Dosing & Uses
Dosage Forms & Strengths
tablet
- 150mg
Vulvovaginal candidiasis
Treatment
- Indicated for treatment of adult and postmenarchal pediatric females with vulvovaginal candidiasis (VVC)
- 300 mg PO q12hr x 1 day
- Total treatment dosage: 600 mg
Reduction in incidence of recurrent vulvovaginal candidiasis
- Indicated for reducing the incidence of recurrent vulvovaginal candidiasis (RVVC) in adult and postmenarchal pediatric females
- 300 mg PO q12hr x 1 day; repeat monthly for 6 months
Dosage Modifications
Coadministration with CYP3A4 inhibitors
- Mild or moderate: No dosage adjustment necessary
- Strong: Reduce dose of ibrexafungerp to 150 mg PO q12hr
Coadministration with CYP3A4 inducers
- Strong or moderate: Avoid coadministration
Hepatic impairment
- Mild-moderate (Child-Pugh class A-B): No dosage adjustment recommended
- Severe (Child-Pugh Class C): Not studied
Dosing Considerations
Prior to initiation, verify pregnancy status in females of reproductive potential
Dosage Forms & Strengths
tablet
- 150mg
Vulvovaginal candidiasis
Premenarchal patients: Safety and efficacy not established
Treatment
- Indicated for treatment of adult and postmenarchal pediatric females with vulvovaginal candidiasis (VVC)
-
Postmenarchal patients
- 300 mg PO q12hr x 1 day
- Total treatment dosage: 600 mg
Reduction in incidence of recurrent vulvovaginal candidiasis
- Indicated for reducing the incidence of recurrent vulvovaginal candidiasis (RVVC) in adult and postmenarchal pediatric females
-
Postmenarchal patients
- 300 mg PO q12hr x 1 day; repeat monthly for 6 months
Dosage Modifications
Coadministration with CYP3A4 inhibitors
- Mild or moderate: No dosage adjustment necessary
- Strong: Reduce dose of ibrexafungerp to 150 mg PO q12hr
Coadministration with CYP3A4 inducers
- Strong or moderate: Avoid coadministration
Hepatic impairment
- Mild-moderate (Child-Pugh class A-B): No dosage adjustment recommended
- Severe (Child-Pugh Class C): Not studied
Dosing Considerations
- Prior to initiation, verify pregnancy status in females of reproductive potential
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (4)
- elacestrant
ibrexafungerp will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mobocertinib
ibrexafungerp will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- omaveloxolone
ibrexafungerp will increase the level or effect of omaveloxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unavoidable, reduce omaveloxolone dose to 100 mg/day. Closely monitor for adverse effects. If adverse effects emerge, further reduce to 50 mg/day.
- pacritinib
ibrexafungerp will increase the level or effect of pacritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
Monitor Closely (10)
- atogepant
ibrexafungerp will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- daridorexant
ibrexafungerp will increase the level or effect of daridorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Daridorexant dose should not exceed 25 mg per night when coadministered with moderate CYP3A4 inhibitors.
- finerenone
ibrexafungerp will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or moderate CYP3A4 inhibitors. Adjust finererone dosage as needed.
- isavuconazonium sulfate
ibrexafungerp will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lumateperone
ibrexafungerp will increase the level or effect of lumateperone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce lumateperone dose to 21 mg/day if coadministered with moderate CYP3A4 inhibitors.
- mavacamten
ibrexafungerp will increase the level or effect of mavacamten by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Inititiation of moderate CYP3A4 inhibitors may require decreased mavacamten dose.
- sparsentan
ibrexafungerp will increase the level or effect of sparsentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No dosage adjustment needed. Monitor blood pressure, serum potassium, edema, and kidney function regularly if sparsentan is coadministered with moderate CYP3A4 inhibitors.
- vardenafil
ibrexafungerp will increase the level or effect of vardenafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Vardenafil dose may need to be reduced if coadministered with moderate or strong CYP3A4 inhibitors
- voclosporin
voclosporin, ibrexafungerp. 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.
- zanubrutinib
ibrexafungerp will increase the level or effect of zanubrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce zanubrutinib (a CYP3A4 substrate) to 80 mg PO BID to when coadministered with a moderate CYP3A4 inhibitor. Interrupt dose as recommended for adverse reactions. After discontinuing the CYP3A4 inhibitor, resume previous dose of zanubrutinib.
