Dosing & Uses
Dosage Forms & Strengths
capsule
- 150mg
- NOTE: Fluconazole is not supplied in carton
Vulvovaginal Candidiasis
Indicated to reduce incidence of recurrent vulvovaginal candidiasis (RVVC) in females with history of RVVC who are NOT of reproductive potential
Oteseconazole-only regimen
- Day 1: 600 mg PO x 1 dose, THEN
- Day 2: 450 mg PO x 1 dose, THEN
- Beginning on Day 14: 150 mg PO qWeek for 11 weeks (Weeks 2 through 12)
Fluconazole and oteseconazole regimen
- Days 1, 4, and 7: Fluconazole 150 mg PO x 1 dose, THEN
- Days 14 through 20: Oteseconazole 150 mg PO qDay x 7 Days, THEN
- Beginning on Day 28: Oteseconazole 150 mg PO qWeek for 11 weeks (Weeks 4 through 14)
Dosage Modifications
Renal impairment
- Mild or moderate (eGFR 30-89 mL/min): No dosage adjustment necessary
- Severe and end-stage renal disease with or without dialysis (eGFR <29 mL/min) Not recommended
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment necessary
- Moderate or severe (Child-Pugh B or C): Not recommended
Dosing Considerations
Contraindicated in females of reproductive potential and in pregnant and lactating females
Females who are NOT of reproductive potential are defined as: Persons who are biological females who are postmenopausal or have other reasons for permanent infertility (eg, tubal ligation, hysterectomy, salpingo-oophorectomy)
Usage
- May institute antifungal therapy before results of fungal cultures are known
- Once results are available, adjust antifungal therapy accordingly
Premenarchal females: Safety and effectiveness not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (2)
- pitavastatin
oteseconazole will increase the level or effect of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- rimegepant
oteseconazole will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
Monitor Closely (37)
- alpelisib
oteseconazole will increase the level or effect of alpelisib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- atorvastatin
oteseconazole will increase the level or effect of atorvastatin by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- chlorothiazide
oteseconazole will increase the level or effect of chlorothiazide by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- cimetidine
oteseconazole will increase the level or effect of cimetidine by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- daunorubicin
oteseconazole will increase the level or effect of daunorubicin by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- dipyridamole
oteseconazole will increase the level or effect of dipyridamole by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- doxorubicin
oteseconazole will increase the level or effect of doxorubicin by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- ethinylestradiol
oteseconazole will increase the level or effect of ethinylestradiol by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- fluvastatin
oteseconazole will increase the level or effect of fluvastatin by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- glyburide
oteseconazole will increase the level or effect of glyburide by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- imatinib
oteseconazole will increase the level or effect of imatinib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- irinotecan
oteseconazole will increase the level or effect of irinotecan by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- lapatinib
oteseconazole will increase the level or effect of lapatinib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- ledipasvir/sofosbuvir
oteseconazole will increase the level or effect of ledipasvir/sofosbuvir by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- leflunomide
oteseconazole will increase the level or effect of leflunomide by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- lenvatinib
oteseconazole will increase the level or effect of lenvatinib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- methotrexate
oteseconazole will increase the level or effect of methotrexate by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- mitoxantrone
oteseconazole will increase the level or effect of mitoxantrone by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- nitrofurantoin
oteseconazole will increase the level or effect of nitrofurantoin by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- osimertinib
oteseconazole will increase the level or effect of osimertinib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- ozanimod
oteseconazole will increase the level or effect of ozanimod by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- pantoprazole
oteseconazole will increase the level or effect of pantoprazole by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- pazopanib
oteseconazole will increase the level or effect of pazopanib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- riociguat
oteseconazole will increase the level or effect of riociguat by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- selexipag
oteseconazole will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- selumetinib
oteseconazole will increase the level or effect of selumetinib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- sofosbuvir
oteseconazole will increase the level or effect of sofosbuvir by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- sulfasalazine
oteseconazole will increase the level or effect of sulfasalazine by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- talazoparib
oteseconazole will increase the level or effect of talazoparib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- tenofovir AF
oteseconazole will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- tenofovir DF
oteseconazole will increase the level or effect of tenofovir DF by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- topotecan
oteseconazole will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- ubrogepant
oteseconazole will increase the level or effect of ubrogepant by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- velpatasvir
oteseconazole will increase the level or effect of velpatasvir by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- vemurafenib
oteseconazole will increase the level or effect of vemurafenib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- voclosporin
voclosporin, oteseconazole. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Coadministration with drugs associated with nephrotoxicity may increase the risk for acute and/or chronic nephrotoxicity.
