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Polyethylene glycol
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DB09287 |
[Polyethylene glycol is a polyether compound used for many purposes ranging from industrial manufacturing processes to medicine. PEG is the basis of a number of laxatives (e.g., macrogol-containing products, such as Movicol and polyethylene glycol 3350, or SoftLax, MiraLAX,ClearLAX, Osmolax or GlycoLax). Irrigation of the bowel with polyethylene glycol and electrolytes is included in bowel preparation therapy, normally indicated before a colonoscopy to ensure adequate visualization of the bowel. Therapeutic classification is as an Osmotic Laxative that works by drawing water into the lumen of the intestinal tract. Shown to decrease consistency and increase weight of stool in constipated patients at low doses.] |
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Tianeptine
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DB09289 |
[Tianeptine is a drug used primarily in the treatment of major depressive disorder and has been studied in the treatment of irritable bowel syndrome (IBS) [A31983]. Structurally, it is classified as a tricyclic antidepressant (TCA), however, it possesses different pharmacological properties than typical tricyclic antidepressants [A31969].
Tianeptine was discovered and patented by The French Society of Medical Research in the 1960s [L2946]. Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in several other European countries under the trade name “Coaxil” as well as in Asia (including Singapore) and Latin America as “Stablon” and “Tatinol” but it is not available in Australia, Canada, New Zealand, the U.K. or the U.S.] |
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Streptococcus pneumoniae type 4 capsular polysaccharide diphtheria crm197 protein conjugate antigen
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DB10286 |
[Streptococcus pneumoniae type 4 capsular polysaccharide diphtheria crm197 protein conjugate antigen is a sterile vaccine that contains saccharides of the capsular antigens of *Streptococcus pneumoniae* serotype 4 individually conjugated to the CRM197 protein, a nontoxic variant of diphtheria toxin isolated from cultures of *Corynebacterium diphtheriae* strain C7 (β197) . It is contained in the vaccine under the market name Prevnar that contains the saccharides for serotypes 4, 6B, 9V, 14, 18C, 19F, and 23F for intramuscular injection. The saccharides in the vaccine are prepared from purified polysaccharides that are chemically activated then conjugated to the protein carrier CRM197 to form the glycoconjugate.] |
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Neisseria meningitidis serogroup B recombinant LP2086 B01 protein variant antigen
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DB10285 |
[Neisseria meningitidis serogroup b recombinant lp2086 b01 protein variant antigen is a sterile vaccine for intramuscular injection indicated for the active immunization to prevent invasive disease caused by *Neisseria meningitidis* serogroup B. It is contained in the suspension of Trumenba, which is a vaccine is composed of two recombinant lipidated factor H binding protein (fHBP) variants from N. meningitidis serogroup B, one from fHBP subfamily A and one from subfamily B (A05 and B01, respectively).] |
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Neisseria meningitidis serogroup B recombinant LP2086 A05 protein variant antigen
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DB10284 |
[Neisseria meningitidis serogroup B recombinant lp2086 a05 protein variant antigen is a sterile vaccine for intramuscular injection indicated for the active immunization to prevent invasive disease caused by *Neisseria meningitidis* serogroup B. It is contained in the suspension of Trumenba, which is a vaccine is composed of two recombinant lipidated factor H binding protein (fHBP) variants from N. meningitidis serogroup B, one from fHBP subfamily A and one from subfamily B (A05 and B01, respectively).] |
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Rabies virus inactivated antigen, A
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DB10283 |
[Rabies virus inactivated antigen, A is an inactivated virus vacine for the intramuscular injection. It is an active immunization against rabies that can be administered pre- or post-exposure to the rabies virus.] |
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Streptococcus pneumoniae type 14 capsular polysaccharide diphtheria crm197 protein conjugate antigen
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DB10289 |
