Ibrexafungerp

Identification

Summary

Ibrexafungerp is a triterpene antifungal indicated in the treatment of vulvovaginal candidiasis in post-menarchal patients.

Brand Names
Brexafemme
Generic Name
Ibrexafungerp
DrugBank Accession Number
DB12471
Background

Ibrexafungerp, also known as SCY-078 or MK-3118, is a novel enfumafungin derivative oral triterpene antifungal approved for the treatment of vulvovaginal candidiasis (VVC), also known as a vaginal yeast infection.1,9 It was developed out of a need to treat fungal infections that may have become resistant to echinocandins or azole antifungals.1 Ibrexafungerp is orally bioavailable compared to the echinocandins caspofungin, micafungin, and anidulafungin; which can only be administered parenterally.1,2 Similar to echinocandins, ibrexafungerp targets the fungal β-1,3-glucan synthase, which is not present in humans, limiting the chance of renal or hepatic toxicity.6,9

Ibrexafungerp was granted FDA approval on 1 June 2021.9

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 730.051
Monoisotopic: 729.519305657
Chemical Formula
C44H67N5O4
Synonyms
  • Ibrexafungerp
External IDs
  • MK-3118
  • SCY-078
  • WHO 10597

Pharmacology

Indication

Ibrexafungerp is indicated in the treatment of vulvovaginal candidiasis in post-menarchal patients.9

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Ibrexafungerp is an enfumafungin derivative oral triterpene antifungal approved for the treatment of vulvovaginal candidiasis.1,9 It has a moderate duration of action, as it is taken twice daily, and a wide therapeutic index as patients took more than the recommended dose in clinical trials without severe adverse effects.9 Patients should be counselled regarding the risk of fetal toxicity.9

Mechanism of action

β-1,3-glucan synthase is composed of a catalytic subunit, FKS1 or FKS2, and a GTP-binding regulatory subunit, Rho1.5,6 This synthase is involved in the synthesis of β-1,3-glucan, a fungal cell wall component.6

Ibrexafungerp acts similarly to the echinocandin antifungals, by inhibiting the synthesis of β-1,3-glucan synthase.1,9 While echinocandins bind to the FKS1 domain of β-1,3-glucan synthase, enfumafungin and its derivatives bind at an alternate site which allows them to maintain their activity against fungal infections that are resistant to echinocandins.3,4

Ibrexafungerp has been shown in animal studies to distribute well to vaginal tissue, making it a favourable treatment for vulvovaginal candidiasis.4

TargetActionsOrganism
U1,3-beta-glucan synthase component GSC2
inhibitor
Baker's yeast
UGTP-binding protein RHO1
inhibitor
Baker's yeast
Absorption

Ibrexafungerp given at a dose of 300 mg twice daily reaches a Cmax of 435 ng/mL, with a Tmax of 4-6 hours, and an AUC0-24 of 6832 h*ng/mL.7,9

Volume of distribution

The volume of distribution at steady state is approximately 600 L.9

Protein binding

Ibrexafungerp is 99.5-99.8% protein bound in plasma, mainly to albumin.1,9

Metabolism

Ibrexafungerp is hydroxylated by CYP3A4 before glucuronide or sulfate conjugation of the hydroxyl group before elimination.8,9

Route of elimination

90% of a radiolabelled oral dose of ibrexafungerp is recovered in the feces, with 51% as the unchanged parent drug.9 1% of a radiolabelled oral dose is recovered in the urine.9

Half-life

The elimination half life of ibrexafungerp is approximately 20 hours.7,9

Clearance

Clearance values of 53.6 L/h and 56.1 L/h have been reported.7

Adverse Effects
Adverseeffects
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Toxicity

Data regarding overdoses of ibrexafungerp are not readily available, however patients did take higher than recommended doses in clinical trials without significant adverse effects.9 Patients experiencing an overdose of ibrexafungerp may experience and increased risk and severity of adverse effects. Patients should be treated with symptomatic and supportive measures.9