- voxilaprevir
oteseconazole will increase the level or effect of voxilaprevir by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
Minor (0)
Adverse Effects
1-10%
Headache (eg, headache, migraine, sinus headache) (7.4%)
Nausea (3.6%)
Dyspepsia (<2%)
Hot flush (<2%)
Dysuria (<2%)
Menorrhagia (eg, genital hemorrhage, menorrhagia, menometrorrhagia, uterine hemorrhage, vaginal hemorrhage) (<2%)
Metrorrhagia (<2%)
Vulvovaginal irritation (eg, vulvovaginal burning sensation, vulvovaginal discomfort, vulvovaginal pain) (<2%)
Elevated serum creatine phosphokinase ≥10x ULN (1.9%)
<1%
Allergic dermatitis (<0.2%)
Warnings
Contraindications
Females of reproductive potential
Pregnant and lactating females
Hypersensitivity to oteseconazole
Cautions
Based on animal studies, fetal harm may occur (see Pregnancy & Lactation)
Drug interaction overview
- Inhibitor of breast cancer resistance protein (BCRP)
-
BCRP substrates
- Use lowest possible starting dose of BCRP substrate, or consider reducing BCRP substrate dose; monitor adverse reactions
- Oteseconazole may increase effects and toxicities of BCRP substrates
Pregnancy & Lactation
Pregnancy
Contraindicated in females of reproductive potential and in pregnant females
Drug exposure window is ~690 days (based on 5x the half-life of oteseconazole) to prevent any risks of embryofetal toxicities
Animal data
- Ocular abnormalities (eg, cataracts, opacities, exophthalmos/buphthalmos, optic nerve/retinal atrophy, lens degeneration, hemorrhage) observed in rat offspring from Gestation Day 6 through Lactation Day 20 at doses 3.5x the recommended human dose
- Data are insufficient to exclude any potential risk of cataracts or other eye abnormalities in human infants
Lactation
Contraindicated in lactating females
There are no data on presence of oteseconazole in human or animal milk or its effects on milk production
There were no reported adverse effects in breastfed infants following maternal exposure to oteseconazole during lactation
Owing to limited duration of follow-up of oteseconazole-exposed infants during postnatal period, no conclusions can be drawn from data
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Azole metalloenzyme inhibitor targets fungal sterol 14-alpha demethylase (CYP51) Inhibition of CYP51 results in accumulation of 14-methylated sterols, which may be toxic to fungi
Active against most isolates of following microorganisms associated with RVVC:
- Candida albicans
- Candida glabrata
- Candida krusei
- Candida parapsilosis
- Candida tropicalis
- Candida lusitaniae
- Candida dubliniensis
- Note: Clinical significance unknown
Absorption
Peak plasma concentration: 2.8 mcg/mL
Minimum plasma concentration: 2.5 mcg/mL
Peak plasma time: 5-10 hr
AUC: 64.2 mcg·hr/mL
Effect of food
- High-fat, high-calorie meal (800-100 calories; 50% fat): Increased peak plasma concentration by 45% and AUC by 35%
- Low-fat, low-calorie meal: No significant difference
Distribution
Vd: 423 L
Protein bound: 99.5-99.7%
Metabolism
No significant metabolism
Elimination
Half-life: 138 days
Excretion: 56% (feces vial biliary excretion); 26% (urine)
Administration
Oral Administration
Administer with food
Swallow capsule whole; do NOT chew, crush, dissolve, or open
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
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