[Streptococcus pneumoniae type 14 capsular polysaccharide diphtheria crm197 protein conjugate antigen is a sterile vaccine that contains saccharides of the capsular antigens of *Streptococcus pneumoniae* serotype 14 individually conjugated to the CRM197 protein, a nontoxic variant of diphtheria toxin isolated from cultures of *Corynebacterium diphtheriae* strain C7 (β197) . It is contained in the vaccine under the market name Prevnar that contains the saccharides for serotypes 4, 6B, 9V, 14, 18C, 19F, and 23F for intramuscular injection. The saccharides in the vaccine are prepared from purified polysaccharides that are chemically activated then conjugated to the protein carrier CRM197 to form the glycoconjugate.] |
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Streptococcus pneumoniae type 9v capsular polysaccharide diphtheria crm197 protein conjugate antigen
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DB10288 |
[Streptococcus pneumoniae type 9v capsular polysaccharide diphtheria crm197 protein conjugate antigen is a sterile vaccine that contains saccharides of the capsular antigens of *Streptococcus pneumoniae* serotype 9v individually conjugated to the CRM197 protein, a nontoxic variant of diphtheria toxin isolated from cultures of *Corynebacterium diphtheriae* strain C7 (β197) . It is contained in the vaccine under the market name Prevnar that contains the saccharides for serotypes 4, 6B, 9V, 14, 18C, 19F, and 23F for intramuscular injection. The saccharides in the vaccine are prepared from purified polysaccharides that are chemically activated then conjugated to the protein carrier CRM197 to form the glycoconjugate.] |
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Streptococcus pneumoniae type 6b capsular polysaccharide diphtheria crm197 protein conjugate antigen
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DB10287 |
[Streptococcus pneumoniae type 6b capsular polysaccharide diphtheria crm197 protein conjugate antigen is a sterile vaccine that contains saccharides of the capsular antigens of *Streptococcus pneumoniae* serotype 6b individually conjugated to the CRM197 protein, a nontoxic variant of diphtheria toxin isolated from cultures of *Corynebacterium diphtheriae* strain C7 (β197) . It is contained in the vaccine under the market name Prevnar that contains the saccharides for serotypes 4, 6B, 9V, 14, 18C, 19F, and 23F for intramuscular injection. The saccharides in the vaccine are prepared from purified polysaccharides that are chemically activated then conjugated to the protein carrier CRM197 to form the glycoconjugate.] |
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Rolapitant
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DB09291 |
[Rolapitant is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist approved for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Delayed-phase CINV typically occurs >24 hours after chemotherapy treatment and is principally mediated by Neurokinin-1 and its ligand Substance P, which is released in the gut following chemotherapy administration. Neurokinin-1 is also known as Tachykinin Receptor 1 (TACR1), Neurokinin 1 Receptor (NK1R), and Substance P Receptor (SPR).
By blocking Substance P from interacting with NK-1 receptors in the gut and the central nervous system, rolapitant prevents late-phase CINV. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long elimination half-life, allowing a single dose to prevent both acute and late-phase CINV during the first 120 hours post-chemotherapy.] |
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Ramosetron
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DB09290 |
[Ramosetron is a _serotonin 5-HT3 receptor antagonist_ commonly employed to treat nausea and vomiting, in addition to certain diarrheal conditions. It is believed to have higher potency and longer antiemetic action than other 1st generation 5-HT3 antagonists such as ondansetron. Currently, ramosetron is only approved for use Japan and in certain Southeast Asian countries.] |
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Iodide I-131
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DB09293 |
[Iodide I-131 (as Sodium iodide I-131) is a radioisotopic drug used for the treatment and palliation of thyroid malignancy. Iodine-131 is notable for causing mutation and death in cells that it penetrates, which is due to its mode of beta decay. As a result of beta decay, approximately 10% of its energy and radiation dose is via gamma radiation, while the other 90% (beta radiation) causes tissue damage without contributing to any ability to see or image the isotope. Low levels of beta radiation are also known for causing cancer as this dose is highly mutagenic. For this reason, less toxic iodine isotopes such as I-123 are more frequently used in nuclear imaging, while I-131 is reserved for its tissue destroying effects. Because the thyroid gland naturally takes up iodine from the body, therapeutic methods using radioisotopes can take advantage of this mechanism for localization of drug to the site of malignancy.
