Drug reference

oteseconazole

Antifungal (selective tetrazole CYP51 inhibitor)

START

150 mg PO daily ×3 d, then 150 mg weekly for 11 weeks

TYPICAL MAX

150 mg/day (loading) or 150 mg weekly (maintain)

STOP IF

Hypersensitivity; pregnancy

WATCH

Pregnancy status (very long t½ ~138 d); take with food

CDSCO approvedATC J02AC06

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 2h · absorption
PEAK: 7h · Tmax
t½: 19.7w · t½ ~138 d
DURATION: 1w · weekly

EXCRETION

Mainly faecal; minimal renal

route + CYP

INTERACTIONS

—

none in our sources

PREGNANCY

Contraindicated — embryotoxic/teratogenic in animals; very long half-life.

FDA category + note

Mechanism

Selective inhibitor of fungal CYP51 (lanosterol 14-α-demethylase) with reduced affinity for human CYP enzymes — disrupts ergosterol synthesis with low off-target interactions.

Indications

Prevention of recurrent vulvovaginal candidiasis (RVVC) in non-reproductive-potential adults

Dosing

Adult: RVVC: 150 mg PO once daily on days 1, 2, 3 — then 150 mg PO once weekly for 11 weeks (load + maintain regimen).
Pediatric: Not established.
Renal adjustment: No adjustment for any eGFR.
Hepatic adjustment: No adjustment for any hepatic impairment.
Geriatric: No specific adjustment.
Max dose: 150 mg/day (loading); 150 mg weekly (maintenance)

Pharmacokinetics

Onset

Antifungal effect across weeks (prophylaxis)

Peak effect

~5–10 h (Tmax)

Duration

Long — supports weekly dosing

Half-life

~138 days (extremely long)

Bioavailability

Increased with food

Protein binding

>99%

Metabolism

Minimal hepatic; primarily faecal elimination

Excretion

Mainly faecal; minimal renal

Contraindications

Females of reproductive potential
Pregnancy / breastfeeding
Hypersensitivity

Side effects

Common

HeadacheNausea

Serious

Hypersensitivity reactions (rare)

Pregnancy & lactation

Pregnancy

Contraindicated — embryotoxic/teratogenic in animals; very long half-life.

Lactation

Contraindicated (very long t½).

Drug interactions

Bcrp Substrates

Moderate

Database

BCRP inhibition

Limit rosuvastatin dose; monitor