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Ibrexafungerp can be increased when it is combined with Abametapir.
AbirateroneThe metabolism of Ibrexafungerp can be decreased when combined with Abiraterone.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be increased when used in combination with Ibrexafungerp.
AmiodaroneThe serum concentration of Ibrexafungerp can be increased when it is combined with Amiodarone.
AmprenavirThe serum concentration of Ibrexafungerp can be increased when it is combined with Amprenavir.
ApalutamideThe serum concentration of Ibrexafungerp can be decreased when it is combined with Apalutamide.
AprepitantThe metabolism of Ibrexafungerp can be decreased when combined with Aprepitant.
AtazanavirThe serum concentration of Ibrexafungerp can be increased when it is combined with Atazanavir.
BerotralstatThe metabolism of Ibrexafungerp can be decreased when combined with Berotralstat.
BexaroteneThe serum concentration of Ibrexafungerp can be decreased when it is combined with Bexarotene.
Interactions
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Food Interactions
  • Take with or without food. A high fat meal increases the AUC by 38% and Cmax by 32%, which is not considered significant.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Ibrexafungerp citrateM4NU2SDX3E1965291-08-0WKIRTJACGBEXBZ-FQGZCCSZSA-N
Ibrexafungerp phosphate76HJ8T68WO1965291-14-8OAKUEXTYOMFKTF-FQGZCCSZSA-N
International/Other Brands
Brexafemme (Scynexis, Inc.)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BrexafemmeTablet, film coated150 mg/1OralScynexis, Inc.2021-07-01Not applicableUS flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as hydroxysteroids. These are compounds containing an steroid backbone, with at least one hydrogen substituted by a hydroxyl group.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
Hydroxysteroids
Alternative Parents
Sesquiterpenoids / Naphthopyrans / Pyridyl-1,2,4-triazoles / Naphthalenes / Pyrans / Oxanes / Triazoles / Heteroaromatic compounds / Amino acids / Monocarboxylic acids and derivatives
show 8 more
Substituents
1,2,4-triazole / 15-hydroxysteroid / Amine / Amino acid / Amino acid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Azole / Carbonyl group / Carboxylic acid
show 25 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
  • Candida albicans and other yeasts

Chemical Identifiers

UNII
A92JFM5XNU
CAS number
1207753-03-4
InChI Key
BODYFEUFKHPRCK-ZCZMVWJSSA-N
InChI
InChI=1S/C44H67N5O4/c1-27(2)28(3)39(7)18-19-41(9)30-12-13-33-40(8)23-52-25-44(33,31(30)14-17-42(41,10)34(39)37(50)51)22-32(35(40)53-24-43(11,45)38(4,5)6)49-36(47-26-48-49)29-15-20-46-21-16-29/h14-16,20-21,26-28,30,32-35H,12-13,17-19,22-25,45H2,1-11H3,(H,50,51)/t28-,30+,32-,33+,34-,35+,39-,40-,41-,42+,43+,44+/m1/s1
IUPAC Name
(1R,5S,6R,7R,10R,11R,14R,15S,20R,21R)-21-[(2R)-2-amino-2,3,3-trimethylbutoxy]-5,7,10,15-tetramethyl-7-[(2R)-3-methylbutan-2-yl]-20-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-17-oxapentacyclo[13.3.3.0^{1,14}.0^{2,11}.0^{5,10}]henicos-2-ene-6-carboxylic acid
SMILES
[H][C@]12CC[C@@]3([H])[C@@]4(C)COC[C@@]3(C[C@H]([C@@H]4OC[C@](C)(N)C(C)(C)C)N3N=CN=C3C3=CC=NC=C3)C1=CC[C@@]1(C)[C@H](C(O)=O)[C@](C)(CC[C@]21C)[C@H](C)C(C)C

