Identification

Name
Posaconazole
Accession Number
DB01263
Description

Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients.

Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Thumb
Weight
Average: 700.7774
Monoisotopic: 700.329708282
Chemical Formula
C37H42F2N8O4
Synonyms
  • Posaconazole
External IDs
  • Sch 56592
  • SCH-56592
  • SCH56592
  • Schering 56592

Pharmacology

Indication

For prophylaxis of invasive Aspergillus and Candida infections in patients, 13 years of age and older, who are at high risk of developing these infections due to being severely immunocompromised as a result of procedures such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or due to hematologic malignancies with prolonged neutropenia from chemotherapy. Also for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Posaconazole is used as an alternative treatment for invasive aspergillosis, Fusarium infections, and zygomycosis in patients who are intolerant of, or whose disease is refractory to, other antifungals.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Posaconazole is an antifungal agent structurally related to itraconazole. It is a drug derived from itraconzaole through the replacement of the chlorine substituents with flourine in the phenyl ring, as well as hydroxylation of the triazolone side chain. These modifications enhance the potency and spectrum of activity of the drug. Posaconazole can be either fungicial or fungistatic in action.

Mechanism of action

As a triazole antifungal agent, posaconazole exerts its antifungal activity through blockage of the cytochrome P-450 dependent enzyme, sterol 14α-demethylase, in fungi by binding to the heme cofactor located on the enzyme. This leads to the inhibition of the synthesis of ergosterol, a key component of the fungal cell membrane, and accumulation of methylated sterol precursors. This results in inhibition of fungal cell growth and ultimately, cell death.

TargetActionsOrganism
ACytochrome P450 51
antagonist
Yeast
Absorption

Posaconazole is absorbed with a median Tmax of approximately 3 to 5 hours.

Volume of distribution
  • 1774 L
Protein binding

Posaconazole is highly protein bound (>98%), predominantly to albumin.

Metabolism

Posaconazole primarily circulates as the parent compound in plasma. Of the circulating metabolites, the majority are glucuronide conjugates formed via UDP glucuronidation (phase 2 enzymes). Posaconazole does not have any major circulating oxidative (CYP450 mediated) metabolites. The excreted metabolites in urine and feces account for ~17% of the administered radiolabeled dose.

Route of elimination

The excreted metabolites in urine and feces account for ~17% of the administered radiolabeled dose.

Half-life

Posaconazole is eliminated with a mean half-life (t½) of 35 hours (range 20 to 66 hours).

Clearance
  • 32 L/hr
  • 51 L/hr [Single-Dose Suspension Administration of 200 mg, fasted]
  • 21 L/hr [Single-Dose Suspension Administration of 200 mg, nonfat meal]
  • 14 L/hr [Single-Dose Suspension Administration of 200 mg, high fat meal]
  • 91 L/hr [Single-Dose Suspension Administration of 400 mg, fasted]
  • 43 L/hr [Single-Dose Suspension Administration of 400 mg with liquid nutritional supplement (14 g fat)]
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

During the clinical trials, some patients received posaconazole up to 1600 mg/day with no adverse events noted that were different from the lower doses. In addition, accidental overdose was noted in one patient who took 1200 mg BID for 3 days. No related adverse events were noted by the investigator.

Affected organisms
  • Aspergillis, Candida and other fungi
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Posaconazole can be increased when it is combined with Abametapir.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Posaconazole.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Posaconazole.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Posaconazole.
AcebutololThe risk or severity of QTc prolongation can be increased when Posaconazole is combined with Acebutolol.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Posaconazole.
AcrivastineThe risk or severity of QTc prolongation can be increased when Posaconazole is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Posaconazole is combined with Adenosine.
AfatinibThe serum concentration of Posaconazole can be increased when it is combined with Afatinib.
AjmalineThe risk or severity of QTc prolongation can be increased when Posaconazole is combined with Ajmaline.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with food. Posaconazole suspension can also be taken with a nutritional supplement drink or carbonated beverage if a full meal cannot be consumed.

