Generic
Oteseconazole
6 brands available in the market
At a glance
Oteseconazole is an antifungal drug used to reduce the incidence of recurrent vulvovaginal candidiasis (RVVC). It inhibits CYP51 enzyme to disrupt fungal cell membrane integrity.
Description
Oteseconazole is an azole metalloenzyme inhibitor targeting fungal sterol 14α demethylase (CYP51), an enzyme that catalyzes an early step in the biosynthetic pathway of ergosterol, required for fungal cell membrane formation and integrity. Inhibition of CYP51 results in accumulation of 14-methylated sterols, some of which are toxic to fungi.
Indications
- Reduction of incidence of recurrent vulvovaginal candidiasis (RVVC) in females not of reproductive potential
Therapeutic class
Other Antifungal Preparations
Pharmacological class
Azole Antifungal
Pharmacology
Oteseconazole inhibits CYP51 (14α demethylase) to prevent ergosterol synthesis required for fungal cell membrane integrity, resulting in accumulation of toxic 14-methylated sterols and fungal cell death.
Mechanism of action
Reduces incidence of RVVC by disrupting fungal cell membrane integrity.
Dosage
Oteseconazole-only Regimen:
- Day 1: 600 mg (single dose)
- Day 2: 450 mg (single dose)
- Starting Day 14: 150 mg once weekly for 11 weeks
Fluconazole/Oteseconazole Regimen:
- Days 1, 4 & 7: Fluconazole 150 mg
- Days 14-20: Oteseconazole 150 mg once daily for 7 days
- Starting Day 28: 150 mg once weekly for 11 weeks
Administration
- Take with food
- Swallow capsule whole; do not chew, crush, dissolve or open
Missed dose
If you miss a dose, take at next scheduled time; do not take additional dose.
Side effects
Common Side Effects (>2%):
- Headache
- Nausea
Precautions & warnings
- Contraindicated in females of reproductive potential (embryo-fetal toxicity)
- Contraindicated in pregnant and lactating women
- Drug exposure window of approximately 690 days (5 times half-life) limits mitigation of embryo-fetal toxicity risks
Contraindications
- Females of reproductive potential
- Pregnant and lactating women
- Hypersensitivity
Drug interactions
- Concomitant use with BCRP substrates may increase substrate exposure; use lowest possible dose or reduce dose
Food interactions
Take with food for better absorption.
Use in pregnancy
Use in Pregnancy: Oteseconazole is highly unsafe during pregnancy; definite evidence of severe fetal harm. Completely contraindicated.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Oteseconazole is contraindicated during breastfeeding; contraindicated in females of reproductive potential.
Pediatric use
Contraindicated in females of reproductive potential (includes pediatric).
Geriatric use
Insufficient numbers of patients 65 years and older included.
Renal / hepatic impairment
Renal Impairment: No dosage adjustment recommended in mild to moderate renal impairment.
Hepatic Impairment: No dosage adjustment recommended in mild hepatic impairment (Child-Pugh A).
Overdose effects
Limited information on overdose; symptomatic treatment.
Storage conditions
Store at 20-25°C; protect from light when removed from outer carton; keep out of reach of children.
Chemical structure
Oteseconazole