Zoliflodacin

NUZOLVENCE is an antibacterial drug [see Microbiology (12.4) ] .

• NUZOLVENCE is a spiropyrimidinetrione bacterial type II topoisomerase inhibitor indicated for the 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. ( 1.1 ) Usage to Reduce Development of Drug-Resistant Bacteria To reduce the development of drug-resistant bacteria and maintain the effectiveness of NUZOLVENCE and other antibacterial drugs, NUZOLVENCE should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

• NUZOLVENCE is contraindicated in: patients with a known history of hypersensitivity to NUZOLVENCE [see Warnings and Precautions (5.4) ] . patients who use concomitant moderate or strong CYP3A4 inducers because concomitant use is predicted to result in decreased plasma concentrations of zoliflodacin and may reduce the efficacy of NUZOLVENCE [see Drug Interactions (7.1) and Clinical Pharmacology (12.3) ].contraindicated

Pregnancy Testing: Obtain a pregnancy test in females of reproductive potential prior to initiating NUZOLVENCE. ( 2.1 ) NUZOLVENCE must be mixed with water before administering. ( 2.2 ) Do not mix NUZOLVENCE with other liquids or sprinkle on food. ( 2.2 ) Administer the entire dose within 15 minutes of mixing. If the dose is not administered within 15 minutes of mixing, a new dose of NUZOLVENCE must be prepared. ( 2.2 , 2.4 ) Adults and pediatric patients 12 years of age and older, weighing at least 35 kg: Recommended dose is 3 g (one packet) administered as a single dose orally. ( 2.3 ) Patients weighing 35 kg to less than 50 kg: Administer NUZOLVENCE on an empty stomach, 1 hour before or 2 hours after food. ( 2.3 ) Patients weighing greater than or equal to 50 kg: Administer NUZOLVENCE with food. ( 2.3 ) See full prescribing information for complete details on preparation and administration of NUZOLVENCE. ( 2.4 ) 2.1 Pregnancy Testing in Females of Reproductive Potential Obtain a pregnancy test in females of reproductive potential prior to initiating treatment with NUZOLVENCE [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1 , 8.3) ]. 2.2 Important Administration Instructions NUZOLVENCE must be mixed with water before administering. Do not mix NUZOLVENCE with other liquids or sprinkle on food. Do not take NUZOLVENCE in the dry form. Administer the entire dose within 15 minutes of mixing. If the dose is not administered within 15 minutes of mixing, a new dose of NUZOLVENCE must be prepared [see Dosage and Administration (2.4) ] .

Embryo-Fetal Toxicity: Potential Risk for Pregnant Females: May cause fetal harm when administered during pregnancy based on data from animal studies. Advise pregnant females about the potential risk to the fetus with maternal exposure to NUZOLVENCE. Avoid use of NUZOLVENCE during pregnancy. ( 5.1 , 8.1 , 8.3 ) Embryo-Fetal Toxicity: Potential Risk Related to Males with Female Partners of Reproductive Potential: Advise males with female partners of reproductive potential to use effective contraception for at least 3 months after administration of NUZOLVENCE. ( 5.2 , 8.3 , 13.1 ) Testicular Toxicity and Risks to Male Fertility: May cause testicular toxicity and impair male fertility based on data from animal studies. An assessment of spermatogenesis has not been conducted in humans. Advise males of the potential risk. ( 5.3 , 8.3 , 13.1 ) Hypersensitivity Reactions: Hypersensitivity reactions, including rash and pruritus, have been reported in patients receiving NUZOLVENCE. Discontinue NUZOLVENCE and institute appropriate supportive measures, if an allergic reaction occurs. ( 5.4 ) Clostridioides difficile Infection: Evaluate if diarrhea occurs. ( 5.5 ) 5.1 Embryo-Fetal Toxicity: Potential Risk for Pregnant Females Based on data from animal studies, NUZOLVENCE may cause fetal harm when administered to a pregnant female at clinically relevant doses.

The following clinically significant adverse reactions are discussed in the Warnings and Precautions section of the labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.4) ] The most common adverse reactions including laboratory abnormalities (incidence ≥2%) with NUZOLVENCE are neutropenia, headache, leukopenia, dizziness, nausea, and diarrhea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Entasis Therapeutics, Inc. at 1-800-651-3861 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. A total of 782 patients received a 3 g dose of zoliflodacin across all phases of clinical trials. The safety of NUZOLVENCE was evaluated in a phase 3, randomized, open-label, active-controlled, multicenter, multinational trial (NCT03959527) (Trial 1). In total, 927 patients with suspected uncomplicated gonorrhea due to N. gonorrhoeae were randomized (2:1) and treated with either a single oral 3 g dose of NUZOLVENCE (N=619) or a combination of a single 500 mg intramuscular dose of ceftriaxone and a single 1 g oral dose of azithromycin (N=308) [see Clinical Studies (14) ] . Patients were eligible for enrollment if they were ≥12 years old and ≥35 kg.

