Isavuconazole - CAS 241479-67-4
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Not Intended for Therapeutic Use. For research use only.
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Isavuconazole is a new triazole currently undergoing phase III clinical trials. This compound has shown in vitro activity against a large number of clinical important yeasts and molds including Aspergillus spp., Fusarium spp., Scedosporium spp., Candida spp., the Zygomycetes and Cryptococcus spp.
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BAL-4815; RO-0094815
1.Pharmacology, In Vitro Activity, and In Vivo Efficacy of New Antifungal Agents
Nathan P. Wiederhold. Current Fungal Infection Reports 2009, 3:77–85
Isavuconazole (BAL-4815) is an investigational antifungal agent and member of the triazole class (Table 1). Like the other members of this class, isavuconazole inhibits 14-α-demethylase, a key component of the ergosterol biosynthetic pathway. This triazole is available as isavuconazonium (BAL-8557, formerly RO-0098557), a water-soluble prodrug that consists of a tetrazolium salt (an [N-(3-acetoxypropyl)-N-methylamino]-carboxymethyl group) linked to an aminocarboxy moiety (Fig. 1) [3]. The water-soluble prodrug avoids problems associated with lipophilicity that may occur with other triazoles such as itraconazole, posaconazole, and voriconazole. These problems include limited oral bioavailability or the need to include cyclodextrin within intravenous formulations. After oral or intravenous administration, the prodrug is rapidly cleaved into the active component by plasma esterases in humans and other species. Structurally, isavuconazole is similar to that of the investigational agent ravuconazole, with a substitution of a 2,5-dil uoro-substituted benzene moiety in place of the 2,4-dihalo group, which is found in the other members of this class.
2.Successful isavuconazole salvage therapy in a patient with invasive
J. Ervens • M. Ghannoum • B. Graf • S. Schwartz. Infection (2014) 42:429–432
Antifungal treatment was resumed on day 104 with isavuconazole. Initially, isavuconazole was administered intravenously (days 104–105: 200 mg t.i.d. daily; day 106–107: 200 mg daily q.d.) with a switch to oral therapy on day 108 (200 mg q.d.). During 14 days of isavuconazole therapy, the plasma trough concentration did not exceed 0.86 lg/mL, and the concentration in soft tissue samples ranged from 1.09 to 1.38 lg/g (Table 1), which although higher than the MIC of the infecting isolate was still lower than the trough concentration expected from the isavuconazole dose given (C2 lg/mL). To enhance isavuconazole concentrations, which might have been limited by yet unknown drug–drug interactions, concomitant therapy with various drugs was either terminated between days 117 and 141 or limited to this period, while treatment with amlodipine, mesalazine (both prior to isavuconazole—ongoing after end of isavuconazole), ranitidine (terminated on day 174) and heparin (dalteparin: given prior to treatment to day 113 and on days 119–174; unfractioned heparin: days 114–118) was maintained. The drugs termi- nated were ciprofloxacin eardrops (days 121–127), clindamycine (days 114–118), fentanyl (days 112, 119), loperamide (days 118–119), lorazepam (days 121–132), lormetazepam (days 119–120, 124), metamizole (days 113–119), mirtazapine (prior isavuconazole—day 125), morphine (day 119), ondansetron (day 117), paracematol (days 113–118), propofol (days 112, 119), tramadol (days 120–132) and valproate (prior isavuconazole—day 133).
3.Treatment Options for Mucormycosis
Marisa H. Miceli, Carol A. Kauffman. Curr Treat Options Infect Dis (2015) 7:142–154
Isavuconazole is a recently approved extended-spectrum azole agent that is active against the Mucorales, including Rhizomucor spp., Rhizopus spp., and Mucor spp. Approval of isavuconazole for the treatment of mucormycosis was based on the results of a phase 3, open-label, noncomparative, multi-center study of invasive fungal infections that included 37 patients who had invasive mucormycosis. Of the 37 patients, 32 (86 %) had proven invasive mucormycosis and 5 (14 %) had probable invasive mucormycosis. Sixteen patients (43 %) received isavuconazole as salvage therapy after failing or being intolerant of standard therapy. Twenty-one patients (57 %) received only isavuconazole for mucormycosis. The endpoints were overall clinical response and mortality at day 42. The overall success at day 42 was judged to be 32 %, and mortality was 38 %. Mortality was highest among patients with refractory disease (46 %).
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CAS 241479-67-4 Isavuconazole

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