References

General References
  1. Wring SA, Randolph R, Park S, Abruzzo G, Chen Q, Flattery A, Garrett G, Peel M, Outcalt R, Powell K, Trucksis M, Angulo D, Borroto-Esoda K: Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis. Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: AAC.02068-16. doi: 10.1128/AAC.02068-16. Print 2017 Apr. [Article]
  2. Hector RF, Bierer DE: New beta-glucan inhibitors as antifungal drugs. Expert Opin Ther Pat. 2011 Oct;21(10):1597-610. doi: 10.1517/13543776.2011.603899. Epub 2011 Jul 25. [Article]
  3. Kuhnert E, Li Y, Lan N, Yue Q, Chen L, Cox RJ, An Z, Yokoyama K, Bills GF: Enfumafungin synthase represents a novel lineage of fungal triterpene cyclases. Environ Microbiol. 2018 Sep;20(9):3325-3342. doi: 10.1111/1462-2920.14333. Epub 2018 Sep 13. [Article]
  4. Larkin EL, Long L, Isham N, Borroto-Esoda K, Barat S, Angulo D, Wring S, Ghannoum M: A Novel 1,3-Beta-d-Glucan Inhibitor, Ibrexafungerp (Formerly SCY-078), Shows Potent Activity in the Lower pH Environment of Vulvovaginitis. Antimicrob Agents Chemother. 2019 Apr 25;63(5). pii: AAC.02611-18. doi: 10.1128/AAC.02611-18. Print 2019 May. [Article]
  5. Ha YS, Covert SF, Momany M: FsFKS1, the 1,3-beta-glucan synthase from the caspofungin-resistant fungus Fusarium solani. Eukaryot Cell. 2006 Jul;5(7):1036-42. doi: 10.1128/EC.00030-06. [Article]
  6. Perlin DS: Mechanisms of echinocandin antifungal drug resistance. Ann N Y Acad Sci. 2015 Sep;1354:1-11. doi: 10.1111/nyas.12831. Epub 2015 Jul 17. [Article]
  7. Wring S, Murphy G, Atiee G, Corr C, Hyman M, Willett M, Angulo D: Clinical Pharmacokinetics and Drug-Drug Interaction Potential for Coadministered SCY-078, an Oral Fungicidal Glucan Synthase Inhibitor, and Tacrolimus. Clin Pharmacol Drug Dev. 2019 Jan;8(1):60-69. doi: 10.1002/cpdd.588. Epub 2018 Jun 27. [Article]
  8. Ghannoum M, Arendrup MC, Chaturvedi VP, Lockhart SR, McCormick TS, Chaturvedi S, Berkow EL, Juneja D, Tarai B, Azie N, Angulo D, Walsh TJ: Ibrexafungerp: A Novel Oral Triterpenoid Antifungal in Development for the Treatment of Candida auris Infections. Antibiotics (Basel). 2020 Aug 25;9(9). pii: antibiotics9090539. doi: 10.3390/antibiotics9090539. [Article]
  9. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]
PubChem Compound
46871657
PubChem Substance
347828709
ChemSpider
64873335
RxNav
2560213
ChEMBL
CHEMBL4297513
Wikipedia
Ibrexafungerp

