|Other names||TR-700, torezolid|
|Drug class||Oxazolidinone antibiotic|
|Main uses||Skin and skin structure infection|
|By mouth, intravenous|
|Elimination half-life||12 hours|
|Chemical and physical data|
|Molar mass||370.344 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Tedizolid, sold under the brand name Sivextro, is an antibiotic used for skin and skin structure infection including cellulitis and skin abscesses. This includes cases due to meticillin-resistant Staphylococcus aureus (MRSA). It can be given by mouth or by gradual injection into a vein.
Common side effects include nausea, headache, diarrhea, and vomiting. Other side effects may include Clostridioides difficile infection. Safety in pregnancy and breastfeeding is unclear. It is in the oxazolidinone class of medications and works by blocking bacteria from making protein.
Tedizolid was approved for medical use in the United States in 2014 and Canada and Europe in 2015. In the United States a 6 day course of treatment costs about 2,300 USD as of 2021. This amount in the United Kingdom costs the NHS about £862.
Tedizolid is used for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by certain susceptible bacteria, including Staphylococcus aureus (including methicillin-resistant strains, MRSA, and methicillin-susceptible strains), various Streptococcus species (S. pyogenes, S. agalactiae, and S. anginosus group including S. anginosus, S. intermedius, and S. constellatus), and Enterococcus faecalis.
The recommended dosage for treatment is 200 mg once daily for a total duration of six days, either by mouth (with or without food) or through an intravenous injection (if patient is older than 18 years old).
The most common side effects found in the clinical trials were nausea, headache, diarrhea, vomiting, and dizziness. Tedizolid has also been found to have hematologic (blood) effects, as shown in Phase-I studies in which subjects exposed to doses longer than 6 days showed a possible dose and duration effect on hematologic parameters. Its safety in patients with decreased levels of white blood cells has not been established. Patients on tedizolid are also at low risk of peripheral and optic neuropathy, similar to other members of the oxazolidinone class.
Mechanism of action
Tedizolid phosphate (TR-701) is a prodrug activated by plasma or intestinal phosphatases to tedizolid (TR-700) following administration of the drug either orally or intravenously. Once activated, tedizolid exerts its bacteriostatic microbial activity through inhibition of protein synthesis by binding to the 50S ribosomal subunit (on the acceptor site) of the bacteria.
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).
Tedizolid is the second treatment approved by the FDA under the new federal law Generating Antibiotic Incentives Now (known as the GAIN Act). New antibiotics manufactured under this new act will be designed as a Qualified Infectious Disease Product (QIDP), allowing an expedited review by the FDA and an additional five years of market exclusivity.
Tedizolid showed noninferiority to linezolid in two phase-III trials, known as the ESTABLISH trials.
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