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Tedizolid
Tedizolid (formerly torezolid, trade name Sivextro), is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals), and is marketed for the treatment of acute bacterial skin and skin structure infections (also known as complicated skin and skin-structure infections (cSSSIs)). The most common side effects include nausea (feeling sick), headache, diarrhoea and vomiting. These side effects were generally of mild or moderate severity. Tedizolid was approved for medical use in the United States in June 2014, and for medical use in the European Union in March 2015. Medical uses Tedizolid was approved by the U.S Food and Drug Administration (FDA) on June 20, 2014, with the indication for the treatment of acute bacterial Skin and skin structure infections (ABSSSI) caused by certain susceptible bacteria ...
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Tedizolid Phosphate
Tedizolid (formerly torezolid, trade name Sivextro), is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals), and is marketed for the treatment of acute bacterial skin and skin structure infections (also known as complicated skin and skin-structure infections (cSSSIs)). The most common side effects include nausea (feeling sick), headache, diarrhoea and vomiting. These side effects were generally of mild or moderate severity. Tedizolid was approved for medical use in the United States in June 2014, and for medical use in the European Union in March 2015. Medical uses Tedizolid was approved by the U.S Food and Drug Administration (FDA) on June 20, 2014, with the indication for the treatment of acute bacterial Skin and skin structure infections (ABSSSI) caused by certain susceptible bacteri ...
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Trius Therapeutics
Trius Therapeutics () was a biopharma company based in San Diego, CA that focused on the development of antibiotics. Business profile The lead compound from Trius, tedizolid phosphate (formerly torezolid phosphate, TR-701), successfully completed its first Phase 3 clinical trial (ESTABLISH 1) in acute skin and skin structure infections (ABSSSI). It is a once daily, IV and oral, oxazolidinone being developed for the treatment of serious gram-positive infections, including those caused by methicillin-resistant ''Staphylococcus aureus'' (MRSA). The Phase 3 trials are being conducted under a Special Protocol Agreement with the US Food and Drug Administration and are using the draft FDA guidance of cessations of lesion spread at 48–72 hours as the primary endpoint. In the ESTABLISH 1 Study, 200 mg of Tedizolid given for a short course of therapy (six days) was shown to be safe, well tolerated and was as effective as the traditional length of therapy with linezolid (600 mg fo ...
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Linezolid
Linezolid is an antibiotic used for the treatment of infections caused by Gram-positive bacteria that are resistant to other antibiotics. Linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant ''Staphylococcus aureus'' (MRSA). The main uses are infections of the skin and pneumonia although it may be used for a variety of other infections including drug-resistant tuberculosis. It is used either by injection into a vein or by mouth. When given for short periods, linezolid is a relatively safe antibiotic. It can be used in people of all ages and in people with liver disease or poor kidney function. Common side effects with short-term use include headache, diarrhea, rash, and nausea. Serious side effects may include serotonin syndrome, bone marrow suppression, and high blood lactate levels, particularly when used for more than two weeks. If used for longer periods it ...
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Oxazolidinone
2-Oxazolidone is a heterocyclic organic compound containing both nitrogen and oxygen in a 5-membered ring. Oxazolidinones Evans auxiliaries Oxazolidinones are a class of compounds containing 2-oxazolidone in the structure. In chemistry, they are useful as Evans auxiliaries, which are used for chiral synthesis. Usually, the acid chloride substrate reacts with the oxazolidinone to form an imide. Substituents at the 4 and 5 position of the oxazolidinone direct any aldol reaction to the alpha position of the carbonyl of the substrate. Pharmaceuticals Oxazolidinones are mainly used as antimicrobials. The antibacterial effect of oxazolidinones is by working as protein synthesis inhibitors, targeting an early step involving the binding of N-formylmethionyl-tRNA to the ribosome. (See Linezolid#Pharmacodynamics) Some of the most important oxazolidinones are antibiotics. Examples of antibiotic oxazolidinones include: *Linezolid (Zyvox), which is available for intravenous administratio ...
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Cubist Pharmaceuticals
Cubist Pharmaceuticals was an American biopharmaceutical company that targeted pathogens like MRSA. . The company employed 638 people, mostly in Lexington, MA. On 8 December 2014, Merck & Co. acquired Cubist for $102 per share in cash ($8.4 billion). History Cubist was founded in May 1992 by John K. Clarke, Paul R. Schimmel, Ph.D. and Barry M. Bloom, Ph.D, all of whom were also directors. Cubist appeared on Fortune 2010’s List of fastest growing companies, and was named to the 2010 Deloitte Technology Fast 500. In 2011, the company acquired Adolor, maker of a drug for treatment of constipation. The company expected sales of its drug Cubicin to grow to more than 1 billion dollars per year. In July 2013, Cubist Pharmaceuticals agreed to purchase Trius Therapeutics and Optimer Pharmaceuticals for around $1.6 billion. In 2014, succeeding Michael Bonney as President, Robert J. Perez, was announced to take leadership on January 1, 2015. In January 2015 Cubist Pharmaceutic ...
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Oxazolidinone Antibiotics
2-Oxazolidone is a heterocyclic organic compound containing both nitrogen and oxygen in a 5-membered ring. Oxazolidinones Evans auxiliaries Oxazolidinones are a class of compounds containing 2-oxazolidone in the structure. In chemistry, they are useful as Evans auxiliaries, which are used for chiral synthesis. Usually, the acid chloride substrate reacts with the oxazolidinone to form an imide. Substituents at the 4 and 5 position of the oxazolidinone direct any aldol reaction to the alpha position of the carbonyl of the substrate. Pharmaceuticals Oxazolidinones are mainly used as antimicrobials. The antibacterial effect of oxazolidinones is by working as protein synthesis inhibitors, targeting an early step involving the binding of N-formylmethionyl-tRNA to the ribosome. (See Linezolid#Pharmacodynamics) Some of the most important oxazolidinones are antibiotics. Examples of antibiotic oxazolidinones include: *Linezolid (Zyvox), which is available for intravenous administratio ...
