Tedizolid phosphate is a nextgeneration oxazolidinone with activity against both methicillinresistant staphylococcus aureus and vancomycinresistant enterococcus spp. T1653 tedizolid phosphate references choi s, im w, bartizal k. Tedizolid phosphate pharmacokinetics absorption bioavailability. Tedizolid phosphate is a novel oxazolidinone prodrug whose active moiety, tedizolid, has improved potency against grampositive pathogens and pharmacokinetics, allowing oncedaily administration.
Tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, its microbiologically active form. The primary safety data base is the phase 3 clincal studies in which 662 su bjects received 200 mg tedizolid phosphate. Tedizolid was found to be a weak, reversible inhibitor of maoa and maob activity with only minimal effects observed with the prodrug, tedizolid phosphate. As a result, tedizolid inhibits bacterial translation and protein synthesis. The rmp details important risks of tedizolid phosphate, how these risks can be minimised, and how more information will be obtained about tedizolid phosphate. Activity of tedizolid phosphate tr701 in murine models of infection with penicillinresistant and penicillinsensitive streptococcus pneumoniae. Tedizolid has consistently shown potency advantages over linezolid against grampositive microorganisms including those with reduced susceptibility to linezolid.
For mice infected with pssp type iii, the 100% survival rate is achieved with tedizolid phosphate tr701fa at a minimum total daily dose of 10 mgkg. Tedizolid is administered once daily and available in both intravenous and oral formulations. To determine whether the expected dose of tedizolid phosphate can be delivered via nasogastric tube in patients who have difficulty swallowing and in whom venous access is not suitable, this in vitro study evaluated the recovery of tedizolid phosphate. Sivextro 200 mg filmcoated tablets summary of product. Additionally, tedizolid was studied in 30 human subjects concomitantly given tyramine to test the dose needed to increase blood pressure by 30 mmhg compared to placebo. Tedizolid has phosphate added to the aring which increases its water solubility. Highlights of prescribing information these highlights do not include all the information needed to use sivextro safely and effectively. Tedizolid phosphate is approved for the treatment of acute bacterial skin and skin structure infections. Pdf intracellular activity of tedizolid phosphate and. Mao inhibition causes levels of the neurotransmitter serotonin to increase. No warranty, express or implied, is made and labchem inc. Tedizolid phosphate is a novel antibacterial prodrug with potent activity against grampositive pathogens. Tedizolid phosphate reference guide for safe and effective use from the american.
Stability of crushed tedizolid phosphate tablets for. M for monoamine oxidase maoa and maob, respectively. Material safety data sheet of tedizolid phosphate abmole. Tedizolid phosphate is a white to yellow solid and is administered orally or by intravenous infusion. The intra and interassay precision relative standard deviations sds were 3. Pdf tedizolid phosphate for the treatment of acute bacterial skin. Intracellular activity of tedizolid phosphate and ach702 versus. Tedizolid phosphate is a prodrug form of tedizolid, an antibiotic with activity against grampositive bacteria.
In murine models of penicillinresistant streptococcus pneumoniae infection, tedizolid was as effective as or more effective than linezolid and showed less inflammatory cell invasion into alveolar spaces. Tedizolid phosphate has one asymmetric center, leading to two possible enantiomers. Tedizolid is a secondgeneration oxazolidinone found to be effective against grampositive pathogens. Tedizolid phosphate, also know as tr701fa tedizolid, torezolid trade name sivextro, is an oxazolidinone drug being developed by cubist pharmaceuticals following acquisition of trius. Tedizolid tr700, formerly torezolid is the active moiety of the prodrug tedizolid phosphate tr701, a nextgeneration oxazolidinone, with high potency against grampositive species, including methicillinresistant staphylococcus aureus mrsa 2. The findings indicated that after intravenous or oral administration of tedizolid phosphate 200 mg once daily, no dose. The primary safety data base is the phase 3 clincal studies in which 662 su bjects received 200 mg tedizolid phosphate orally and or. Tedizolid plasma exposure was similar in elderly and younger control subjects.
