. Other Ciba-Geigy and Sandoz businesses were sold, or, like Ciba Specialty Chemicals, spun off as independent companies. The Sandoz bran ...
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Biomedical Primate Research Centre
The Biomedical Primate Research Centre (BPRC) is Europe's largest primate animal testing research centre. It is a scientific research institute that performs research that contributes to the identification and development of new medicines against deadly diseases. It is located in Rijswijk (South Holland) and employs about 110 people. The BPRC is funded by the Dutch Ministry of Education, Culture and Science. Before it became an independent foundation on December 7, 1994, it was part of the Netherlands Organisation for Applied Scientific Research. The main research areas are Immunobiology, Parasitology, Virology, Ethology and Alternatives for Animal Research. The BPRC houses rhesus macaques and marmosets to be used in biomedical research involving AIDS, malaria, hepatitis, tuberculosis and auto-immune diseases. In 2002 the Dutch government forbade any further testing on chimpanzees, though it allowed trials already in progress to end. In 2015, BPRC was reported to use about 20 ...
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Swiss Tropical Institute
The Swiss Tropical and Public Health Institute or Swiss TPH (formerly known as the Swiss Tropical Institute) is an international public health institute working in various disciplines with a particular focus on low- and middle-income countries. It was founded in 1943 through the initiative of Rudolf Geigy. Swiss TPH endeavors to the improve the health of populations internationally and nationally through research, services, education, and training, with a focus on developing countries. In June 2009, the Institute for Social and Preventive Medicine of the University of Basel was integrated into the Swiss Tropical Institute, and in January 2010 the Swiss Tropical Institute changed its name to the Swiss Tropical and Public Health Institute. The Swiss TPH is an associated institute of the University of Basel, and as a public organization it is partially supported by the Swiss Federal Council and the Canton of Basel-Stadt. The greater part of its funding comes from competitively acquir ...
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Plasmodium Falciparum
''Plasmodium falciparum'' is a Unicellular organism, unicellular protozoan parasite of humans, and the deadliest species of ''Plasmodium'' that causes malaria in humans. The parasite is transmitted through the bite of a female ''Anopheles'' mosquito and causes the disease's most dangerous form, falciparum malaria. It is responsible for around 50% of all malaria cases. ''P. falciparum'' is therefore regarded as the deadliest parasite in humans. It is also associated with the development of blood cancer (Burkitt's lymphoma) and is classified as a List of IARC Group 2A carcinogens, Group 2A (probable) carcinogen. The species originated from the malarial parasite ''Laverania'' found in gorillas, around 10,000 years ago. Alphonse Laveran was the first to identify the parasite in 1880, and named it ''Oscillaria malariae''. Ronald Ross discovered its transmission by mosquito in 1897. Giovanni Battista Grassi elucidated the complete transmission from a female Anopheles, anopheline mosquit ...
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Phenotypic
In genetics, the phenotype () is the set of observable characteristics or traits of an organism. The term covers the organism's morphology or physical form and structure, its developmental processes, its biochemical and physiological properties, its behavior, and the products of behavior. An organism's phenotype results from two basic factors: the expression of an organism's genetic code, or its genotype, and the influence of environmental factors. Both factors may interact, further affecting phenotype. When two or more clearly different phenotypes exist in the same population of a species, the species is called polymorphic. A well-documented example of polymorphism is Labrador Retriever coloring; while the coat color depends on many genes, it is clearly seen in the environment as yellow, black, and brown. Richard Dawkins in 1978 and then again in his 1982 book ''The Extended Phenotype'' suggested that one can regard bird nests and other built structures such as caddis ...
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Plasmodium Berghei
''Plasmodium berghei'' is a species in the genus ''Plasmodium'' subgenus ''Vinckeia''. It is a protozoan parasite that causes malaria in certain rodents. Originally, isolated from thicket rats in Central Africa, ''P. berghei'' is one of four ''Plasmodium'' species that have been described in African murine rodents, the others being '' P. chabaudi'', '' P. vinckei'', and '' P. yoelii''. Due to its ability to infect rodents and relative ease of genetic engineering, ''P. berghei'' is a popular model organism for the study of human malaria. Biology Like all malaria parasites of mammals, including the four human malaria parasites, ''P. berghei'' is transmitted by ''Anopheles'' mosquitoes and it infects the liver after being injected into the bloodstream by a bite of an infected female mosquito. After a short period (a few days) of development and multiplication, these parasites leave the liver and invade erythrocytes (red blood cells). The multiplication of the parasite in the bloo ...
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Artemisinin
Artemisinin () and its semisynthetic derivatives are a group of drugs used in the treatment of malaria due to ''Plasmodium falciparum''. It was discovered in 1972 by Tu Youyou, who shared the 2015 Nobel Prize in Physiology or Medicine for her discovery. Artemisinin-based combination therapies (ACTs) are now standard treatment worldwide for ''P. falciparum'' malaria as well as malaria due to other species of ''Plasmodium''. Artemisinin is extracted from the plant ''Artemisia annua'', sweet wormwood, a herb employed in Chinese traditional medicine. A precursor compound can be produced using a genetically engineered yeast, which is much more efficient than using the plant. Artemisinin and its derivatives are all sesquiterpene lactones containing an unusual peroxide bridge. This endoperoxide 1,2,4-trioxane ring is responsible for their antimalarial properties. Few other natural compounds with such a peroxide bridge are known. Artemisinin and its derivatives have been used for the t ...
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Antimalarial Agents
Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria, in the latter case, most often aiming at two susceptible target groups, young children and pregnant women. As of 2018, modern treatments, including for severe malaria, continued to depend on therapies deriving historically from quinine and artesunate, both parenteral (injectable) drugs, expanding from there into the many classes of available modern drugs. Incidence and distribution of the disease ("malaria burden") is expected to remain high, globally, for many years to come; moreover, known antimalarial drugs have repeatedly been observed to elicit resistance in the malaria parasite—including for combination therapies featuring artemisinin, a drug of last resort, where resistance has now been observed in Southeast Asia. As such, the needs for new antimalarial agents and new strategies of treatment (e.g., new combin ...
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Tryptamines
Substituted tryptamines, or serotonin analogues, are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino (NH2) group via an ethyl (−CH2–CH2−) sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and DMT. In South America, dimethyltryptamine is obtained from numerous plant sources, like chacruna, and it is often used in ayahuasca brews. Many synthetic tryptamines ...
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