General Information of Drug (ID: DMUL5EW)

Drug Name
Posaconazole Drug Info
Synonyms
Noxafil; Spriafil; Posaconazole SP; Posaconazole in combination with MGCD290; SCH56592; Sch 56592; X2N; Noxafil (TN); Noxafil, Posaconazole; SCH-56592; Posaconazole (USAN/INN); Posaconazole [USAN:INN:BAN]; 1-((1S,2S)-1-Ethyl-2-hydroxypropyl)-4-{4-[4-(4-{[(5S,3R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazolylmethyl)oxolan-3-yl]methoxy}phenyl)piperazinyl]phenyl}-1,2,4-triazolin-5-one; 4-(p-(4-(p-(((3R,5R)-5-(2,4-Difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furyl)methoxy)phenyl)-1-piperazinyl)phenyl)-1-((1S,2S)-1-ethyl-2-hydroxypropyl)-delta(sup 2)-1,2,4-triazolin-5-one; 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one; 4-[4-[4-[4-[[(5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one
Indication
Disease Entry ICD 11 Status REF
Aspergillosis 1F20 Approved [1]
Candidiasis 1F23 Approved [2]
Chromomycosis Approved [2]
Coccidioidomycosis 1F25 Approved [2]
Fusariosis Approved [2]
Therapeutic Class
Antifungal Agents
Cross-matching ID
PubChem CID
468595
ChEBI ID
CHEMBL64355
CAS Number
CAS 171228-49-2
TTD Drug ID
DMUL5EW
VARIDT Drug ID
DR00111
INTEDE Drug ID
DR1316
ACDINA Drug ID
D00542

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [8]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [8]
Ketoconazole DMPZI3Q Blastomycosis 1F22 Approved [9]
Miconazole DMPMYE8 Cutaneous candidiasis 1F23.14 Approved [8]
Oxiconazole DME7KRM Tinea corporis 1F28.Y Approved [10]
Fluconazole DMOWZ6B Cryptococcal meningitis Approved [8]
Terconazole DMJ13KI Candidiasis 1F23 Approved [11]
Bifonazole DM3KN7V Fungal infection 1F29-1F2F Approved [12]
Tioconazole DMNYPGS Onychomycosis EE12.1 Approved [13]
Econazole DMFSWGH Cutaneous candidiasis 1F23.14 Approved [14]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [15]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [16]
Methotrexate DM2TEOL Anterior urethra cancer Approved [17]
Folic Acid DMEMBJC Colorectal carcinoma Approved [18]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [17]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [17]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [17]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [22]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [24]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [25]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [26]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [28]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [29]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [23]
Verapamil DMA7PEW Angina pectoris BA40 Approved [30]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [31]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [32]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [33]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [34]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [35]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [36]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [37]
Metronidazole DMTIVEN Abscess Approved [38]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [39]
Ethanol DMDRQZU Chronic pain MG30 Approved [40]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [41]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [42]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [42]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [43]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [41]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [42]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [44]
Gefitinib DM15F0X Colon adenocarcinoma Approved [41]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [7]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [41]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Candida Cytochrome P450 51 (Candi ERG11) TTTSOUD CP51_CANAL Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [5]
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME DEYGVN4 UD11_HUMAN Substrate [6]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [7]

References

1 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022003.
2 Posaconazole FDA Label
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25 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
26 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
27 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
28 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
29 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
30 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
31 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
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33 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
34 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
35 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
36 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
37 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
38 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
39 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
40 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
41 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
42 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
43 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
44 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.