Therapeutic solutions of Sodium Iodide-131 are indicated for the treatment of hyperthyroidism and thyroid carcinomas that take up iodine. Palliative effects may be observed in patients with advanced thyroid malignancy if the metastatic lesions take up iodine. It is also indicated for use in performance of the radioactive iodide (RAI) uptake test to evaluate thyroid function.] |
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Sacubitril
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DB09292 |
[Sacubitril is a prodrug neprilysin inhibitor used in combination with valsartan to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It was approved by the FDA after being given the status of priority review for on July 7, 2015.
Sacubitril's active metabolite, LBQ657 inhibits neprilysin, a neutral endopeptidase that would typically cleave natiuretic peptides such as atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP). ANP and BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis. Under normal conditions, neprilysin breaks down other vasodilating peptides and also vasoconstrictors such as angiotensin I and II, endothelin-1 and peptide amyloid beta-protein. Inhibition of neprilysin therefore leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II.] |
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Talniflumate
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DB09295 |
[Talniflumate, is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma [L1400]. In addition, it is used in inflammatory conditions such as rheumatoid arthritis. Phase I trials with talniflumate for the treatment of cystic fibrosis and COPD were completed in August 2001, and phase II trials were performed in Ireland for the treatment of cystic fibrosis but this research has now been discontinued [L1402, L1405]. Talniflumate has been approved for approximately 20 years in Argentina other countries (excluding the United States, Europe, and Japan) [L1405].] |
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Paritaprevir
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DB09297 |
[Paritaprevir 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 paritaprevir. As a newer generation and directly acting HCV antiviral, paritaprevir products have better Sustained Virological Response (SVR) rates, higher barriers to resistance, fewer side effects, and a reduced pill burden compared to older agents such as [DB08873], [DB05521], [DB00008], [DB00022], and [DB00811]. By combining multiple antiretroviral medications into fixed dose products, the viral lifecycle can be targeted at multiple stages while simultaneously reducing the risk of developing resistant viral strains [A19593]. Within Canada and the United States, paritaprevir is currently available in three fixed dose products: Viekira Pak (FDA), Technivie (FDA and Health Canada), and Holkira Pak (Health Canada).
More specifically, paritaprevir prevents viral replication by inhibiting the NS3/4A serine protease of Hepatitis C Virus (HCV) [FDA Label]. Following viral replication of HCV genetic material and translation into a single polypeptide, Nonstructural Protein 3 (NS3) and its activating cofactor Nonstructural Protein 4A (NS4A) are responsible for cleaving genetic material into the following structural and nonstructural proteins required for assembly into mature virus: NS3, NS4A, NS4B, NS5A, and NS5B [A19643]. By inhibiting viral protease NS3/4A, paritaprevir therefore prevents viral replication and function.
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 Paritaprevir as a first line therapy option when used in combination with other antivirals for genotypes 1a, 1b, and 4[L852]. Depending on the genotype, Paritaprevir is often used in combination with other antivirals such as [DB09296], [DB09183], [DB00503], and [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]. Treatment with direct acting antivirals such as paritaprevir is associated with very minimal side effects, with the most common being headache and fatigue [FDA Label]. Lack of significant side effects and short duration of therapy is a considerable advantage over older interferon-based regimens, which were limited by infusion site reactions, reduced blood count, and neuropsychiatric effects [A19635].
Paritaprevir first came on the market as a fixed-dose combination product with [DB09296], [DB09183], and [DB00503] as the FDA-approved product Viekira Pak. First approved in December 2014, Viekira Pak is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis.
Paritaprevir is also available as a fixed-dose combination product with [DB09296] and [DB00503] as the FDA- and Health Canada-approved product Technivie. First approved in July 2015, Technivie is indicated in combination with [DB00811] for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis or with compensated cirrhosis.
In Canada, paritaprevir is also available as a fixed-dose combination product with [DB09296], [DB09183], and [DB00503] as the Health Canada-approved, commercially available product Holkira Pak. First approved in January 2015, Holkira Pak is indicated for the treatment of HCV genotype 1b with or without cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a with or without cirrhosis.] |
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Ombitasvir
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DB09296 |
[Ombitasvir 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 Ombitasvir. Ombitasvir is an inhibitor of NS5A, a protein essential for viral replication and virion assembly [FDA Label]. The barrier for develoment of resistance to NS5A inhibitors is lower than that of NS5B inhibitors, another class of DAAs [A19593].
