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Niludipine
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DB09240 |
[Niludipine is a calcium channel blocker.] |
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Moxonidine
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DB09242 |
[Moxonidine is a new-generation centrally acting antihypertensive drug approved for the treatment of mild to moderate essential hypertension. It is suggested to be effective in cases where other agents such as thiazides, beta-blockers, ACE inhibitors, and calcium channel blockers are not appropriate or irresponsive. As well, moxonidine has been shown to present blood pressure-independent beneficial effects on insulin resistance syndrome.] |
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Methylene blue
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DB09241 |
[Methylene blue is an oxidation-reduction agent. The intravenous form of methylene blue is approved by the FDA for the treatment of pediatric and adult patients with acquired methemoglobinemia. Historically, it has been widely used in Africa to treat malaria, but now it disappeared when chloroquine (CQ) and other drugs entered the market. Its use as an urinary tract antiseptic has also been investigated.
Methylthioninium chloride (INN, or methylene blue, proposed trade name Rember) is an investigational drug being developed by the University of Aberdeen and TauRx Therapeutics that has been shown in early clinical trials to be an inhibitor of Tau protein aggregation. The drug is of potential interest for the treatment of patients with Alzheimer's disease.] |
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Pirlindole
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DB09244 |
[This drug is classified as a reversible inhibitor of monoamine oxidase A enzyme (also known as a RIMA drug). It was developed and is currently used as an antidepressant in Russia. Its chemical structure is similar to metralindole, and it also shares pharmacological properties with this drug.
Pirlindole is a selective, reversible inhibitor of monoamine oxidase (MAO) subtype A (MAO-A) that is approved in several European and non-European countries for the treatment of major depression. The antidepressant efficacy and safety of pirlindole have been demonstrated in numerous studies and, supported by many years of clinical experience in the treatment of depression. Pirlindole's efficacy and safety have also been shown in the treatment of fibromyalgia.] |
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Hydracarbazine
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DB09243 |
[Hydracarbazine is a pyridazine that has found use as an antihypertensive agent [A19790] It was once marketed in France under the tradename Normatensyl.] |
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Benmoxin
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DB09246 |
[Benmoxin is an irreversible and nonselective monoamine oxidase inhibitor (MAOI) of the hydrazine class. It was first synthesized in 1967 and rapidly used in Europe as an antidepressant. However, this agent is no longer marketed.] |
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Toloxatone
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DB09245 |
[Toloxatone is an antidepressant agent, the first ever use of which was in France, 1984. It acts as a selective and reversible inhibitor of monoamine oxidase-A (MOA) [L1388].] |
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Mebanazine
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DB09248 |
[Mebanazine, also known as _Actomol_, is a monoamine oxidase inhibitor (MAOI) belonging to the _hydrazine_ class of chemicals. It was used in the past as an antidepressant in the 1960s, but has since been discontinued because of its hepatotoxic potential.] |
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Iproclozide
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DB09247 |
[Iproclozide is an irreversible and selective hydrazine class based monoamine oxidase inhibitor (MAOI). Although it was employed as an antidepressant for a time, the fact that the agent is capable of causing fulminant hepatitis and that its use has been documented as the cause for at least three reported fatalities has resulted ultimately in the agent being discontinued.] |
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Light Mineral Oil
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DB11579 |
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Hard fat
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DB11578 |
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Aluminum chlorohydrate
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DB11573 |
[Aluminum chlorohydrate is a group of water-soluble aluminum complexes with the general formula AlnCl(3n-m)(OH)m. It is included up to 25% in over-the-counter hygiene products as an active antiperspirant agent. The primary site of action of aluminum chlorohydrate is at the level of the stratum corneum layer, which is relatively near the skin surface [A27159]. It is also used as a coagulant in the water purification process.] |
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Thrombin alfa
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DB11572 |
[Thrombin Alfa is a human coagulation protein produced via recombinant DNA technology from a genetically modified CHO cell line. Thrombin Alfa is identical in amino acid sequence and structurally similar to naturally occurring human thrombin. Thrombin Alfa precursor is secreted to culture medium as single chain form that is proteolytically converted to a two-chain active form (using a protein derived from snakes) and is purified by a chromatographic process that yields a product having hemostatic activities similar to native human thrombin. The cell line used to manufacture Thrombin Alfa has been tested and shown to be free of known infectious agents. The cell culture process used in the manufacture of Thrombin Alfa employs no additives of human or animal origin. The purification process includes solvent-detergent treatment and nano-filtration steps dedicated to viral clearance. The thrombin alfa product ultimate comes from recombinant human prethrombin-1 [L2079].
Nevertheless, because the incidence of hemostasis within a timely manner is relatively comparable between the use of thrombin alfa and the placebo treatment in patient subjects, thrombin alfa is not currently approved by certain organizations like the European Medicines Agency [L2079].] |
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Human Thrombin
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DB11571 |
[Human Thrombin is a sterile solution, pH 6.8-7.2, containing highly purified human thrombin for the activation of clotting. Thrombin is a highly specific serine protease encoded by the F2 gene that transforms soluble fibrinogen into insoluble fibrin. This transformation mimics the final coagulation cascade step which involves the clotting mass that adheres to the wound surface and achieves hemostasis and sealing of open tissues.
