Drug General Information
Drug ID D0V4IB
Drug Name Itraconazole
Synonyms Canadiol; Hyphanox; ITCZ; ITZ; Intraconazole; Itraconazol; Itraconazolum; Itrizole; Oriconazole; Orungal; Prokanazol; Sempera; Spherazole; Sporal; Sporanos; Sporanox; Sporonox; Triasporn; Itraconazol [Spanish]; Itraconazole oral solution; Itraconazolum [Latin]; R 51211; Cis-Itraconazole; Itraconazole & Bovine Lactoferrin; Itraconazole & Nyotran; Itrizole (TN); R-51211; Sporanox (TN); Itraconazole & Nyotran(Liposomal Nystatin); Itraconazole (JAN/USAN); Oriconazole, R51211, Sporanox; Itraconazole [USAN:BAN:INN:JAN]; (+-)-1-sec-Butyl-4-(p-(4-(p-(((2R*,4S*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazinyl)phenyl)-delta(sup 2)-1,2,4-triazolin-5-one; (1)-cis-4-(4-(4-(4-((2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2,4-dihydro-2-sec-butyl-3H-1,2,4-triazol-3-one; 2-(butan-2-yl)-4-{4-[4-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-2,4-dihydro-3H-1,2,4-triazol-3-one; 2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; 2-butan-2-yl-4-[4-[4-[4-[[(2S,4R)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; 2-butan-2-yl-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; 3H-1,2,4-Triazol-3-one, 4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-pipera-zinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl); 4-(4-{4-[4-({[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl}oxy)phenyl]piperazin-1-yl}phenyl)-2-(1-methylpropyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
Drug Type Small molecular drug
Therapeutic Class Antifungal Agents
Company Janssen Pharmaceutica
Structure D0V4IB
Drug Resistance Mutations
Target Name Fungal Heme O synthase (cox10) Target Info
Gene Name cox10
Uniprot ID COX10_ASPFU
Species Neosartorya fumigata
Reference Sequence MIYLRSSLLRSGLARDPARLCSQCFSRLSPSRRPVAVRSFFSSSRLRAGIADHESTPSTV
QKTYFSANRTADGLLASLSAVNSSPRSIADNALSQGAASSESITSQSTSQELPHRRRKRL
KEEAAKNNAAETELPPDASSQLSTLSSALPATSLRRKLAAFLALTKPRLSFLIVLTTTSA
YGMYPISSLLTLDPSMTPLPTLSTSTLTFLYLTTGTFLSSCSANTLNMLLEPKYDALMSR
TRNRPLVRGLLSRRAAVLFAIATAAAGLGLLYIGTNPTTTALSASNICLYAFVYTPLKRI
SVINTWVGAVVGGIPPLMGWTAAAGQTATTGHDSWRDMLFSKDSIGGWLLGGILFAWQFP
HFNALSYMIREEYKAAGYRMLAWTNPAANARVALRYSLLMFPFSVGLWWVGVVGNGFLVG
STAANGWLVKEAYKFWRHQGANGSARRLFWASIWQLPILLVGGLVTKKGLWDGVWNNVFG
QPVEDEDDYLWEDEDEVAEAERKMIPAKTSSS [Neosartorya fumigata]
Targeted Disease Aspergillosis
Drug Resistance Mutations
Mutation info Missense: R243Q [1]
Mutation Frequency 1 out of 105 isolates
Target Name Fungal Lanosterol 14-alpha demethylase (cyp51A) Target Info
Gene Name cyp51A
Uniprot ID B3V1X6_ASPFM
Species Aspergillus fumigatus
Reference Sequence MVPMLWLTAYMAVAVLTAILLNVVYQLFFRLWNRTEPPMVFHWVPYLGSTISYGIDPYKF
FFACREKYGDIFTFILLGQKTTVYLGVQGNEFILNGKLKDVNAEEVYSPLTTPVFGSDVV
YDCPNSKLMEQKKFIKYGLTQSALESHVPLIEKEVLDYLRDSPNFQGSSGRVDISAAMAE
ITIFTAARALQGQEVRSKLTAEFADLYHDLDKGFTPINFMLPWAPLPHNKKRDAAHARMR
SIYVDIITQRRLDGEKDSQKSDMIWNLMNCTYKNGQQVPDKEIAHMMITLLMAGQHSSSS
ISAWIMLRLASQPKVLEELYQEQLANLGPAGPDGSLPPLQYKDLDKLPFHQHVIRETLRI
HSSIHSIMRKVKSPLPVPGTPYMIPPGRVLLASPGVTALSDEHFPNAGCWDPHRWENQAT
KEQENDKVVDYGYGAVSKGTSSPYLPFGAGRHRCIGEKFAYVNLGVILATIVRHLRLFNV
DGKKGVPETDYSSLFSGPMKPSIIGWEKRSKNTSK [Aspergillus fumigatus]
Targeted Disease Aspergillosis
Drug Resistance Mutations
Mutation info Missense: F219L [1]
Mutation Frequency 1 out of 105 isolates
References
REF 1 Screening and Characterization of a Non-cyp51A Mutation in an Aspergillus fumigatus cox10 Strain Conferring Azole Resistance. Antimicrob Agents Chemother. 2016 Dec 27;61(1). pii: e02101-16.

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