Tedizolid

Products

Tedizolid is commercially available as an infusion preparation and in tablet form (Sivextro). It was approved in the United States in 2014 and in many countries and the EU in 2015.

Structure and properties

Tedizolid (C17H15FN6O3, Mr = 370.3 g/mol) is present in the drug in the form of the prodrug tedizolid phosphate, a white to yellow solid. Tedizolid phosphate is metabolized in the body by phosphatases to the active drug tedizolid.

Effects

Tedizolid (ATC J01XX11) has antibacterial properties against Gram-positive pathogens (staphylococci, enterococci, and streptococci). The effects are due to binding to the 50S subunit of bacterial ribosomes, resulting in inhibition of protein synthesis. The half-life is in the range of 12 hours.

Indications

For the treatment of acute bacterial skin and soft tissue infections (ABSSSI, acute bacterial skin and skin structure infections) with susceptible Gram-positive pathogens (, , ).

Dosage

According to the SmPC. The drug is administered once daily for six days.

Contraindications

  • Hypersensitivity
  • Neutropenia

For complete precautions, see the drug label.

Adverse effects

The most common possible adverse effects include nausea, headache, diarrhea, and vomiting.