Oteseconazole is indicated to reduce the recurrence of vulvovaginal candidiasis (RVVC) in females with a history of RVVC who are not of reproductive potential. If fungal culture samples are taken before starting therapy, treatment may be initiated before the results are available. Once culture results are obtained, therapy should be adjusted accordingly.

Oteseconazole is an antifungal agent. Its exposure-response relationship and pharmacodynamic time course are not fully established. It belongs to the azole class and acts as a metalloenzyme inhibitor targeting fungal sterol 14α-demethylase (CYP51), which plays a key role in ergosterol synthesis. Ergosterol is essential for fungal cell membrane structure and function. Inhibition of CYP51 leads to accumulation of toxic 14-methylated sterols, which damages fungal cells. Due to the presence of a tetrazole metal-binding group, oteseconazole has reduced affinity for human CYP enzymes, improving selectivity.

There are two recommended Oteseconazole dosage regimens:

For the Oteseconazole-only dosage regimen:

• On Day 1: Administer Oteseconazole 600 mg (as a single dose), then
• On Day 2: Administer Oteseconazole 450 mg (as a single dose), then
• Beginning on Day 14: Administer Oteseconazole 150 mg once a week (every 7 days) for 11 weeks (Weeks 2 through 12).

For the Fluconazole/Oteseconazole dosage regimen, prescribe Fluconazole and:

• On Day 1, Day 4, and Day 7: Administer fluconazole 150 mg orally, then
• On Days 14 through 20: Administer Oteseconazole 150 mg once daily for 7 days, then
• Beginning on Day 28: Administer Oteseconazole 150 mg once a week (every 7 days) for 11 weeks (Weeks 4 through 14).

Administer Oteseconazole orally with food. Swallow the capsules whole. Do not chew, crush, dissolve, or open the capsules.

Concomitant use of Oteseconazole with BCRP (Breast Cancer Resistance Protein) substrate drugs may increase their exposure, which can raise the risk of adverse effects. In such cases, it is recommended to start with the lowest possible dose of the BCRP substrate, or consider dose reduction with careful monitoring for side effects.

Oteseconazole is contraindicated in

• females of reproductive potential,
• pregnant women, lactating women,
• and patients with known hypersensitivity to the drug.

The most commonly reported side effects (more than 2%) include headache and nausea.

Oteseconazole is contraindicated during pregnancy, lactation, and in females of reproductive potential. Animal studies suggest potential fetal harm when used in pregnancy.

The drug has a very long elimination window (approximately 690 days), which limits the ability to fully avoid fetal exposure risks.

It is also contraindicated during breastfeeding. There is no confirmed data on its presence in human or animal milk or its effect on milk production. Although no adverse effects were reported in limited follow-up of exposed infants, the data are insufficient to draw conclusions.

Embryo-Fetal Toxicity: Oteseconazole is contraindicated in pregnancy, lactation, and females of reproductive potential due to potential fetal risk. Animal studies showed fetal toxicity including eye abnormalities such as cataracts, retinal damage, optic nerve atrophy, and hemorrhage. These effects occurred at exposures slightly above clinical levels. The long drug elimination period (~690 days) increases concern for prolonged fetal exposure risk.

Pediatric Use: Contraindicated in females of reproductive potential. May cause fetal harm or risk to breastfed infants based on animal data.

Geriatric Use: Limited data; insufficient evidence to determine differences in response in patients aged 65 years and older.

Renal Impairment: No dose adjustment required in mild to moderate renal impairment.

Hepatic Impairment: No dose adjustment required in mild hepatic impairment (Child-Pugh A).

Other antifungal preparations.

Store at 20°C to 25°C. Protect from light after removing from the outer carton. Keep out of reach of children.