oteseconazole

Oteseconazole is a systemic antifungal medication used to treat recurrent vulvovaginal candidiasis in women without reproductive potential.

Candidiasis is a type of yeast infection caused by Candida species of fungi. Oteseconazole may be used as monotherapy or in combination with fluconazole, another systemic antifungal medication.

Oteseconazole is a synthetic azole metalloenzyme inhibitor that works by inhibiting the activity of a fungal enzyme essential for fungal survival and growth. Oteseconazole selectively inhibits fungal sterol 14-alpha demethylase (CYP51), an enzyme essential for the formation and integrity of the fungal cell membrane. The inhibition of CYP51 results in the accumulation of 14-alpha methylated sterols which are toxic to fungi.

Oteseconazole is active against the following Candida species of fungi associated with recurrent vulvovaginal candidiasis:

• Candida albicans
• Candida glabrata
• Candida krusei
• Candida parapsilosis
• Candida tropicalis
• Candida lusitaniae
• Candida dubliniensis

• Do not use in patients with known hypersensitivity to oteseconazole or any of its components.
• Do not use in women of reproductive potential or women who are pregnant or breastfeeding.

Common side effects of oteseconazole include:

• Headache
• Sinus headache
• Migraine
• Nausea
• Indigestion (dyspepsia)
• Hot flush
• Painful urination (dysuria)
• Increased creatine phosphokinase (CPK) in blood
• Allergic dermatitis
• Abnormally heavy menstrual bleeding (menorrhagia)
• Irregular bleeding between periods (metrorrhagia)
• Menometrorrhagia
• Vaginal hemorrhage
• Uterine hemorrhage
• Vulvovaginal discomfort, irritation, pain, and burning sensation

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

• Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
• Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
• Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
• Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Capsule

• 150 mg
• NOTE: Fluconazole is not supplied in carton

Adult:

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/minute): 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 (e.g., 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

Administration

• Administer with food
• Swallow capsule whole; do NOT chew, crush, dissolve, or open

Pediatric:

• Premenarchal females: Safety and effectiveness not established

• There is insufficient information about overdose of oteseconazole. Overdose may increase the risk for severe adverse effects.
• Oteseconazole overdose may be treated with symptomatic and supportive care.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

• Oteseconazole has no severe interactions with other drugs.
• Oteseconazole has serious interactions with the following drugs:
  • pitavastatin
  • rimegepant
• Oteseconazole has moderate interactions with at least 37 other drugs.
• Oteseconazole has no minor interactions with other drugs.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• Do not use oteseconazole in women who are pregnant or have reproductive potential. Animal studies show evidence of embryo-fetal toxicity from maternal use of oteseconazole.
• Do not use oteseconazole in nursing mothers. There is insufficient information to establish safety of oteseconazole use in nursing mothers, its effects on milk production and on breastfed infants.

• Take oteseconazole exactly as prescribed.
• Store oteseconazole carefully out of reach of children.
• In case of accidental overdose, seek medical help immediately or contact Poison Control.