Isavuconazole - CAS 241479-67-4
Catalog number:
241479-67-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C22H17F2N5OS
Molecular Weight:
437.47
COA:
Inquire
Targets:
Antifungal
Description:
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.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
BAL-4815; RO-0094815
MSDS:
Inquire
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 %).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Antifungal Products


CAS 101827-46-7 Butenafine HCl

Butenafine HCl
(CAS: 101827-46-7)

Butenafine HCl is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.

CAS 135575-42-7 Pneumocandin B0

Pneumocandin B0
(CAS: 135575-42-7)

Pneumocandin B0, also called as L 688786, is an inhibitor of ß-(1,3)-D-glucan (a component of fungal cell walls) synthesis with an antifungal effect (IC50s = 70...

CAS 65277-42-1 Ketoconazole

Ketoconazole
(CAS: 65277-42-1)

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. It is used primarily to treat fun...

CAS 166663-25-8 Anidulafungin

Anidulafungin
(CAS: 166663-25-8)

Anidulafungin, is a semisynthetic echinocandin that inhibits glucan synthase, an enzyme important in the formation of (1→3)-β-D-glucan, a major fungal cell wall...

CAS 68890-66-4 Piroctone olamine

Piroctone olamine
(CAS: 68890-66-4)

Piroctone olamine, a pyridine derivate, is an anti-dandruff agent with fungicidal effect used in shampoo formulations.

CAS 131436-22-1 Cercosporamide

Cercosporamide
(CAS: 131436-22-1)

Cercosporamide, a natural antifungal phytotoxin, has been found to be a selective Mnk inhibitor and shows probable antileukemic effects.

CAS 110588-57-3 R66905

R66905
(CAS: 110588-57-3)

R66905, also known as saperconazole, is a broad-spectrum antifungal triazole.

CAS 73151-29-8 Fenticonazole Nitrate

Fenticonazole Nitrate
(CAS: 73151-29-8)

Fenticonazole Nitrate is an azole antifungal agent.

CAS 63824-12-4 Aliconazole

Aliconazole
(CAS: 63824-12-4)

An antifungal azole derivative

CAS 99592-39-9 Sertaconazole nitrate

Sertaconazole nitrate
(CAS: 99592-39-9)

Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and muc...

CAS 130-26-7 Clioquinol

Clioquinol
(CAS: 130-26-7)

Clioquinol, a quinoline derivative, is an antifungal and antiprotozoal agent and has also been found to have probable effect against cancer and Alzheimer's dise...

CAS 141-94-6 Hexetidine

Hexetidine
(CAS: 141-94-6)

Hexetidine, mixture of stereoisomers, is an antibacterial and antifungal agent that destroy fungi by suppressing their ability to grow or reproduce.

CAS 35554-44-0 Enilconazole

Enilconazole
(CAS: 35554-44-0)

Enilconazole Is An Agricultiral Fungicide, particularly in the growing of citrus fruits, also used as a topical antimycotic.

CAS 911208-73-6 Tenofovir exalidex

Tenofovir exalidex
(CAS: 911208-73-6)

Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a highly potent prodrug of the antiviral tenofovir, appeared safe and well-tolerated in patients...

CAS 136212-91-4 Dermaseptin

Dermaseptin
(CAS: 136212-91-4)

Dermaseptin is a 34-residue antimicrobial peptide.

CAS 159532-41-9 Fluconazole mesylate

Fluconazole mesylate
(CAS: 159532-41-9)

Fluconazole (mesylate) is the mesylate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses....

CAS 777-11-7 Haloprogin

Haloprogin
(CAS: 777-11-7)

Haloprogin is an antifungal drug. It can be used for the treatment of athlete's foot and other fungal infections.

CAS 137234-62-9 Voriconazole

Voriconazole
(CAS: 137234-62-9)

Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates

CAS 65899-73-2 Tioconazole

Tioconazole
(CAS: 65899-73-2)

Tioconazole is an antifungal medication of the imidazole class used to treat infections caused by a fungus or yeast, with an average IC50 of 1.7 μM.

CAS 29342-05-0 Ciclopirox

Ciclopirox
(CAS: 29342-05-0)

Ciclopirox olamine (used in preparations called Batrafen, Loprox, Rejuvenail, Mycoster, Penlac and Stieprox) is a synthetic antifungal agent for topical dermato...

Chemical Structure

CAS 241479-67-4 Isavuconazole

Quick Inquiry

Verification code

Featured Items