A Phase 1, Single-dose, Open-label, Randomized, 4-way Crossover Zoliflodacin Bioequivalence Study of the Reference Product (ZoliPa) With the Test Product (ZoliDr) in Healthy Adult Volunteers Under Fasted and Specific Fed Conditions Paired With an Investigation of the Effect of Cytochrome P450 3A4 Inhibition by Itraconazole on 3g Zoliflodacin (ZoliPa) Single-dose Pharmacokinetics

this study will be a Phase 1, single-dose, two parallel cohorts, open-label, randomized study in healthy subjects with Cohort 1 as bioequivalence (BE) and food effect study and Cohort 2 as a drug-drug interaction (DDI) study.

Start Date09 Nov 2022

Sponsor / Collaborator

Global Antibiotic Research & Development Partnership

[+2]

NCT03959527

/ CompletedPhase 3IIT

A Multi-center, Randomized, Open-label, Non Inferiority Trial to Evaluate the Efficacy and Safety of a Single, Oral Dose of Zoliflodacin Compared to a Combination of a Single Intramuscular Dose of Ceftriaxone and a Single Oral Dose of Azithromycin in the Treatment of Patients With Uncomplicated Gonorrhoea

This trial is a multi-center, open label, randomized controlled, non-inferiority phase III trial evaluating the safety and efficacy of a 3 g oral dose of zoliflodacin compared to a combination of a single intra-muscular 500 mg dose of ceftriaxone and a single 1 g oral dose of azithromycin for the treatment of uncomplicated gonorrhoea.

Start Date06 Nov 2019

Sponsor / Collaborator

Global Antibiotic Research & Development Partnership

NCT03718806

/ CompletedPhase 1IIT

A Phase 1, Open-Label, Study to Investigate Pharmacokinetics, Effect of Food and Safety of a New Immediate-Release Formulation of Zoliflodacin in Healthy Subjects

This is a phase I, parallel, open-label, randomized, cross-over, single-center study with zoliflodacin administered as granules for oral suspension with or without food.
It is planned to enroll 2 cohorts (Cohorts 1 and 2) of 24 subjects each (48 subjects in total), with the target of achieving data in 20 evaluable subjects per cohort. Single doses of zoliflodacin will be assessed within each cohort in a two period cross-over design.
Each subject will receive one of the following regimens per period, depending on cohort, in a sequence according to the randomization schedule (per cohort, subjects will be randomized immediately before dosing in Period 1), separated by a minimum 4 day washout between each period. The actual length of washout period may change pending emerging PK data.
Cohort 1:
* Regimen A: 3 g zoliflodacin oral suspension; oral administration after an overnight fast
* Regimen B: 3 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast
Cohort 2
* Regimen C: 4 g zoliflodacin oral suspension; oral administration after an overnight fast
* Regimen D: 4 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast

Start Date03 Oct 2018

Sponsor / Collaborator

Drugs for Neglected Diseases initiative

[+1]

100 Clinical Results associated with Zoliflodacin

100 Translational Medicine associated with Zoliflodacin

100 Patents (Medical) associated with Zoliflodacin

Literatures (Medical) associated with Zoliflodacin

01 Nov 2025·Annals of Laboratory Medicine

In-vitro Activities of Zoliflodacin and Solithromycin Against Neisseria gonorrhoeae Isolates from Korea

Article

Author: Roh, Kyoung Ho ; Lee, Hyukmin ; Seo, Young Hee ; Luong, Nguyen Dinh ; Unemo, Magnus ; Liu, Changseung ; Lee, Kyungwon

