Chemical Property of Tedizolid Phosphate
Chemical Property:
- Melting Point:256.9℃
- Boiling Point:725.6±70.0 °C(Predicted)
- PKA:1.81±0.10(Predicted)
- PSA：162.60000
- Density:1.75±0.1 g/cm3(Predicted)
- LogP:1.57770
- Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
- Solubility.:DMSO (Slightly, Sonicated)
- XLogP3:0.3
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:11
- Rotatable Bond Count:6
- Exact Mass:450.08529741
- Heavy Atom Count:31
- Complexity:702
- Purity/Quality:
-
99% *data from raw suppliers
Tedizolid Phosphate *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4CC(OC4=O)COP(=O)(O)O)F
- Isomeric SMILES:CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4C[C@@H](OC4=O)COP(=O)(O)O)F
- Recent ClinicalTrials:A Study of Safety and Efficacy of MK-1986 (Tedizolid Phosphate) and Comparator in Participants From Birth to Less Than 12 Years of Age With Acute Bacterial Skin and Skin Structure Infections (MK-1986-018)
- Recent EU Clinical Trials:Oral antimicrobial treatment vs. outpatient parenteral for infective
-
Indications
Tedizolid (Tedizolid Phosphate, Tidizolamide) is oxazolidinone compounds for serious Gram-positive bacterial infection treatment:
Acute bacterial skin and skin structure infections and complex skin and soft tissue infections (absssi/cSSTI, IV/oral) (to be approved).
Hospital Acquired/Ventilator-Associated Bacterial Pneumonia (HABP/VABP) (Clinical Phase II).
SIVEXTRO is a class of oxazolidinone-based antimicrobials designed for Acute bacterial skin and skin structure infections (ABSSSI). In order to reduce the development of resistant bacteria and to maintain the effectiveness of SIVEXTRO and other antimicrobial agents, SIVEXTRO should only be used to treat or prevent infections that have been proven or strongly suspected to be bacterial-induced.
-
Description
Tedizolid phosphate was approved by the US FDA in June 2014
for treatment of acute bacterial skin and skin structure infections
caused by susceptible gram-positive pathogens, including
MRSA. Tedizolid phosphate was discovered by Dong-A Pharmaceuticals
in South Korea and developed in the USA by Cubist
Pharmaceuticals (acquired from Trius Therapeutics in 2013,
became a wholly owned subsidiary of Merck in 2015). The
worldwide commercialization rights for tedizolid phosphate are
divided between Cubist in the USA, Canada, and EU, and Bayer in
Asia–Pacific, Latin America, and Africa. This second-generation
oxazolidinone prodrug is rapidly converted to the active form tedizolid
in the presence of endogenous phosphatases. It inhibits
bacterial protein synthesis by binding to the 23S ribosomal RNA
of the 50S subunit of the ribosome, preventing formation of the
70S ribosomal initiation complex, and is 4-fold to 16-fold more
potent against staphylococci and enterococci compared to linezolid.
251 With high oral bioavailability (approximately 90%) and
long half-life (approximately 12 hours), tedizolid phosphate is
the first oxazolidinone antibiotic which can be dosed once daily
either orally or intravenously.
-
Uses
Tedizolid, known as TR-700, is an oral and i.v administered intracellular antibacterial drug.
-
Clinical Use
Reversible non-selective MAO inhibitor:
Antibacterial agent
-
Drug interactions
Potentially hazardous interactions with other drugs
Alcohol: some alcoholic and de-alcoholised drinks
contain tyramine which can cause hypertensive crisis.
Alpha-blockers: avoid concomitant use with
indoramin; enhanced hypotensive effect.
Analgesics: CNS excitation or depression with
pethidine, other opioids and nefopam - avoid;
increased risk of serotonergic effects and convulsions
with tramadol - avoid.
Antidepressants: enhancement of CNS effects and
toxicity; avoid MAOIs, SSRIs and vortioxetine for 2
weeks after use; care with all antidepressants.
Antiepileptics: antagonism of anticonvulsant effect;
avoid carbamazepine with or within 2 weeks of
MAOIs.
Antimalarials: avoid concomitant use with
artemether/lumefantrine and piperaquine with
artenimol.
Antipsychotics: effects enhanced by clozapine.
Atomoxetine: possible increased risk of convulsions
- avoid concomitant use and for 2 weeks after use.
Bupropion: avoid with or for 2 weeks after MAOIs.
Dapoxetine: increased risk of serotonergic effects,
avoid with or for 2 weeks after MAOIs.
Dexamfetamine and lisdexamfetamine: risk of
hypertensive crisis, avoid with or for 2 weeks after
MAOIs.
Dopaminergics: avoid concomitant use with
entacapone and tolcapone; hypertensive crisis with
levodopa and rasagiline - avoid for at least 2 weeks
after stopping MAOI; hypotension with selegiline.
5HT1
agonist: risk of CNS toxicity with
sumatriptan, rizatriptan and zolmitriptan - avoid
sumatriptan and rizatriptan for 2 weeks after MAOI.
Metaraminol: risk of hypertensive crisis, avoid with
or for 2 weeks after MAOIs.
Methyldopa: avoid concomitant use.
Opicapone: avoid concomitant use.
Sympathomimetics: hypertensive crisis with
sympathomimetics - avoid.
Tetrabenazine: risk of CNS excitation and
hypertension - avoid.