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingPreventionRecurrent Vulvovaginal Candidiasis1
3CompletedTreatmentCandida Vulvovaginitis2
3RecruitingTreatmentAllergic Bronchopulmonary Aspergillosis / Aspergillosis; Pulmonary, Invasive (Etiology) / Blastomycosis / Candidiasis, Invasive / Chronic Pulmonary Aspergillosis / Coccidioidomycosis / Histoplasmosis / Mucocutaneous candida infection / Other Emerging Fungi / Recurrent Vulvovaginal Candidiasis1
3RecruitingTreatmentCandidemia / Candidiasis, Invasive1
2CompletedTreatmentCandida Vulvovaginitis1
2CompletedTreatmentCandidemia / Candidiasis, Invasive / Mycoses1
2CompletedTreatmentVulvovaginal Candidiasis1
2RecruitingTreatmentAspergillosis; Pulmonary, Invasive (Etiology)1
1CompletedOtherInfections, Fungal1
1CompletedOtherPharmacokinetics2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral150 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8188085No2012-05-292030-08-28US flag
US10370406No2019-08-062035-01-19US flag
US10174074No2019-01-082035-01-19US flag
US10927142No2021-02-232035-01-19US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
pKa2.4, 5.5, 9.0Wring, et al., 2017
Predicted Properties
PropertyValueSource
Water Solubility0.000346 mg/mLALOGPS
logP3.28ALOGPS
logP4.9ChemAxon
logS-6.3ALOGPS
pKa (Strongest Acidic)4.39ChemAxon
pKa (Strongest Basic)9.75ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area125.38 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity230.85 m3·mol-1ChemAxon
Polarizability84.64 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets2
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Kind
Protein
Organism
Baker's yeast
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Possible binding site
General Function
Alternate catalytic subunit of the 1,3-beta-glucan synthase (GS). Synthesizes 1,3-beta-glucan, a major structural component of the yeast cell wall. Required for spore wall assembly. Negative regulation of activity by SMK1 is important for spore wall deposition. Activity is positively regulated by RHO1.
Specific Function
1,3-beta-d-glucan synthase activity
Gene Name
GSC2
Uniprot ID
P40989
Uniprot Name
1,3-beta-glucan synthase component GSC2
Molecular Weight
216987.85 Da
References
  1. Pfaller MA, Messer SA, Motyl MR, Jones RN, Castanheira M: In vitro activity of a new oral glucan synthase inhibitor (MK-3118) tested against Aspergillus spp. by CLSI and EUCAST broth microdilution methods. Antimicrob Agents Chemother. 2013 Feb;57(2):1065-8. doi: 10.1128/AAC.01588-12. Epub 2012 Dec 10. [Article]
  2. Lepak AJ, Marchillo K, Andes DR: Pharmacodynamic target evaluation of a novel oral glucan synthase inhibitor, SCY-078 (MK-3118), using an in vivo murine invasive candidiasis model. Antimicrob Agents Chemother. 2015 Feb;59(2):1265-72. doi: 10.1128/AAC.04445-14. Epub 2014 Dec 15. [Article]
  3. Pfaller MA, Messer SA, Motyl MR, Jones RN, Castanheira M: Activity of MK-3118, a new oral glucan synthase inhibitor, tested against Candida spp. by two international methods (CLSI and EUCAST). J Antimicrob Chemother. 2013 Apr;68(4):858-63. doi: 10.1093/jac/dks466. Epub 2012 Nov 28. [Article]
  4. Pfaller MA, Messer SA, Rhomberg PR, Borroto-Esoda K, Castanheira M: Differential Activity of the Oral Glucan Synthase Inhibitor SCY-078 against Wild-Type and Echinocandin-Resistant Strains of Candida Species. Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: AAC.00161-17. doi: 10.1128/AAC.00161-17. Print 2017 Aug. [Article]
Kind
Protein
Organism
Baker's yeast
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Possible binding site
General Function
Acts as a central regulator in the cell wall integrity signaling pathway, which is regulated by the cell cycle and in response to various types of cell wall stress. Integrates signals from different cell surface sensors, and activates a set of effectors, regulating processes including beta-glucan synthesis at the site of wall remodeling, gene expression related to cell wall biogenesis, organization of the actin cytoskeleton, and protein- and secretory vesicle-targeting to the growth site. Activates the protein kinase C (PKC1) MAP kinase cascade, the beta-1,3-glucan synthase (FKS1), the formin BNI1, the exocyst component SEC3 and the transcription factor SKN7.
Specific Function
G-protein beta-subunit binding
Gene Name
RHO1
Uniprot ID
P06780
Uniprot Name
GTP-binding protein RHO1
Molecular Weight
23152.32 Da
References
  1. Pfaller MA, Messer SA, Motyl MR, Jones RN, Castanheira M: In vitro activity of a new oral glucan synthase inhibitor (MK-3118) tested against Aspergillus spp. by CLSI and EUCAST broth microdilution methods. Antimicrob Agents Chemother. 2013 Feb;57(2):1065-8. doi: 10.1128/AAC.01588-12. Epub 2012 Dec 10. [Article]
  2. Lepak AJ, Marchillo K, Andes DR: Pharmacodynamic target evaluation of a novel oral glucan synthase inhibitor, SCY-078 (MK-3118), using an in vivo murine invasive candidiasis model. Antimicrob Agents Chemother. 2015 Feb;59(2):1265-72. doi: 10.1128/AAC.04445-14. Epub 2014 Dec 15. [Article]
  3. Pfaller MA, Messer SA, Motyl MR, Jones RN, Castanheira M: Activity of MK-3118, a new oral glucan synthase inhibitor, tested against Candida spp. by two international methods (CLSI and EUCAST). J Antimicrob Chemother. 2013 Apr;68(4):858-63. doi: 10.1093/jac/dks466. Epub 2012 Nov 28. [Article]
  4. Pfaller MA, Messer SA, Rhomberg PR, Borroto-Esoda K, Castanheira M: Differential Activity of the Oral Glucan Synthase Inhibitor SCY-078 against Wild-Type and Echinocandin-Resistant Strains of Candida Species. Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: AAC.00161-17. doi: 10.1128/AAC.00161-17. Print 2017 Aug. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...

Components:
References
  1. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands.

Components:
References
  1. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Wring S, Murphy G, Atiee G, Corr C, Hyman M, Willett M, Angulo D: Lack of Impact by SCY-078, a First-in-Class Oral Fungicidal Glucan Synthase Inhibitor, on the Pharmacokinetics of Rosiglitazone, a Substrate for CYP450 2C8, Supports the Low Risk for Clinically Relevant Metabolic Drug-Drug Interactions. J Clin Pharmacol. 2018 Oct;58(10):1305-1313. doi: 10.1002/jcph.1146. Epub 2018 May 10. [Article]
  2. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Transporter
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: Brexafemme (Ibrexafungerp) Oral Tablet [Link]

Drug created on October 20, 2016 22:30 / Updated on July 03, 2021 01:49