Zoliflodacin (Nuzolvence) for Treatment of Uncomplicated Gonorrhea

Zoliflodacin (Nuzolvence) is a single-dose oral antibiotic in the spiropyrimidinetrione drug class. This class of bactericidal antibiotics inhibits DNA synthesis and has shown in vitro activity against drug-resistant strains of Neisseria gonorrhoeae.¹ Zoliflodacin is labeled for the treatment of uncomplicated urogenital gonorrhea in adults and adolescents 12 years and older who weigh at least 35 kg (77 lbs).

No long-term safety data for zoliflodacin are available. In one clinical trial, incidence and types of adverse events were similar to those observed with comparator therapy of ceftriaxone 500 mg (intramuscular) plus azithromycin 1 g (oral).² Zoliflodacin should not be prescribed for patients who are taking moderate or strong cytochrome P4503A4 inducers (eg, rifampin, carbamazepine, St. John's wort) because these medicines may reduce the effectiveness of zoliflodacin.¹ Clinical trials did not include pregnant or breastfeeding patients. Animal studies suggest a risk of fetal harm when administered to pregnant patients or their male sex partners. The manufacturer suggests pregnancy testing before administration for those who may become pregnant. Male sex partners should use effective contraception for 3 months after receiving treatment. Zoliflodacin has been associated with male infertility in animal studies when given at higher than typical clinical doses.¹

Zoliflodacin is generally well tolerated. The most frequently reported adverse effects are headache (10%), dizziness (3%), nausea (3%), and diarrhea (2%). Rates of these adverse events are similar to those observed in comparator groups.^2,3

Zoliflodacin has been evaluated in a study of 930 patients with suspected uncomplicated gonorrheal infection without demonstrated resistance to ceftriaxone plus azithromycin. A single 3-g dose of zoliflodacin or ceftriaxone, 500 mg, plus azithromycin, 1 g, were randomly assigned to 621 participants and 309 participants, respectively. Zoliflodacin produced a 91% microbiologic cure rate at urogenital sites compared with a 96% cure rate with ceftriaxone plus azithromycin.²

Zoliflodacin has not been compared with oral cefixime or studied in patients who did not respond to other therapies. It produces low cure rates for pharyngeal and rectal infections (79.2% and 87.3%, respectively) and is not labeled for treatment of these infections.²

The World Health Organization and Centers for Disease Control and Prevention currently do not recommend zoliflodacin. A 95% cure rate is recommended by the World Health Organization for treatment of gonorrhea, which is higher than that found with zoliflodacin (upper end of 95% CI, 93.3%).^2,4

Although zoliflodacin has been approved by the US Food and Drug Administration, it is not yet available in pharmacies, and its cost is unknown. A single dose of ceftriaxone costs approximately $15, with an additional administration fee.⁵

Zoliflodacin should be taken orally as a single 3-g dose. It is supplied as granules in a sachet. Patients should mix zoliflodacin with 60 mL of water and consume it within 15 minutes of preparation. Patients should not ingest the granules in dry form.¹