Zoliflodacin
Chemical compound
From Wikipedia, the free encyclopedia
Zoliflodacin, sold under the brand name Nuzolvence, is an antibiotic used for the treatment of antibiotic-resistant Neisseria gonorrhoeae (gonorrhea).[1][3] Zoliflodacin is a spiropyrimidinetrione bacterial type II topoisomerase inhibitor.[1] Zoliflodacin is being developed as part of a public-private partnership between Innoviva Specialty Therapeutics and the Global Antibiotic Research & Development Partnership (GARDP).[4] Zoliflodacin is taken by mouth.[1][3]
Skeletal structure of zoliflodacin | |
 Ball-and-stick model of zoliflodacin | |
| Clinical data | |
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| Trade names | Nuzolvence |
| Other names | AZD0914; ETX0914 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a626017 |
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| Routes of administration | By mouth |
| Drug class | Antibacterial |
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| Pharmacokinetic data | |
| Bioavailability | 97.8% |
| Metabolism | Liver |
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| Elimination half-life | 5.3–6.3 h |
| Excretion | |
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| Formula | C22H22FN5O7 |
| Molar mass | 487.444 g·mol−1 |
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The most common side effects include low white blood cell counts, headache, dizziness, nausea, and diarrhea.[3]
Zoliflodacin was approved for medical use in the United States in December 2025.[3] The US Food and Drug Administration considers it to be a first-in-class medication.[5][6]
Medical uses
Zoliflodacin is indicated for the treatment of uncomplicated urogenital gonorrhea due to Neisseria gonorrhoeae in people who weigh at least 35 kilograms (77 lb).[1][3]
Susceptible bacteria
Zoliflodacin has shown in vitro activity against the following species of bacteria:[7] Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, and Chlamydia trachomatis
Adverse effects
Animal studies showed that zoliflodacin might cause birth defects, pregnancy loss, or male fertility problems.[3]
Mechanism of action
Zoliflodacin is a spiropyrimidinetrione antibacterial agent (first-in-class) that inhibits bacterial type II topoisomerases, including DNA gyrase and topoisomerase IV.[8] It binds to these enzymes at a site that is distinct from fluoroquinolone binding sites, leading to inhibition of DNA replication and bacterial cell death.[9] This novel mechanism confers activity against strains resistant to other topoisomerase inhibitors and involves inhibition of bacterial type II topoisomerases.[7][10]
History
A high throughput screening campaign aimed at identifying compounds with whole cell antibacterial activity performed at Pharmacia & Upjohn identified compound PNU-286607, a progenitor of Zoliflodacin, as having the desired activity.[11]
Subsequent research at AstraZeneca led to the discovery that the nitroaromatic in PNU-286607 could be replaced with a fused benzisoxazole ring,[12] which allowed for an exploration of different groups at the 3-position of the heterocycle. This work was continued at Entasis Pharmaceuticals where extensive optimization resulted in the discovery of ETX0914.[7]
Researchers tested zoliflodacin in a study with 930 participants who had uncomplicated urogenital gonorrhea.[3] Two-thirds of participants received a single 3-gram dose of zoliflodacin dissolved in water.[3] The other third received the standard treatment of ceftriaxone shot plus azithromycin pill.[3] The study measured how well the medicines cleared the bacteria 4 to 8 days after treatment.[3] The study showed 91% of participants who took zoliflodacin were cured and 96% of participants who received the standard treatment were cured.[3]
Society and culture
Legal status
Zoliflodacin was approved for medical use in the United States in December 2025.[4][13]
The US Food and Drug Administration (FDA) granted the application for zoliflodacin fast track, qualified infectious disease product, and priority review designations for the uncomplicated urogenital gonorrhea indication.[3] The FDA approval for Nuzolvence was granted to Entasis Therapeutics.[3]
Names
Zoliflodacin is the international nonproprietary name.[14]
Zoliflodacin is sold under the brand name Nuzolvence.[4]