8.1 Pregnancy Risk Summary Based on findings from animal studies, NUZOLVENCE may cause fetal malformations or increased embryo-fetal loss when administered to a pregnant female. In pregnant mice, repeat oral administration of zoliflodacin during organogenesis was associated with fetal malformations (exencephaly) and increased embryo-fetal loss at AUC exposures 1.6-fold the MRHD and decreased fetal weights at 2.9-fold the MRHD. In pregnant rats, zoliflodacin administration resulting in AUC exposures 8.5-fold the MRHD increased embryo-fetal loss, and exposures 3.2-fold the MRHD decreased fetal weights. There was no effect on embryo-fetal survival at exposures 5.5-fold the MRHD to zoliflodacin in pregnant rats. When zoliflodacin was administered to rats throughout pregnancy, parturition, and lactation, no effects on pup survival, birth weight, or growth were observed at maternal exposures up to 2.4-fold the MRHD (see Data ). There are no human data on NUZOLVENCE use in pregnancy to evaluate the drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. Advise pregnant females about the potential risk to the fetus with maternal exposure to NUZOLVENCE [see Warnings and Precautions (5.1) and Use in Specific Populations (8.3) ] . A postmarketing descriptive pregnancy safety study is available for NUZOLVENCE.

Metabolism

Zoliflodacin, as single doses, generally displayed dose-proportional increases in exposure up to 800 mg (0.27 times the recommended dosage). Increases above 800 mg led to slightly less than dose-proportional increases in exposure up to 4 g (1.3 times the recommended dosage).

• Dec 12, 2025NDANDA219491Entasis Therap

The 9 most recently updated of 9 ClinicalTrials.gov registrations naming Zoliflodacin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Study to Evaluate the Effect of a Single Oral Dose of Zoliflodacin 3 g on Testicular Function in Healthy Adult Men
  Not yet recruiting · Phase 4 · Interventional · 200 enrolled · Global Antibiotics Research and Development Partnership
  NCT07640477updated 2026-06-10
• Zoliflodacin in Uncomplicated Gonorrhoea
  Completed · Phase 3 · Interventional · 1,011 enrolled · Global Antibiotics Research and Development Partnership
  NCT03959527updated 2025-10-08
• Zoliflodacin Bioequivalence and Drug-Drug Interaction Study
  Completed · Phase 1 · Interventional · 50 enrolled · Global Antibiotics Research and Development Partnership
  NCT05635305updated 2023-03-01
• Thorough QT/QTC (TQT) Clinical Trial to Evaluate the Effect of Zoliflodacin on Cardiac Repolarization in Healthy Male and Female Subjects
  Completed · Phase 1 · Interventional · 72 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT03613649updated 2020-03-27
• A Study to Evaluate the Safety, Tolerability and Plasma PK of a Single Oral Dose of Zoliflodacin in Healthy Male and Female Volunteers
  Completed · Phase 1 · Interventional · 8 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT03404167updated 2019-03-18
• Study to Investigate Effect of Food and Safety of a New Formulation of Zoliflodacin
  Completed · Phase 1 · Interventional · 48 enrolled · Drugs for Neglected Diseases
  NCT03718806updated 2018-12-06
• Randomized, Open-label Phase 2 Study of Oral AZD0914 in the Treatment of Gonorrhea
  Completed · Phase 2 · Interventional · 180 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT02257918updated 2017-03-22
• AZD0914 Phase 1 ADME Study in Healthy Volunteers
  Completed · Phase 1 · Interventional · 6 enrolled · Entasis Therapeutics
  NCT02298920updated 2015-06-03
• A Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD0914
  Completed · Phase 1 · Interventional · 100 enrolled · AstraZeneca
  NCT01929629updated 2014-04-15

Frequently asked questions

How does Zoliflodacin work?

NUZOLVENCE is an antibacterial drug [see Microbiology (12.4) ] .

What is Zoliflodacin used for?

According to FDA labeling, Zoliflodacin carries indications including: NUZOLVENCE is a spiropyrimidinetrione bacterial type II topoisomerase inhibitor indicated for the 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. ( 1.1 ) Usage to Reduce Development of Drug-Resistant Bacteria To reduce the development of drug-resistant bacteria and maintain the effectiveness of NUZOLVENCE and other antibacterial drugs, NUZOLVENCE should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Zoliflodacin?

Zoliflodacin is classified as Cytochrome P450 3A4 Inducers, DNA Gyrase Inhibitors, Topoisomerase 4 Inhibitors, Decreased DNA Replication, Decreased Transcription to RNA.

What are the brand names for Zoliflodacin?

Zoliflodacin is marketed under brand names including Nuzolvence.

What are the contraindications for Zoliflodacin?

Zoliflodacin labeling lists contraindications including: NUZOLVENCE is contraindicated in: patients with a known history of hypersensitivity to NUZOLVENCE [see Warnings and Precautions (5.4) ] . patients who use concomitant moderate or strong CYP3A4 inducers because concomitant use is predicted to result in decreased plasma concentrations of zoliflodacin and may reduce the efficacy of NUZOLVENCE [see Drug Interactions (7.1) and Clinical Pharmacology (12.3) ].. Always consult the full prescribing information and a clinician.