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Zoliflodacin
View on Wikipedia
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| Clinical data | |
|---|---|
| Trade names | Nuzolvence |
| Other names | AZD0914; ETX0914 |
| AHFS/Drugs.com | nuzolvence |
| License data |
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| Routes of administration | By mouth |
| Drug class | Antibacterial |
| ATC code |
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| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 97.8% |
| Metabolism | Liver |
| Onset of action |
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| Elimination half-life | 5.3–6.3 h |
| Excretion | |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| DrugBank | |
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| KEGG | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C22H22FN5O7 |
| Molar mass | 487.444 g·mol−1 |
| 3D model (JSmol) | |
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Zoliflodacin, sold under the brand name Nuzolvence, is an antibiotic used for the treatment of antibiotic-resistant Neisseria gonorrhoeae (gonorrhea).[2] Zoliflodacin is being developed as part of a public-private partnership between Innoviva Specialty Therapeutics and the Global Antibiotic Research & Development Partnership (GARDP).[3] Zoliflodacin is taken by mouth.[2]
The most common side effects include low white blood cell counts, headache, dizziness, nausea, and diarrhea.[2]
Zoliflodacin was approved for medical use in the United States in December 2025.[2]
Medical uses
[edit]Zoliflodacin is indicated for the treatment of uncomplicated urogenital gonorrhea in people who weigh at least 77 pounds (35 kg).[2]
Susceptible bacteria
[edit]Zoliflodacin has shown in vitro activity against the following species of bacteria:[4] Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, and Chlamydia trachomatis
Adverse effects
[edit]Animal studies showed that zoliflodacin might cause birth defects, pregnancy loss, or male fertility problems.[2]
Mechanism of action
[edit]Zoliflodacin is a spiropyrimidinetrione antibacterial agent (first-in-class) that inhibits bacterial type II topoisomerases, including DNA gyrase and topoisomerase IV.[5] 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.[6] This novel mechanism confers activity against strains resistant to other topoisomerase inhibitors and involves inhibition of bacterial type II topoisomerases.[4][7]
History
[edit]
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.[8]
Subsequent research at AstraZeneca led to the discovery that the nitroaromatic in PNU-286607 could be replaced with a fused benzisoxazole ring,[9] 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.[4]
Researchers tested zoliflodacin in a study with 930 participants who had uncomplicated urogenital gonorrhea.[2] Two-thirds of participants received a single 3-gram dose of zoliflodacin dissolved in water.[2] The other third received the standard treatment of ceftriaxone shot plus azithromycin pill.[2] The study measured how well the medicines cleared the bacteria 4 to 8 days after treatment.[2] The study showed 91% of participants who took zoliflodacin were cured and 96% of participants who received the standard treatment were cured.[2]
Society and culture
[edit]Legal status
[edit]Zoliflodacin was approved for medical use in the United States in December 2025.[3][10]
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.[2] The FDA approval for zoliflodacin was granted to Entasis Therapeutics.[2]
Names
[edit]Zoliflodacin is the international nonproprietary name.[11]
Zoliflodacin is sold under the brand name Nuzolvence.[3]
References
[edit]- ^ "Highlights of prescribing information - NUZOLVENCE (zoliflodacin) for oral suspension" (PDF). innovivaspecialtytherapeutics.com.
- ^ a b c d e f g h i j k l m n "FDA Approves Two Oral Therapies to Treat Gonorrhea". U.S. Food and Drug Administration (FDA) (Press release). 12 December 2025. Retrieved 13 December 2025.
This article incorporates text from this source, which is in the public domain.
- ^ a b c Pierre G (12 December 2025). "Nuzolvence (Zoliflodacin) Receives U.S. FDA Approval". Global Antibiotic Research & Development Partnership (GARDP). Retrieved 13 December 2025.
- ^ a b c Basarab GS, Kern GH, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, et al. (July 2015). "Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases". Scientific Reports. 5 (1) 11827. Bibcode:2015NatSR...511827B. doi:10.1038/srep11827. PMC 4501059. PMID 26168713.
- ^ Taylor R (2020). "In Vitro Activity and Mechanism of Zoliflodacin, a Novel Spiropyrimidinetrione Antibiotic". Antimicrobial Agents and Chemotherapy. 64 (10). doi:10.1128/AAC.00950-20. PMID 32329999.
- ^ Bradford PA, Miller AA, O'Donnell J, Mueller JP (June 2020). "Zoliflodacin: An Oral Spiropyrimidinetrione Antibiotic for the Treatment of Neisseria gonorrheae, Including Multi-Drug-Resistant Isolates". ACS Infectious Diseases. 6 (6): 1332–1345. doi:10.1021/acsinfecdis.0c00021. PMID 32329999.
- ^ Pisano L, Giovannuzzi S, Supuran CT (June 2024). "Management of Neisseria gonorrhoeae infection: from drug resistance to drug repurposing". Expert Opinion on Therapeutic Patents. 34 (6): 511–524. doi:10.1080/13543776.2024.2367005. PMID 38856987.
- ^ Miller AA, Bundy GL, Mott JE, Skepner JE, Boyle TP, Harris DW, et al. (August 2008). "Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors". Antimicrobial Agents and Chemotherapy. 52 (8): 2806–2812. doi:10.1128/AAC.00247-08. PMC 2493097. PMID 18519725.
- ^ Basarab GS, Brassil P, Doig P, Galullo V, Haimes HB, Kern G, et al. (November 2014). "Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization". Journal of Medicinal Chemistry. 57 (21): 9078–9095. doi:10.1021/jm501174m. PMID 25286019.
- ^ "U.S. FDA Approves Nuzolvence (zoliflodacin), a First-in-Class, Single-dose, Oral Antibiotic for the Treatment of Uncomplicated Urogenital Gonorrhea in Adults and Adolescents" (Press release). Innoviva Specialty Therapeutics. 12 December 2025. Retrieved 28 December 2025 – via Business Wire.[dead link]
- ^ World Health Organization (2016). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 76". WHO Drug Information. 30 (3). hdl:10665/331020.
Further reading
[edit]- Luckey A, Balasegaram M, Barbee LA, Batteiger TA, Broadhurst H, Cohen SE, et al. (2025). "Zoliflodacin versus ceftriaxone plus azithromycin for treatment of uncomplicated urogenital gonorrhoea: an international, randomised, controlled, open-label, phase 3, non-inferiority clinical trial". The Lancet. doi:10.1016/S0140-6736(25)01953-1.
- Taylor SN, Marrazzo J, Batteiger BE, Hook EW, Seña AC, Long J, et al. (November 2018). "Single-Dose Zoliflodacin (ETX0914) for Treatment of Urogenital Gonorrhea". The New England Journal of Medicine. 379 (19): 1835–1845. doi:10.1056/NEJMoa1706988. hdl:1805/19865. PMID 30403954.
External links
[edit]- Clinical trial number NCT03959527 for "Zoliflodacin in Uncomplicated Gonorrhoea" at ClinicalTrials.gov