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Complicated Skin And Skin-structure Infections
Skin and skin structure infections (SSSIs), also referred to as skin and soft tissue infections (SSTIs), or acute bacterial skin and skin structure infections (ABSSSIs), are infections of skin and associated soft tissues (such as loose connective tissue and mucous membranes). Historically, the pathogen involved has most frequently been a bacterial species—always, since redescription of SSSIs as ABSSSIs—and as such, these infections require treatment by antibiotics. Types Until 2008, a distinction was made between two types: complicated SSSIs (cSSSIs) and uncomplicated SSSIs (uSSSIs), which had different regulatory approval requirements. Uncomplicated SSSIs included "simple abscesses, impetiginous lesions, furuncles, and cellulitis." Complicated SSSIs included "infections either involving deeper soft tissue or requiring significant surgical intervention, such as infected ulcers, burns, and major abscesses or a significant underlying disease state that complicates the response to ...
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Skin And Skin Structure Infection
Skin and skin structure infections (SSSIs), also referred to as skin and soft tissue infections (SSTIs), or acute bacterial skin and skin structure infections (ABSSSIs), are infections of skin and associated soft tissues (such as loose connective tissue and mucous membranes). Historically, the pathogen involved has most frequently been a bacterial species—always, since redescription of SSSIs as ABSSSIs—and as such, these infections require treatment by antibiotics. Types Until 2008, a distinction was made between two types: complicated SSSIs (cSSSIs) and uncomplicated SSSIs (uSSSIs), which had different regulatory approval requirements. Uncomplicated SSSIs included "simple abscesses, impetiginous lesions, furuncles, and cellulitis." Complicated SSSIs included "infections either involving deeper soft tissue or requiring significant surgical intervention, such as infected ulcers, burns, and major abscesses or a significant underlying disease state that complicates the response to ...
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Enterococcus Faecalis
''Enterococcus faecalis'' – formerly classified as part of the group D ''Streptococcus'' system – is a Gram-positive, commensal bacterium inhabiting the gastrointestinal tracts of humans. Like other species in the genus ''Enterococcus'', ''E. faecalis'' is found in healthy humans and can be used as a probiotic. The probiotic strains such as Symbioflor1 and EF-2001 are characterized by the lack of specific genes related to drug resistance and pathogenesis. As an opportunistic pathogen, ''E. faecalis'' can cause life-threatening infections, especially in the nosocomial (hospital) environment, where the naturally high levels of antibiotic resistance found in ''E. faecalis'' contribute to its pathogenicity. ''E. faecalis'' has been frequently found in reinfected, root canal-treated teeth in prevalence values ranging from 30% to 90% of the cases. Re-infected root canal-treated teeth are about nine times more likely to harbor ''E. faecalis'' than cases of primary infections. Physi ...
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Pyridines
Pyridine is a basic heterocyclic organic compound with the chemical formula . It is structurally related to benzene, with one methine group replaced by a nitrogen atom. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell. Pyridine is colorless, but older or impure samples can appear yellow, due to the formation of extended, unsaturated polymeric chains, which show significant electrical conductivity. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Historically, pyridine was produced from coal tar. As of 2016, it is synthesized on the scale of about 20,000 tons per year worldwide. Properties Physical properties The molecular electric dipole moment is 2.2 debyes. Pyridine is diamagnetic and has a diamagnetic susceptibility of −48.7 × 10−6 cm3·mol−1. The standard enthalpy of formation is 100.2 kJ·mol−1 in the liquid phase ...
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Tetrazoles
Tetrazoles are a class of synthetic organic heterocyclic compound, consisting of a 5-member ring of four nitrogen atoms and one carbon atom. The name tetrazole also refers to the parent compound with formula CH2N4, of which three isomers can be formulated. Structure and bonding Three isomers of the parent tetrazole exist, differing in the position of the double bonds: 1''H''-, 2''H''-, and 5''H''-tetrazole. The 1''H''- and 2''H''- isomers are tautomers, with the equilibrium lying on the side of 1''H''-tetrazole in the solid phase. In the gas phase, 2''H''-tetrazole dominates. These isomers can be regarded as aromatic, with 6 π-electrons, while the 5''H''-isomer is nonaromatic. Synthesis 1''H''-Tetrazole was first prepared by the reaction of anhydrous hydrazoic acid and hydrogen cyanide under pressure. Treatment of organic nitriles with sodium azide in the presence of iodine or silica-supported sodium bisulfate as a heterogeneous catalyst enables an advantageous synthesis ...
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Optic Neuropathy
Optic neuropathy is damage to the optic nerve from any cause. The optic nerve is a bundle of millions of fibers in the retina that sends visual signals to the brain. Damage and death of these nerve cells, or neurons, leads to characteristic features of optic neuropathy. The main symptom is loss of vision, with colors appearing subtly washed out in the affected eye. A pale disc is characteristic of long-standing optic neuropathy. In many cases, only one eye is affected and patients may not be aware of the loss of color vision until the doctor asks them to cover the healthy eye. Optic neuropathy is often called optic atrophy, to describe the loss of some or most of the fibers of the optic nerve. Ischemic optic neuropathy In ischemic optic neuropathies, there is insufficient blood flow (ischemia) to the optic nerve. The anterior optic nerve is supplied by the short posterior ciliary artery and choroidal circulation, while the retrobulbar optic nerve is supplied intraorbitally by ...
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