Novel antimicrobial agents are continually developed to address the global threat of multidrug-resistant Neisseria gonorrhoeae. Promising candidates include zoliflodacin and, possibly, solithromycin. We evaluated their in-vitro activities against gonococcal isolates collected in Korea. In total, 250 N. gonorrhoeae isolates obtained across Korea between 2016 and 2018 were used to determine the minimum inhibitory concentrations (MICs) of 10 therapeutic agents using the CLSI agar dilution method. Most isolates (94.8%, 237/250) demonstrated non-susceptibility to penicillin G, tetracycline, and ciprofloxacin, and susceptibility to ceftriaxone and spectinomycin was substantially high. The half-maximal IC (MIC50) and 90% IC (MIC90) values for zoliflodacin were 0.03 and 0.06 μg/mL, respectively; 0.06 and 0.12 μg/mL, respectively, for solithromycin; and 0.03 and 0.12 μg/mL, respectively, for ceftriaxone. Notably, no cross-resistance was observed between zoliflodacin and ciprofloxacin, despite both targeting DNA topoisomerase II enzymes. Zoliflodacin and solithromycin demonstrated significant in-vitro activity against multidrug-resistant N. gonorrhoeae isolates, and zoliflodacin has shown non-inferiority to ceftriaxone/azithromycin dual therapy in a clinical phase 3 trial. Collectively, our findings highlight the potential of zoliflodacin as a novel therapeutic agent for gonococcal infections, particularly in the context of rising multidrug resistance, and highlight the need for continued surveillance and development of alternative antimicrobial strategies.

10 Jan 2025·FEMS MICROBIOLOGY LETTERS

In vitro evolution of ciprofloxacin resistance in Neisseria commensals and derived mutation population dynamics in natural Neisseria populations

Article

Author: Robinson, Leah R ; McDevitt, Caroline J ; Quail, Sophie L ; Regan, Molly R ; Wadsworth, Crista B

Abstract:

Commensal Neisseria are members of a healthy human oropharyngeal microbiome; however, they also serve as a reservoir of antimicrobial resistance for their pathogenic relatives. Despite their known importance as sources of novel genetic variation for pathogens, we still do not understand the full suite of resistance mutations commensal species can harbor. Here, we use in vitro selection to assess the mutations that emerge in response to ciprofloxacin selection in commensal Neisseria by passaging four replicates of four different species in the presence of a selective antibiotic gradient for 20 days; then categorized derived mutations with whole genome sequencing. Ten out of sixteen selected cells lines across the four species evolved ciprofloxacin resistance (≥1 ug/ml); with resistance-contributing mutations primarily emerging in DNA gyrase subunit A and B (gyrA and gyrB), topoisomerase IV subunits C and E (parC and parE), and the multiple transferable efflux pump repressor (mtrR). Of note, these derived mutations appeared in the same loci responsible for ciprofloxacin-reduced susceptibility in the pathogenic Neisseria, suggesting conserved mechanisms of resistance across the genus. Additionally, we tested for zoliflodacin cross-resistance in evolved strain lines and found 6 lineages with elevated zoliflodacin minimum inhibitory concentrations. Finally, to interrogate the likelihood of experimentally derived mutations emerging and contributing to resistance in natural Neisseria, we used a population-based approach and identified GyrA 91I as a substitution circulating within commensal Neisseria populations and ParC 85C in a single gonococcal isolate. A small cluster of gonococcal isolates shared commensal alleles at parE, suggesting recent cross-species recombination events.

11 Oct 2024·ACS Infectious Diseases

Role of DNA Double-Strand Break Formation in Gyrase Inhibitor-Mediated Killing of Nonreplicating Persistent Mycobacterium tuberculosis in Caseum

Article

Author: Ashwath, Priyanka ; Sarathy, Jansy P. ; Via, Laura E. ; Weiner, Danielle ; Osiecki, Paulina

Tuberculosis is the leading cause of mortality by infectious agents worldwide. The necrotic debris, known as caseum, which accumulates in the center of pulmonary lesions and cavities is home to nonreplicating drug-tolerant Mycobacterium tuberculosis that presents a significant hurdle to achieving a fast and durable cure. Fluoroquinolones such as moxifloxacin are highly effective at killing this nonreplicating persistent bacterial population and boosting TB lesion sterilization. Fluoroquinolones target bacterial DNA gyrase, which catalyzes the negative supercoiling of DNA and relaxes supercoils ahead of replication forks. In this study, we investigated the potency of several other classes of gyrase inhibitors against M. tuberculosis in different states of replication. In contrast to fluoroquinolones, many other gyrase inhibitors kill only replicating bacterial cultures but produce negligible cidal activity against M. tuberculosis in ex vivo rabbit caseum. We demonstrate that while these inhibitors are capable of inhibiting M. tuberculosis gyrase DNA supercoiling activity, fluoroquinolones are unique in their ability to cleave double-stranded DNA at low micromolar concentrations. We hypothesize that double-strand break formation is an important driver of gyrase inhibitor-mediated bactericidal potency against nonreplicating persistent M. tuberculosis populations in the host. This study provides general insight into the lesion sterilization potential of different gyrase inhibitor classes and informs the development of more effective chemotherapeutic options against persistent mycobacterial infections.

