Fezolinetant
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From MedlinePlus, U.S. National Library of Medicine
Boxed warning
WARNING: RISKS OF HEPATOTOXICITY Hepatotoxicity has occurred with the use of VEOZAH in the postmarketing setting ( 5.1 ). • Perform hepatic laboratory tests prior to initiation of treatment to evaluate for hepatic function and injury. Do not start VEOZAH if either aminotransferase is ≥ 2 x the upper limit of normal (ULN) or if the total bilirubin is ≥ 2 x ULN for the evaluating laboratory. • Perform follow-up hepatic laboratory testing monthly for the first 3 months, at 6 months, and 9 months of treatment ( 2.1 , 5.1 ).
• Advise patients to discontinue VEOZAH immediately and seek medical attention including hepatic laboratory tests if they experience signs or symptoms that may suggest liver injury (new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain) ( 2.1 , 5.1 ). • Discontinue VEOZAH if transaminase elevations are > 5 x ULN, or if transaminase elevations are > 3 x ULN and the total bilirubin level is > 2 x ULN. • If transaminase elevations > 3 x ULN occur, perform more frequent follow-up hepatic laboratory tests until resolution ( 5.1 ). WARNING: RISKS OF HEPATOTOXICITY See full prescribing information for complete boxed warning.
Hepatotoxicity has occurred with the use of VEOZAH in the postmarketing setting ( 5.1 ). • Perform hepatic laboratory tests prior to initiation of treatment to evaluate for hepatic function and injury. Do not start VEOZAH if either aminotransferase is ≥ 2 x ULN or if the total bilirubin is ≥ 2 x ULN for the evaluating laboratory. • Perform follow-up hepatic laboratory testing monthly for the first 3 months, at 6 months, and 9 months of treatment ( 2.1 , 5.1 ).
• Advise patients to discontinue VEOZAH immediately and seek medical attention including hepatic laboratory tests if they experience signs or symptoms that may suggest liver injury (new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain) ( 2.1 , 5.1 ). • Discontinue VEOZAH if transaminase elevations are > 5 x ULN, or if transaminase elevations are > 3 x ULN and the total bilirubin level is > 2 x ULN. • If transaminase elevations > 3 x ULN occur, perform more frequent follow-up hepatic laboratory tests until resolution ( 5.1 ).
Neurokinin 3 Receptor Antagonist
Dosing in kidney impairment
Renal Impairment VEOZAH is contraindicated in individuals with severe (eGFR 15 to less than 30 mL/min/1.73 m 2 ) renal impairment or end-stage renal disease (eGFR less than 15 mL/min/1.73 m 2 ) [see Clinical Pharmacology] . No dose adjustment of VEOZAH is recommended for individuals with mild (eGFR 60 to less than 90 mL/min/1.73 m 2 ) or moderate (eGFR 30 to less than 60 mL/min/1.73 m 2 ) renal impairment.
Dosing in liver impairment
Hepatic Impairment Child-Pugh Class A or B hepatic impairment increased the exposure of VEOZAH [see Clinical Pharmacology] . VEOZAH has not been studied in individuals with Child-Pugh Class C hepatic impairment. VEOZAH is contraindicated in individuals with cirrhosis [see Clinical Pharmacology] .
Drug interactions
Check fezolinetant against a medication listLabel text (2 paragraphs)
7 DRUG INTERACTIONS
7.1 Effect of Other Drugs on VEOZAH CYP1A2 Inhibitors VEOZAH is a substrate of CYP1A2. Concomitant use of VEOZAH with drugs that are weak, moderate, or strong CYP1A2 inhibitors, increase the plasma C max and AUC of VEOZAH [see Clinical Pharmacology ( 12.3 )] . VEOZAH is contraindicated in individuals using CYP1A2 inhibitors.
Contraindications
4 CONTRAINDICATIONS VEOZAH is contraindicated in women with any of the following conditions: • Known cirrhosis [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.7 ), and Clinical Pharmacology ( 12.3 )] . • Severe renal impairment or end-stage renal disease [see Use in Specific Populations ( 8.6 ) and Clinical Pharmacology ( 12.3 )] . • Concomitant use with CYP1A2 inhibitors [see Drug Interactions ( 7.1 ) and Clinical Pharmacology ( 12.3 )] . • Known cirrhosis ( 4 , 5.1 ) • Severe renal impairment or end-stage renal disease ( 4 , 8.6 ) • Concomitant use with CYP1A2 inhibitors ( 4 , 7.1 )
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary There are no data on VEOZAH use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In embryo-fetal toxicity animal studies with fezolinetant, embryo-lethality occurred at high doses above the human therapeutic dose in rats and rabbits, but no teratogenicity was observed. In the pre- and post-natal development animal study, delayed parturition and embryo-lethality occurred at high doses above the human therapeutic dose in rats.
Additionally, in the male offspring delayed male reproductive maturation was observed, characterized by incomplete preputial separation, which affected male fertility at doses above the human therapeutic dose in rats [see Data ] . In the U.S. general population, the estimated background risk of major birth defects or miscarriage in clinically recognized pregnancies are 2-4% and 15-20%, respectively. Data Animal Data In embryo-fetal development toxicity studies in rats and rabbits, embryo-lethality was noted at the highest doses (128- and 174-fold the human AUC 24 at the human therapeutic dose for rats and rabbits, respectively).
The no observed adverse effect level (NOAEL) for embryo-fetal development was 50 mg/kg/day in rats and 45 mg/kg/day in rabbits (62- and 16‑fold the human AUC 24 at the human therapeutic dose for rats and rabbits, respectively). Fezolinetant showed no effects on fertility and early embryonic development in rats [see Nonclinical Toxicology ( 13.1 )] . In the pre- and post-natal development study in rats, the NOAEL for maternal and fetal toxicity was 30 mg/kg/day (36‑fold the human AUC 24 at the human therapeutic dose) based on delayed parturition and embryo-lethality at 100 mg/kg/day.
The NOAEL for F 1 generation development was determined to be 100 mg/kg/day for females (204-fold the human AUC 24 at the human therapeutic dose) and 10 mg/kg/day for males (11-fold the human AUC 24 at the human therapeutic dose). The F 1 male showed delayed male reproductive maturation, characterized as incomplete balanopreputial separation at time of mating, at doses of greater than or equal to 30 mg/kg/day (36-fold the human AUC 24 at the human therapeutic dose), which affected male fertility [see Nonclinical Toxicology ( 13.1 )] .
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
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