Minor (0)
Adverse Effects
>10%
-
VVC
- Diarrhea (16.7%)
- Nausea (11.9%)
- Abdominal pain (11.4%)
-
RVVC
- Headache (17.6%)
1-10%
-
VVC
- Dizziness (3.3%)
- Vomiting (2%)
- Dysmenorrhea (2%)
- Flatulence (2%)
- Back pain (2%)
- Elevated transaminases (2%)
- Vaginal bleeding (2%)
- Rash/hypersensitivity reaction (2%)
-
RVVC
- Abdominal pain (10%)
- Diarrhea (7.7%)
- Nausea (5.4%)
- Urinary tract infection (3.8%)
- Fatigue (3.1%)
Warnings
Black Box Warnings
Risk of embryofetal toxicity
- Contraindicated in pregnancy
- May cause fetal harm based on results from animal studies
- For females of reproductive potential, ensure patient is not pregnant before initiating
- Reassess pregnancy status before each dose when used monthly to reduce incidence of recurrent vulvovaginal candidiasis
- Advise females of reproductive potential to use effective contraception during treatment and for 4 days after final dose
Contraindications
Pregnancy
Hypersensitivity to ibrexafungerp
Cautions
Contraindicated to pregnancy; based on animal data, fetal harm may occur
Drug interaction overview
- CYP3A4 substrate
- Inhibitor of CYP3A4, P-gp and OATP1B3 transporter
-
Strong CYP3A4 inhibitors
- Reduce ibrexafungerp dose
- Strong CYP3A inhibitors increase the exposure of ibrexafungerp
-
Strong and moderate CYP3A inducers
- Avoid coadministration
- Strong and moderate CYP3A inducers may significantly reduce the exposure of ibrexafungerp
Pregnancy & Lactation
Pregnancy
Contraindicated
Insufficient data are available on use in pregnant females on any drug-associated risks of major birth defects, miscarriage, or other adverse maternal or fetal outcomes
For females of reproductive potential, verify that the patient is not pregnant prior to initiating treatment; reassessment of pregnancy status prior to each dose recommended when used monthly for 6 months for reduction in incidence of RVVC
If inadvertently administered during pregnancy or if pregnancy is detected within 4 days after receiving therapy, pregnant females exposed and healthcare providers should report pregnancies to SCYNEXIS, Inc. at 1-888-982-SCYX (7299)
Contraception
- Females of reproductive potential: Use effective contraception during treatment and for 4 days after final dose
- For reduction in the incidence of RVVC, advise females of reproductive potential to use effective contraception throughout 6-month treatment period and, for 4 days after last dose
Animal data
- In pregnant rabbits, oral ibrexafungerp administered during organogenesis was associated with rare malformations including absent forelimb(s), absent hindpaw, absent ear pinna, and thoracogastroschisis at dose exposures greater or equal to ~5x the human exposure at the recommended human dose (RHD)
- Oral ibrexafungerp administered to pregnant rats during organogenesis was not associated with fetal toxicity or increased fetal malformations at a dose exposure ~5x the human exposure at the RHD
Lactation
No data are available on drug presence in either human or animal milk, effects on breastfed infants, or effects on milk production
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
Triterpenoid antifungal agent
Inhibits glucan synthase, an enzyme involved in the formation of 1,3-beta-D-glucan, an essential component of the fungal cell wall
Concentration-dependent fungicidal activity against candidal species as measured by time-kill studies
Shown to be active against most isolates of the following microorganisms both in vitro and in clinical infections:
- Candida auris
- Candida dubliniensis
- Candida glabrata
- Candida guilliermondii
- Candida keyfr
- Candida krusei
- Candida lusitaniae
- Candida parapsilosis
- Candida tropicalis
Absorption
- Peak plasma time: 4-6 hr
-
Peak plasma concentration
- Fasted: 435 ng/mL
- Fed: 629 ng/mL
-
AUC
- Fasted: 6832 ng·hr/mL
- Fed: 9867 ng·hr/mL
Effect of food
- High-fat meal (800-1000 calories; 50% fat): Ibrexafungerp peak plasma concentration increased 32% and the AUC increased 38% compared with fasted conditions; not considered clinically significant
Distribution
- Vd (steady-state): ~6000 L
- Protein bound: >99%
Metabolism
Primarily metabolized by hydroxylation by CYP3A4
Followed by glucuronidation and sulfation of a hydroxylated inactive metabolite
Elimination
Half-life: 20 hr
Excretion: Feces (90%; 51% unchanged); urine (1%)
Administration
Oral Administration
Take with or without food
Storage
Tablets: Store at 20-25ºC (68-77ºF); excursion permitted to 15-30ºC (59-86ºF)
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Formulary
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