Comparative pharmacodynamics of the new oxazolidinone tedizolid phosphate and linezolid in a neutropenic murine staphylococcus aureus pneumonia model alexander j. Linezolid is a reversible, nonselective monamine oxidase inhibitor maoi. Reconstitute vial containing 200 mg of tedizolid phosphate by adding 4 ml of. In vitro and in vivo studies demonstrated that the prodrug is rapidly converted by nonspecific phosphatases to the biologically active moiety tedizolid. Methods and material for containment and cleaning up methods for cleaning up wear protective clothing as described in section 8 of this safety data sheet. Tedizolid phosphate, also know as tr701fa tedizolid, torezolid trade name sivextro, is an oxazolidinone drug being developed by cubist pharmaceuticals following acquisition of trius therapeutics originator. Tedizolid phosphate is a novel antibacterial under. See the end of this patient information for a complete list of ingredients in sivextro. There are no other significant circulating metabolites beyond tedizolid which accounts for. Parchem is open and ready to supply materials 18002823982 read more. Tedizolid phosphate is an oxazolidinoneclass antibiotic prodrug indicated in adults for the treatment of acute. The pharmacologically active moiety, tedizolid, is an antibacterial agent of the oxazolidinone class sivextro tablets contain 200 mg of tedizolid phosphate.
Sep 10, 2019 tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, the microbiologically active moiety, following oral and intravenous administration. Tedizolid phosphate sivextro is recommended as an option for restricted use within nhs wales for the treatment of adult patients with acute bacterial and skin structure infections absssi caused by grampositive staphylococcus aureus specifically methicillinresistant mrsa isolates as an alternative oxazolidinione antibacterial. Feb 24, 2015 tedizolid was found to be a weak, reversible inhibitor of maoa and maob activity with only minimal effects observed with the prodrug, tedizolid phosphate. Pharmacokinetics, safety, and tolerability of tedizolid. September 17, 2010 information in this msds is from available published sources and is believed to be accurate. The applicant requested t he active substance tedizolid phosphate contained in the above medicinal product to be considered as a new active substance in itself, as the applicant claims that it is not a. First aid measures description of first aid measures.
Review the establish 1 and establish 2 trial design for more information about sivextro in clinical trials. Introduction outcomes data for patients who received tedizolid for acute bacterial skin and. Phosphate buffer safety data sheet supersedes revision. Identification of the substancemixture and of the companyundertaking product name. Hold eyelids apart and flush eyes with plenty of water for at least 15 minutes. Besides that, tedizolid was found to be the inhibitors of human monoamine oxidase with ic50 values of 8.
Tedizolid phosphate is an oxazolidinone approved for the treatment of acute bacterial skin and skinstructure infections. Development history and fda approval process for sivextro. When treated in vivo, tedizolid was the active moiety converted from the prodrug tedizolid phosphate. The information given is designed only as a guidance for safe handling, use, processing, storage, transportation, disposal and release and is not to be considered a warranty or quality specification. Tedizolid phosphate is a prodrug, which is converted to tedizolid in the presence of phosphatases. Tedizolid phosphate is intended for both oral and intravenous iv administration in the treatment of acute bacterial skin and skin structure. Tedizolid phosphate c17h16fn6o6p cid 11476460 structure, chemical names, physical and. Absorption, distribution, metabolism, and excretion of the. Sivextro tedizolid phosphate is an oxazolidinone antibiotic drug indicated for the treatment of acute bacterial skin and skin structure infections absssi. In a clinical study comparing the single dose 10 mg pharmacokinetics of rosuvastatin breast cancer resistant protein bcrp substrate alone or in combination with tedizolid phosphate oncedaily 200 mg oral dose, rosuvastatin auc and c max increased by approximately 70% and 55%, respectively, when coadministered with tedizolid phosphate. Sivextro tedizolid dosing, indications, interactions.
Retrospective realworld evaluation of outcomes in patients with. In june 2014, the fda approved tedizolid phosphate sivextro, cubist pharmaceuticals as a secondgeneration oxazolidinone with potentially four to 16fold potency against mrsa when compared with. Profile of tedizolid phosphate and its potential in the treatment of acute bacterial skin and skin structure infections ronald g hall 2nd, heidi n michaels texas tech university health sciences center, dallas, tx, usa abstract. The active moiety, tedizolid, is an oxazolidinone antibacterial agent which binds to the 50s subunit of the bacterial ribosome thereby inhibiting bacterial protein synthesis. Tedizolid phosphate trius therapeutic inc, san diego california formerly. Single oral dose radiolabeled 14ctedizolid phosphate kinetic studies in human subjects 100 ci in 204 mg tedizolid phosphate free.
It is the first oxazolidinone to be approved since linezolid in 2000. Tedizolid and linezolid are both oxazolidinones with similar chemical structures. Only the pharmacokinetic profile of tedizolid is discussed further due to negligible systemic exposure of tedizolid phosphate following oral and intravenous administration. The safety of tedizolid phosphate has been evaluated in a total of 1,485 subjects receiving at least one dose of tedizolid phosphate administered either orally or intravenously. Single and multipledose pharmacokinetics and absolute. Linezolid and tedizolid infectious diseases merck manuals. Open access full text article profile of tedizolid. Listing a study does not mean it has been evaluated by the u. In june 2014, the fda approved tedizolid phosphate sivextro, cubist pharmaceuticals as a secondgeneration oxazolidinone with potentially four to 16fold potency against mrsa when compared with linezolid.
