Zoliflodacin (Nuzolvence)

Zoliflodacin (Nuzolvence) photo pending

TOP 3 POINTS

1. Only FDA-approved for treatment of uncomplicated urogenital gonorrhea due to Neisseria gonorrhoeae
2. Provided as a packet with special administration instructions for a one-time oral dose, comes with mixing container
3. Concerns about fetal toxicity should be heeded

KEY POINTS

• Zoliflodacin is a spiropyrimidinetrione bacterial type II topoisomerase inhibitor. It interferes with DNA synthesis by binding to cleaved DNA-gyrase complex, blocking re-ligation, and interacting with conserved amino acids in the gyrase B subunit.
  • Similar in mechanism to fluoroquinolones or gepotidacin, but in a different class
  • Label says it is distributed by La Jolla Pharmaceutical company and a trademark of Entasis Therapeutics, with marketing by Innoviva Specialty Therapeutics
• FDA approved 12 December 2025 for treatment of uncomplicated urogenital gonorrhea due to Neisseria gonorrhoeae in adults and pediatric patients 12 years of age and older, weighing at least 35 kg
  • Dosed as 3 grams (one packet) mixed with water, given oral once
    • There is an inverse relationship with body weight and zoliflodacin exposure
      • Patients weighing 50 kg or more should take it with food
      • Patients weighing 35-49 kg should take it on an empty stomach, an hour before or two hours after food
    • Not recommended to mix with other liquids besides water
    • Recommended to use provided mixing container, after taking dose add another 60 mL, shake again, and consume that too to ensure total dose is delivered
    • Dose to be taken w/in 15 minutes of mixing
• Package insert only lists activity against Neisseria gonorrhoeae
• Contraindicated if (1) history of hypersensitivity reaction to zoliflodacin and (2) not to use w/ moderate or strong CYP3A4 inducers which reduce zoliflodacin concentrations (it is a substrate) and therefore risk efficacy
• Warnings and precautions include:
  • Embryo-fetal toxicity
    • Pregnancy test recommended prior to treating female of reproductive potential
    • Male partners to be advised to use contraceptive for at least 3 months after administration
  • Testicular toxicity
  • Hypersensitivity reaction
  • Clostridioides difficile infection
• The most common side effects are neutropenia, headache, leukopenia, dizziness, nausea, and diarrhea
• Studied against ceftriaxone and azithromycin for safety and efficacy
  • Similar microbiological cure rate (90%+)

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