Products

Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
NoxafilTablet, delayed release100 mgOralMerck Sharp & Dohme Limited2005-10-25Not applicableEU flag
NoxafilTablet, coated100 mg/1OralMerck Sharp & Dohme Corp.2013-11-25Not applicableUS flag00085 4324 02 nlmimage10 24411278
NoxafilInjection, solution, concentrate300 mgIntravenousMerck Sharp & Dohme Limited2005-10-25Not applicableEU flag
NoxafilSuspension40 mg/mlOralMerck Sharp & Dohme Limited2005-10-25Not applicableEU flag
NoxafilSuspension40 mg/1mLOralMerck Sharp & Dohme Corp.2006-09-15Not applicableUS flag
NoxafilTablet, delayed release100 mgOralMerck Sharp & Dohme Limited2005-10-25Not applicableEU flag
NoxafilSolution18 mg/1mLIntravenousMerck Sharp & Dohme Corp.2014-03-13Not applicableUS flag
Posaconazole SpSuspension40 mg/mlOralSchering Plough Europe2005-10-252009-08-03EU flag
PosanolTablet, delayed releaseOralMerck Ltd.2014-05-21Not applicableCanada flag
PosanolSuspensionOralMerck Ltd.2007-06-06Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PosaconazoleTablet, delayed release100 mg/1OralAmerican Health Packaging2020-06-01Not applicableUS flag
PosaconazoleTablet, coated100 mg/1OralPar Pharmaceutical Inc.2019-08-30Not applicableUS flag
PosaconazoleTablet, delayed release100 mg/1OralLannett Company Inc.2019-08-28Not applicableUS flag
Sandoz PosaconazoleTablet, delayed releaseOralSandoz Canada IncorporatedNot applicableNot applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
J02AC04 — Posaconazole
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Phenylpiperazines
Alternative Parents
N-arylpiperazines / Phenyl-1,2,4-triazoles / Aminophenyl ethers / Phenoxy compounds / Aniline and substituted anilines / Dialkylarylamines / Alkyl aryl ethers / Fluorobenzenes / Aryl fluorides / Tetrahydrofurans
show 9 more
Substituents
1,2,4-triazole / Alcohol / Alkyl aryl ether / Amine / Aminophenyl ether / Aniline or substituted anilines / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Azacycle
show 30 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
organofluorine compound, aromatic ether, N-arylpiperazine, triazole antifungal drug, conazole antifungal drug, triazoles, oxolanes (CHEBI:64355)

Chemical Identifiers

UNII
6TK1G07BHZ
CAS number
171228-49-2
InChI Key
RAGOYPUPXAKGKH-XAKZXMRKSA-N
InChI
InChI=1S/C37H42F2N8O4/c1-3-35(26(2)48)47-36(49)46(25-42-47)31-7-5-29(6-8-31)43-14-16-44(17-15-43)30-9-11-32(12-10-30)50-20-27-19-37(51-21-27,22-45-24-40-23-41-45)33-13-4-28(38)18-34(33)39/h4-13,18,23-27,35,48H,3,14-17,19-22H2,1-2H3/t26-,27+,35-,37-/m0/s1
IUPAC Name
4-{4-[4-(4-{[(3R,5R)-5-(2,4-difluorophenyl)-5-[(1H-1,2,4-triazol-1-yl)methyl]oxolan-3-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-1-[(2S,3S)-2-hydroxypentan-3-yl]-4,5-dihydro-1H-1,2,4-triazol-5-one
SMILES
[H][[email protected]@](C)(O)[[email protected]]([H])(CC)N1N=CN(C1=O)C1=CC=C(C=C1)N1CCN(CC1)C1=CC=C(OC[[email protected]]2([H])CO[[email protected]](CN3C=NC=N3)(C2)C2=C(F)C=C(F)C=C2)C=C1

References

Synthesis Reference

Dominic De Souza, "PREPARATION OF POSACONAZOLE INTERMEDIATES." U.S. Patent US20130203994, issued August 08, 2013.