News (Medical) associated with Zoliflodacin

12 Dec 2025

·www.fiercepharma.com

FDA endorses 2nd new gonorrhea treatment, clearing way for Innoviva's Nuzolvence

On consecutive days, the FDA approved two new oral, first-in-class antibiotics for the treatment of gonorrhea. After a three-decade drought of new antibiotics to treat gonorrhea, the FDA has signed off on two first-in-class oral treatments for the sexually transmitted infection (STI), which affects more than 80 million people around the world each year. Friday, the U.S. regulator greenlighted Innoviva’s Nuzolvence (zoliflodacin) for uncomplicated urogenital gonorrhea. The nod comes less than 24 hours after the agency granted an approval in the same indication to GSK’s Blujepa, which was already on the market for uncomplicated urinary tract infections following its approval in March.The endorsements are similar in that both therapies are indicated for those ages 12 and older where standard of care treatment is contraindicated or where patients are intolerant or unwilling to use the first line of treatment.While the clearance for Nuzolvence covers patients weighing at least 35 kg (77 pounds), patients must weigh at least 99 pounds to start on Blujepa, according to the FDA..The approvals come at an important juncture as antimicrobial resistance to gonorrhea treatment has been growing. Gonorrhea has been recognized by the World Health Organization and the U.S. Centers for Disease Control and Prevention (CDC) as a priority pathogen and an urgent public threat.The development of Nuzolvence was part of a private, not-for-profit collaboration with the Global Antibiotic Research and Development Partnership (GARDP), which sponsored and conducted the phase 3 clinical trial on which FDA approval was based. “This approval marks a huge turning point in the treatment of multidrug-resistant gonorrhoea, which until now has been outpacing antibiotic development,” Manica Balasegaram, M.D., executive director of the GARDP, said in a release. “Zoliflodacin shows that a different public-private partnership approach to antibiotic development is possible—one that prioritizes global health needs, strengthens access where the burden is highest, and protects the effectiveness of new drugs for the long-term.” The approval for Innoviva comes one day after the company published (PDF) results in The Lancet from a phase 3 trial demonstrating the noninferiority of Nuzolvence to the standard care combination treatment of injected ceftriaxone and oral azithromycin.“A new antibiotic that does not require injection and can be used for patients who are allergic to penicillin or related drugs meets two important unmet needs in the treatment of gonorrhea.," lead trial investigator Edward Hook III, M.D., of the University of Alabama at Birmingham, said in a release. Innoviva asserts that its study of 930 patients is the largest ever conducted for a new treatment against Neisseria gonorrhoeae, the bacteria behind gonorrhea. The program included 16 trial sites in five countries—Belgium, the Netherlands, South Africa, Thailand and the U.S.—in five different global regions where there is a high prevalence of the STI.“As clinicians, we see the devastating impact drug-resistant gonorrhoea can have on people’s lives in Thailand,” Rossaphorn Kittiyaowamarn, M.D., the principal Investigator for Bangrak STI Medical Center, said in a release. “With the number of cases on the rise, there is also huge value in carrying out trials in high-burden countries and among high-burden populations to bring about effective treatment options." If left untreated or inadequately treated, gonorrhea can lead to infertility and other sexual and reproductive health issues. In 2023, there were more than 600,000 cases of gonorrhea in the U.S., according to the CDC, making it the second-most common STI after chlamydia. For its part, Innoviva traces its roots to 1996, when it was established as a royalty management company called Advanced Medicine. It rebranded with its current name in 2016. Over a span of two months in 2022, the company bought out La Jolla and Entasis and combined them to form a subsidiary, Innoviva Specialty Therapeutics, to commercialize critical care and infectious disease treatments. “The FDA’s approval of Nuzolvence marks a pivotal moment for patients and the broader healthcare community managing gonorrhea infections,” Pavel Raifeld, CEO of Innoviva, said in a statement. “This achievement reflects the strength of our development capabilities and the impact of our collaboration with GARDP and the global scientific community.”

