NUZOLVENCE (zoliflodacin)

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). The pharmacokinetic properties of zoliflodacin in healthy subjects are displayed in Table 4.

Table 4Pharmacokinetic Properties of Zoliflodacin in Healthy Subjects Abbreviations: AUC = area under the concentration-time curv...

A total of 930 patients with suspected uncomplicated gonorrhea due to Neisseria gonorrhoeae were randomized in an open-label, active-controlled, multicenter, multinational trial (NCT03959527; Trial 1). Patients were randomized 2:1 to receive a single, oral, 3 g dose of NUZOLVENCE or a combination of a single intramuscular 500 mg dose of ceftriaxone and a single 1 g oral dose of azithromycin. Patients were eligible for enrollment if they were ≥12 years old and ≥35 kg. Patients with confirmed or suspected complicated or disseminated gonorrhea were excluded from the study. The primary analysis po...

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....

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...

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 contrac...

7 DRUG INTERACTIONS 7.1 Effect of Other Drugs on NUZOLVENCE Moderate and Strong CYP3A4 Inducers Concomitant use of moderate or strong inducers of CYP3A4 with NUZOLVENCE is contraindicated [see Contraindications (4) ] . Zoliflodacin is a CYP3A4 substrate. Moderate and strong CYP3A4 inducers are predicted to result in decreased plasma concentrations of zoliflodacin and may reduce NUZOLVENCE efficacy...