US20130203994
General References
  1. Cornely OA, Maertens J, Winston DJ, Perfect J, Ullmann AJ, Walsh TJ, Helfgott D, Holowiecki J, Stockelberg D, Goh YT, Petrini M, Hardalo C, Suresh R, Angulo-Gonzalez D: Posaconazole vs. fluconazole or itraconazole prophylaxis in patients with neutropenia. N Engl J Med. 2007 Jan 25;356(4):348-59. [PubMed:17251531]
  2. Ullmann AJ, Lipton JH, Vesole DH, Chandrasekar P, Langston A, Tarantolo SR, Greinix H, Morais de Azevedo W, Reddy V, Boparai N, Pedicone L, Patino H, Durrant S: Posaconazole or fluconazole for prophylaxis in severe graft-versus-host disease. N Engl J Med. 2007 Jan 25;356(4):335-47. [PubMed:17251530]
  3. Bhattacharya M, Rajeshwari K, Dhingra B: Posaconazole. J Postgrad Med. 2010 Apr-Jun;56(2):163-7. doi: 10.4103/0022-3859.65281. [PubMed:20622401]
  4. Frampton JE, Scott LJ: Posaconazole : a review of its use in the prophylaxis of invasive fungal infections. Drugs. 2008;68(7):993-1016. [PubMed:18457464]
  5. Schiller DS, Fung HB: Posaconazole: an extended-spectrum triazole antifungal agent. Clin Ther. 2007 Sep;29(9):1862-86. [PubMed:18035188]
  6. Kwon DS, Mylonakis E: Posaconazole: a new broad-spectrum antifungal agent. Expert Opin Pharmacother. 2007 Jun;8(8):1167-78. [PubMed:17516880]
  7. Groll AH, Walsh TJ: Posaconazole: clinical pharmacology and potential for management of fungal infections. Expert Rev Anti Infect Ther. 2005 Aug;3(4):467-87. [PubMed:16107193]
  8. Rachwalski EJ, Wieczorkiewicz JT, Scheetz MH: Posaconazole: an oral triazole with an extended spectrum of activity. Ann Pharmacother. 2008 Oct;42(10):1429-38. doi: 10.1345/aph.1L005. Epub 2008 Aug 19. [PubMed:18713852]
  9. Li Y, Theuretzbacher U, Clancy CJ, Nguyen MH, Derendorf H: Pharmacokinetic/pharmacodynamic profile of posaconazole. Clin Pharmacokinet. 2010 Jun;49(6):379-96. doi: 10.2165/11319340-000000000-00000. [PubMed:20481649]
KEGG Drug
D02555
PubChem Compound
468595
PubChem Substance
46508639
ChemSpider
411709
BindingDB
50181473
RxNav
282446
ChEBI
64355
ChEMBL
CHEMBL1397
ZINC
ZINC000003938482
Therapeutic Targets Database
DAP001101
PharmGKB
PA151958574
PDBe Ligand
X2N
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Posaconazole
AHFS Codes
  • 08:14.08 — Azoles
PDB Entries
2x2n / 4j14 / 4ze1 / 5fsa / 5tl8 / 6e8q
FDA label
Download (183 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceObesity, Morbid1
4CompletedBasic ScienceSystemic Fungal Infections1
4CompletedPreventionAcute Myeloid Leukemia (AML) / Allogeneic Stem Cell Transplant / Graft Versus Host Disease, Acute / Myelo Dysplastic Syndrome1
4CompletedPreventionAcute Myeloid Leukemia (AML) / Aplastic Anemia / Myelodysplastic Syndromes (MDS) / Transplantation, Bone Marrow1
4CompletedPreventionAcute Myeloid Leukemia (AML) / Infections, Fungal / Neutropenia1
4CompletedPreventionHaematological Malignancies1
4CompletedTreatmentAcute Myeloid Leukemia (AML) / Myelodysplastic Syndrome1
4RecruitingPreventionAspergillosis; Pulmonary, Invasive (Etiology)1
4RecruitingTreatmentInfections, Fungal / Invasive Aspergillosis / Invasive Candidiases / Invasive Fungal Infections / Pharmacokinetics / Posaconazole / Prophylaxis1
4TerminatedPreventionInfections, Fungal2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Patheon Inc.
  • Schering Corp.
  • Schering-Plough Inc.
Dosage Forms