Drug ApprovalPhase 3Acquisition

12 Dec 2025

·www.fiercepharma.com

GSK gains FDA expansion for Blujepa to treat gonorrhea

GSK has secured an FDA label expansion for its antibiotic Blujepa to treat patients with gonorrhea. In March of this year, the U.S. regulator signed off on Blujepa as a treatment for uncomplicated urinary tract infections. With an increase in the antimicrobial resistance to therapies for gonorrhea, doctors have been left with fewer options to treat the sexually transmitted infection (STI), which strikes more an 80 million annually around the world.Thursday, the FDA addressed the shortfall with a label expansion for GSK’s Blujepa. The U.S. approval brings a new class of antibiotic treatment to gonorrhea for the first time in more than three decades. It also provides an oral option versus the injected therapies currently used to combat the infection.Blujepa already is on the market, as the U.S. regulator endorsed it in March of this year for an array of uncomplicated urinary tract infections.As for the gonorrhea nod, the FDA has cleared its use for those age 12 and older and who weigh at least 45 kg (100 pounds) in cases where standard of care (SOC) is contraindicated or in cases where patients are intolerant or unwilling to use the first line of treatment.Paving the way for the approval was a phase 3 trial which showed Blujepa was noninferior to the SOC combination therapy of intramuscular ceftriaxone plus oral azithromycin. The SOC antibiotics were originally approved by the FDA in 1982 and 1991, respectively. The study also demonstrated the safety and tolerability of the treatment, with mild to moderate gastrointestinal issues reported as the most common adverse reactions.Tyler Evans, M.D., an infectious disease specialist and the CEO of the Wellness Equity Alliance, called the approval a “rare moment of progress in the fight against antibiotic resistance.”“A first-in-class oral treatment for gonorrhea is a major scientific achievement, especially for a pathogen that has outsmarted nearly every drug we have used against it. Expanding treatment options matters, particularly for patients who face barriers to injectable therapy or have limited alternatives,” Evans added. If left untreated or inadequately treated, gonorrhea can lead to infertility and other sexual and reproductive health issues. In 2023, there were more than 600,000 cases of gonorrhea in the U.S., according to the Centers for Disease Control and Prevention (CDC), making it the second-most common STI after chlamydia. There is no vaccine in the U.S. for the prevention of gonorrhea, which is spread by unprotected sex and can affect the genitals, rectum, eyes and throat.Gonorrhea has been recognized by the World Health Organization and the U.S. CDC as a priority pathogen and an urgent public threat. The development of Blujepa was funded in part by the U.S. Department of Health and Human Services, the Administration for Strategic Preparedness and Response and the Biomedical Advanced Research and Development Authority, GSK said. Another oral antibiotic to treat gonorrhea is on the doorstep of approval in the U.S. as Massachusetts company Innoviva Specialty Therapeutics faces a Monday FDA decision date for zoliflodacin. Thursday, the company revealed (PDF) results from a phase 3 trial which showed the noninferiority of zoliflodacin to the ceftriaxone/azithromycin combo.