In particular, while human thrombin products are made from pooled human source plasma, recombinant thrombin is a human coagulation protein produced via recombinant DNA technology from a genetically modified Chinese hamster ovary cell line [FDA Label]. Furthermore, human thrombin is manufactured by chromatographic purification of prothrombin from cryo-poor plasma followed by activation with calcium chloride [FDA Label].] |
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Padimate O
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DB11570 |
[Padimate O is an active sunscreen agent in cosmetics and over-the-counter sunscreen drug products in concentrations up to 8%, as regulated by the FDA [L2153]. It is a structurally-related compound to [DB02362] that absorbs UV-B rays to prevent photodamage. It penetrates human skin, and is shown to induce non-ligatable strand breaks on DNA _in vitro_ and mutagenic effects on yeast i_n vivo_ [A32458].] |
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Indigotindisulfonic acid
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DB11577 |
[Indolesulfonic acid is a blue-colored dye used a marker in urological procedures, also known as _indigo carmine_ [L2219].
Indigo carmine, or 5, _5'-indigodisulfonic acid_ sodium salt, also known as _indigotine_ or _FD& C Blue #2 _is a pH indicator with the chemical formula C16H8N2Na2O8S2. It is approved for use as a food dye in the United States and the EU and has the E number E132 [L2216]] |
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Ferric oxide
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DB11576 |
[Iron(III) oxide or ferric oxide is the inorganic compound with the formula Fe2O3. It is one of the three main oxides of iron, the other two being iron(II) oxide (FeO) the rarer form, and iron(II,III) oxide (Fe3O4) which naturally as magnetite.] |
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Grazoprevir
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DB11575 |
[Grazoprevir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as Grazoprevir. Grazoprevir is an inhibitor of NS3/4A, a serine protease enzyme, encoded by HCV genotypes 1 and 4 [synthesis]. These enzymes are essential for viral replication and serve to cleave the virally encoded polyprotein into mature proteins like NS3, NS4A, NS4B, NS5A and NS5B [FDA Label]. The barrier for develoment of resistance to NS3/4A inhibitors is lower than that of NS5B inhibitors, another class of DAAs [A19593]. Subtitutions at amino acid positions 155, 156, or 168 are known to confer resistance. The substitutions of the enzyme's catalytic triad consisting of H58, D82, and S139 are also likely to alter the affinity of the drug for NS3/4A or the activity of the enzyme itself. Despite this disadvantage Grazoprevir is still effective against HCV particularly when paired with [DB11574].
In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) recommend Grazoprevir as first line therapy in combination with [DB11574] for genotypes 1a, 1b, and 4 of Hepatitis C [A19593]. Grazoprevir and [DB11574] are used with or without [DB00811] with the intent to cure, or achieve a sustained virologic response (SVR), after 12 weeks of daily therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].
Grazoprevir is available as a fixed dose combination product with [DB11574] (tradename Zepatier) used for the treatment of chronic Hepatitis C. Approved in January 2016 by the FDA, Zepatier is indicated for the treatment of HCV genotypes 1 and 4 with or without [DB00811] depending on the the presence of resistance associated amino acid substitutions in the NS5A protein and previous treatment failure with [DB00811], [DB00008], [DB00022], or other NS3/4A inhibitors like [DB08873], [DB06290], or [DB05521] [FDA Label]. When combined together, Grazoprevir and [DB11574] as the combination product Zepatier have been shown to achieve a SVR between 94% and 97% for genotype 1 and 97% and 100% for genotype 4 after 12 weeks of treatment [L852]. It can be used in patients with compensated cirrhosis, human immunodeficiency virus co-infection, or severe kidney disease.] |
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Elbasvir
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DB11574 |
[Elbasvir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as Elbasvir. Elbasvir is an inhibitor of NS5A, a protein essential for viral replication and virion assembly [synthesis]. The barrier for develoment of resistance to NS5A inhibitors is lower than that of NS5B inhibitors, another class of DAAs [A19593]. Subtitutions at amino acid positions 28, 30, 31, or 93 are known to confer resistance to Elbasvir [FDA Label]. Despite this disadvantage Elbasvir is still effective against HCV particularly when paired with [DB11575].
In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) recommend Elbasvir as first line therapy in combination with [DB11575] for genotypes 1a, 1b, and 4 of Hepatitis C [A19593]. Elbasvir and [DB11575] are used with or without [DB00811] with the intent to cure, or achieve a sustained virologic response (SVR), after 12 weeks of daily therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].
Elbasvir is available as a fixed dose combination product with [DB11575] (tradename Zepatier) used for the treatment of chronic Hepatitis C. Approved in January 2016 by the FDA, Zepatier is indicated for the treatment of HCV genotypes 1 and 4 with or without [DB00811] depending on the the presence of resistance associated amino acid substitutions in the NS5A protein and previous treatment failure with [DB00811], [DB00008], [DB00022], or other NS3/4A inhibitors like [DB08873], [DB06290], or [DB05521] [FDA Label]. When combined together, Elbasvir and [DB11575] as the combination product Zepatier have been shown to achieve a SVR between 94% and 97% for genotype 1 and 97% and 100% for genotype 4 after 12 weeks of treatment [L852]. It can be used in patients with compensated cirrhosis, human immunodeficiency virus co-infection, or severe kidney disease.] |
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Phenoxypropazine
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DB09251 |
[Phenoxypropazine is a non-selective and irreversible monoamine oxidase enzyme inhibitor (MAOI), belonging to the _hydrazine_ chemical class. It was marketed as an antidepressant in 1961 but was later withdrawn in 1966 because of its hepatotoxic potential.] |