Activity of tedizolid phosphate tr701 in murine models of. Donga pharmaceuticals for complicated skin and skinstructure infections csssis, including those caused by methicillinresistant staphylococcus aureus mrsa. Tedizolid phosphate is the first oncedaily oxazolidinone approved by the united states food and drug administration for the treatment of acute bacterial skin and skin. Apexbio tedizolid hcloxazolidinone for grampositive.
Tedizolid phosphate, tedizolid phosphate supplier, tedizolid phosphate distributor, cas 856867555, tedizolid phosphate manufacturer, tedizolid phosphate wholesale skip to main content covid19 status. The above information is believed to be correct but does not purport to be all. It is also unlikely to be metabolized by cyp450 enzymes in the liver. Tedizolid phosphate is a oxazolidinone prodrug that is cleaved rapidly by body phosphatases into the active moiety, tedizolid. Summary of risk management plan for tedizolid phosphate this is a summary of the risk management plan rmp for tedizolid phosphate. Hold eyelids apart and flush eyes with plenty of water for. Material safety data sheet of tedizolid phosphate contains identification of substance and details of the supplier of the safety data sheet. There is limited experience with tedizolid phosphate in the treatment of patients with concomitant acute bacterial skin and skin structure infections and secondary. Enantioseparation of tedizolid phosphate by rphplc, using. Tedizolid phosphate is the second commercially available oxazolidinone antibiotic and is the prodrug form of tedizolid with a fixed oncedaily dose. Profile of tedizolid phosphate and its potential in the.
The sponsor explained that even if study 112 datasets were written in sds version 1. Evidence of need does tedizolid phosphate offer advantages to currently available alternatives. Sep 16, 2019 tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, the microbiologically active moiety, following oral and intravenous administration. Lungs of infected mice treated with tedizolid phosphate show less severe inflammation and edema, as indicated by the mean scores for inflammation and edema. Collect powder using special dust vacuum cleaner with particle filter or carefully sweep into suitable waste disposal containers and seal securely. Background information of tedizolid phosphate torezolid phosphate is a novel oxazolidinone for grampositive infections, has an ic50 of 8. Pdf activity of tedizolid phosphate tr701 in murine. The information provided in this safety data sheet is correct to the best of our knowledge, information and belief at the date of its publication. Sivextro tedizolid phosphate for injection,for intravenous use sivextro tedizolid phosphate.
Safety data sheet tributoxyethyl phosphate date prepared. Tedizolid phosphate tr701 is a prodrug activated by plasma or intestinal phosphatases to tedizolid tr700 following administration of the drug either orally or intravenously. Tedizolid phosphate formerly torezolid phosphate, r701, da7218 is the prodrug of tedizolid formerly torezolid, tr700, da7157. Tedizolid phosphate tr701 fa, mk1986 vs linezolid for.
Tedizolid phosphate tr701 fa, mk1986 vs linezolid for the treatment of nosocomial pneumonia mk 1986002 the safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, the microbiologically active moiety, following oral and intravenous administration. Dailymed sivextro tedizolid phosphate tablet, film coated. Means, standard deviations sds, and medians were reported for. Tedizolid phosphate supplier distributor cas 856867555. In murine models of penicillinresistant streptococcus pneumoniae infection, tedizolid was as effective. Thus, linezolid has the potential for causing serotonin syndrome a hyperserotonergic state characterized by mental status changes, neurologic abnormalities, and autonomic instability when it is used in patients with either of the following. The absolute configuration at the 5position of the oxazolidinone ring is the r optical isomer. Sivextrotedizolid phosphate for injection,for intravenous use sivextro tedizolid phosphate tablet,for oral use initial u.
Sivextro tedizolid phosphate dose, indications, adverse. Tedizolid hcl is a reversible, novel oxazolidinone antibiotic. Tedizolid and ach702 have a good intracellular killing activity comparable to. Safety data sheet according to federal register vol. Full text profile of tedizolid phosphate and its potential. Tedizolid phosphate rapidly converted in vivo by phosphatases to the active moiety, tedizolid. Intracellular activity of tedizolid phosphate and ach702 versus mycobacterium tuberculosis infected macrophages.
Tedizolid phosphate is a prodrug that is converted by plasma phosphatases to microbiologically active tedizolid in vivo. Material safety data sheet sodium phosphate solution, saturated 6 section 16 other information msds creation date. Comparative pharmacodynamics of the new oxazolidinone. Material safety data sheet sodium phosphate solution, saturated.
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