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 Ombitasvir as a first line therapy option when used in combination with other antivirals for genotypes 1a, 1b, and 4 [L852]. Depending on the genotype, Ombitasvir is often used in combination with other antivirals such as [DB09183], [DB09297], [DB00503], and [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]. Treatment with direct acting antivirals such as Ombitasvir is associated with very minimal side effects, with the most common being headache and fatigue [FDA Label]. Lack of significant side effects and short duration of therapy is a considerable advantage over older interferon-based regimens, which were limited by infusion site reactions, reduced blood count, and neuropsychiatric effects [A19635].
Ombutasvir first came on the market as a fixed-dose combination product with [DB09183], [DB09297], and [DB00503] as the FDA-approved product Viekira Pak. First approved in December 2014, Viekira Pak is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with Ribavirin for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis.
Ombutasvir is also available as a fixed-dose combination product with [DB09297] and [DB00503] as the FDA- and Health Canada-approved product Technivie. First approved in July 2015, Technivie is indicated in combination with Ribavirin for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis or with compensated cirrhosis.
In Canada, Ombutasvir is also available as a fixed-dose combination product with [DB09183], [DB09297], and [DB00503] as the Health Canada-approved, commercially available product Holkira Pak. First approved in January 2015, Holkira Pak is indicated for the treatment of HCV genotype 1b with or without cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a with or without cirrhosis.] |
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Tenofovir alafenamide
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DB09299 |
[Tenofovir alafenamide is a novel [tenofovir] prodrug developed in order to improve renal safety when compared to the counterpart [tenofovir disoproxil].[A178060] Both of these prodrugs were first created to cover the polar phosphonic acid group on tenofovir by using a novel oxycarbonyloxymethyl linkers to improve the oral bioavailability and intestinal diffusion.[T239] Tenofovir alafenamide is an alanine ester form characterized for presenting low systemic levels but high intracellular concentration.[A178219] It has been reported to produce a large antiviral efficacy at doses ten times lower than tenofovir disoproxil.[A178327] Tenofovir alafenamide is indicated to treat chronic hepatitis B,[L6241] treat HIV-1,[L4388,L6277,L6280,L6283] and prevent HIV-1 infections.[L4388,L9010]
Tenofovir alafenamide was developed by Gilead Sciences Inc and granted FDA approval on 5 November 2015.[L6271]] |
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Silibinin
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DB09298 |
[Silibinin is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin is presented as a mixture of two diastereomers, silybin A and silybin B, which are found in an approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.] |
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Neon
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DB11589 |
[Neon is a chemical element with a chemical symbol Ne and atomic number 10. It is a noble gas that is colorless, odorless, inert and monatomic. It is the fifth most abundant chemical element in the universe by mass but a rare element on Earth. It displays a reddish-orange light, and is commonly used in low-voltage neon glow lamps, high-voltage discharge tubes, and signs with fluorescent lighting. It is also used in vacuum tubes, high-voltage indicators, lightning arresters, wave meter tubes, television tubes, and helium–neon lasers. Neon may be used in the clinical setting as a diagnostic tracer gas in a gas analyzer for a lung diffusion test. Other clinical applications of neon, such as a radiotherapy in various cancers [A32763], have been studied.] |
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Pipradrol
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DB11584 |
[Pipradrol (Meratran) [L2523] was initially developed in the 1950s as an antidepressant, however, the adverse effects associated with its use and its abuse potential led to its withdrawal and international regulation [L2524]. Pipradrol was made illegal in many countries in 1970s because of its potential for abuse. It is currently classified under the Misuse of Drugs Act as a Class C substance [L2522].
Experimentation with the drug and its derivatives for recreational purposes has led to many cases of acute toxicity and has been linked to three fatalities. The social and in particular acute clinical harms of pipradrol derivatives have led to their control under the Misuse of Drugs Act 1971 in the UK in 2012 [T178].
Interestingly, this drug has been studied for bactericidal properties, however, is not currently, used for this purpose [A32725]. In addition to this, it has shown favorable effects in postpartum depressive symptoms [L2516].] |