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Ibrexafungerp citrate (MK 3118 citrate) is an orally active β-1,3-glucan synthesis inhibitor, with potential antifungal activity. Ibrexafungerp citrate is an investigational agent for the treatment of Candida and Aspergillus infections[1]. | [in vivo]
Pharmacokinetic Analysis
Ibrexafungerp citrate (MK 3118 citrate) exhibits oral bioavailability (mouse 51%, rat 45%, dog 35%) following oral administration (mouse 1 mg/kg, rat 5 mg/kg and dog 5 mg/kg)[3].
Ibrexafungerp citrate (MK 3118 citrate) exhibits moderate half-lives (mouse 5.5, rat 8.7 and, dog 9.3 h) due to high plasma clearance (0.68, 0.44, and 0.45 L/h/kg respectively) combined with large volumes of distribution (5.3, 4.7, and 4.1 L/kg respectively) following intravenous administration (mouse 1 mg/kg, rat 5 mg/kg and dog 5 mg/kg)[3]. | Animal Model: | Female CD1 mice, Male and female Han Wister rats, Male and female beagle dogs[3] | | Dosage: | Mice (1 mg/kg), rats (5 mg/kg) and dogs (5 mg/kg) | | Administration: | Intravenous (i.v.) or oral gavage | | Result: | T1/2s of 5.5, 8.7, and 9.3 h for mice, rats, and dogs, respectively. |
| [References]
[1] James M Apgar, et al. Ibrexafungerp: An orally active β-1,3-glucan synthesis inhibitor. Bioorg Med Chem Lett. 2021 Jan 15;32:127661. DOI:10.1016/j.bmcl.2020.127661
[2] Mahmoud Ghannoum, et al. Ibrexafungerp: A Novel Oral Triterpenoid Antifungal in Development for the Treatment of Candida auris Infections. Antibiotics (Basel). 2020 Aug 25;9(9):539. DOI:10.3390/antibiotics9090539
[3] Stephen A Wring, et al. 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):e02068-16. DOI:10.1128/AAC.02068-16 |
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