Phase 3Drug ApprovalClinical ResultVaccineQualified Infectious Disease Product

12 Dec 2025

·firstwordpharma.com

GSK's oral antibiotic Blujepa expands US label to gonorrhoea

With a decision on Innoviva's rival therapy looming next week, US regulators have handed GSK's oral antibiotic Blujepa (gepotidacin) its second approval of the year, extending its reach to uncomplicated urogenital gonorrhoea. Blujepa was first cleared in March for uncomplicated urinary tract infections (see – Spotlight On: GSK swims against the tide to address growing AMR crisis).Health agencies have for years been warning that gonorrhoea is becoming harder to treat, as cases climb past 600,000 annually in the US and resistance squeezes the utility of older antibiotics.New class in 30 yearsBlujepa now becomes the first new class of gonorrhoea treatment in more than three decades, according to Chief Scientific Officer Tony Wood, and offers an oral option to US patients, who currently rely on injectables to treat the sexually transmitted infection.GSK says the triazaacenaphthylene antibiotic targets bacterial DNA replication at a distinct binding site and provides "well-balanced inhibition" of two Type II topoisomerase enzymes, which supports activity against Neisseria gonorrhoeae and most target uropathogens such as Escherichia coli and Staphylococcus saprophyticus, including strains resistant to current antibiotics."The ability of N. gonorrhoeae to develop resistance to currently available options, including standard of care, makes it important to expand the range of effective oral treatments," said Wood in a release Thursday.GSK's priority review filing was supported by data from the roughly 600-patient EAGLE-1 trial, which tested two 3g oral doses of Blujepa against the combination of intramuscular ceftriaxone plus oral azithromycin. Investigators found Blujepa to be non-inferior, with microbiological response at test-of-cure demonstrating success rates of 92.6%, compared to 91.2% in the ceftriaxone plus azithromycin group. Mild-to-moderate gastrointestinal complaints were the most common side effects, and there were no serious drug-related safety issues.Single-dose option on horizonThere soon may be another new treatment option on the market, however. The Lancet published Phase III results this week for Innoviva's investigational single-dose oral therapy zoliflodacin, showing the drug was non-inferior to dual therapy with ceftriaxone plus azithromycin. The 930-patient study, led by the Global Antibiotic Research & Development Partnership, also found comparable safety across urogenital, pharyngeal and rectal infections.The FDA has set a Dec. 15 deadline for its review of the spiropyrimidinetrione antibiotic.

Phase 3Priority ReviewDrug ApprovalQualified Infectious Disease ProductClinical Result

100 Deals associated with Zoliflodacin

External Link

KEGG	Wiki	ATC	Drug Bank
D11726	Zoliflodacin	-	DB12817

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Gonorrhea	United States	Entasis Therapeutics, Inc.	12 Dec 2025

Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03959527 (CTgov)	Phase 3	Gonorrhea	1,011	zoliflodacin (Zoliflodacin)	utilbpqwie = kosfutfgav izjchiupmo (pmdaodshwk, xmwgrpnwsc - spnspknchl) View more	-	26 Jul 2024
				azithromycin+ceftriaxone (Ceftriaxone and Azithromycin Combination)	utilbpqwie = tywsqaqhax izjchiupmo (pmdaodshwk, kqsqwevnml - uahfmkjqcr) View more
NCT03959527 (Corporate Publications) Manual	Phase 3	Gonorrhea	930	zoliflodacin	wfipdtkmsc(skqtbolhtm) = met omchhozvnb (ndncardmpi ) Met View more	Non-inferior	01 Nov 2023
				ceftriaxone+azithromycin
NCT03404167 (CTgov)	Phase 1	Gonorrhea	8	AZD0914	fabdzlhcvo(nxhnslurxz) = gvuwrtahmk gijityhcbr (siggwsosxo, 7129) View more	-	18 Mar 2019
NCT01929629 \| NCT02298920 (Pubmed \| Antimicrob Agents Chemother)	Phase 2	-	100	Zoliflodacin	qwrclyjnpx(oanquxnhva) = delayed (Tmax, 4h) eledtjctms (ogycipezmx ) View more	-	01 Jan 2019
NCT02257918 (Pubmed \| N Engl J Med)	Phase 2	Gonococcal urethritis	179	Zoliflodacin 2g	dvxjakyoss(pmvzqvslsi) = dmdkfbfpjp bsaqvqsuxo (mzhtchinke )	-	08 Nov 2018
				Zoliflodacin 3g	dvxjakyoss(pmvzqvslsi) = coxmnwzdzr bsaqvqsuxo (mzhtchinke )
NCT02257918 (CTgov)	Phase 2	Gonorrhea	180	AZD0914 (AZD0914/ETX0914 2000mg)	fqcwzwbxji = nsigneryna efiwqvvfnh (yxsjnvrdwo, wqjhfgwjgx - hfgdhohesq) View more	-	08 Feb 2017
				ETX0914 (AZD0914/ETX0914 3000mg)	fqcwzwbxji = pwyprfbhzf efiwqvvfnh (yxsjnvrdwo, vvrpdxhqtp - yukmbsgfbg) View more

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