FormRouteStrength
Injection, solution, concentrateIntravenous300 mg
SolutionIntravenous18 mg/1mL
SuspensionOral40 mg/ml
SuspensionOral40 mg/1mL
TabletOral100 MG
Tablet, coatedOral100 mg/1
Tablet, delayed releaseOral100 mg
Tablet, film coatedOral100 mg
Tablet, delayed release100 mg
Tablet
SuspensionOral4 g
Tablet, delayed releaseOral100 mg/1
SolutionIntravenous
SuspensionOral
SolutionIntravenous300 mg
Tablet, delayed releaseOral
Prices
Unit descriptionCostUnit
Noxafil 40 mg/ml suspension7.08USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5703079No1997-12-302014-08-26US flag
CA2305803No2009-12-222018-10-05Canada flag
CA2179396No2001-04-172014-12-20Canada flag
US5661151No1997-08-262019-07-19US flag
US6958337No2005-10-252018-10-05US flag
US8263600No2012-09-112022-04-01US flag
US9023790No2015-05-052031-07-04US flag
US8410077No2013-04-022029-03-13US flag
US9493582No2016-11-152033-02-27US flag
US9358297No2016-06-072031-06-24US flag
US9750822No2017-09-052029-03-13US flag
US10117951No2018-11-062029-03-13US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
logP5.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.012 mg/mLALOGPS
logP4.71ALOGPS
logP5.41ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)14.83ChemAxon
pKa (Strongest Basic)3.93ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count9ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area111.79 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity200.71 m3·mol-1ChemAxon
Polarizability73.83 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier-0.5499
Caco-2 permeable+0.5332
P-glycoprotein substrateSubstrate0.7822
P-glycoprotein inhibitor IInhibitor0.7338
P-glycoprotein inhibitor IINon-inhibitor0.8895
Renal organic cation transporterNon-inhibitor0.7323
CYP450 2C9 substrateNon-substrate0.8131
CYP450 2D6 substrateNon-substrate0.8354
CYP450 3A4 substrateSubstrate0.6683
CYP450 1A2 substrateNon-inhibitor0.8484
CYP450 2C9 inhibitorInhibitor0.5281
CYP450 2D6 inhibitorNon-inhibitor0.8667
CYP450 2C19 inhibitorNon-inhibitor0.6409
CYP450 3A4 inhibitorNon-inhibitor0.5532
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5074
Ames testAMES toxic0.5235
CarcinogenicityNon-carcinogens0.7341
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8919 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5306
hERG inhibition (predictor II)Inhibitor0.6661
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0f6x-0319000000-ee423505638faa4620d4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0112123900-47df3b00c4a4865b0d1a

Targets

Kind
Protein
Organism
Yeast
Pharmacological action
Yes
Actions
Antagonist
General Function
Sterol 14-demethylase activity
Specific Function
Catalyzes C14-demethylation of lanosterol which is critical for ergosterol biosynthesis. It transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.
Gene Name
ERG11
Uniprot ID
P10613
Uniprot Name
Lanosterol 14-alpha demethylase
Molecular Weight
60674.965 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Chau AS, Mendrick CA, Sabatelli FJ, Loebenberg D, McNicholas PM: Application of real-time quantitative PCR to molecular analysis of Candida albicans strains exhibiting reduced susceptibility to azoles. Antimicrob Agents Chemother. 2004 Jun;48(6):2124-31. [PubMed:15155210]
  4. Li X, Brown N, Chau AS, Lopez-Ribot JL, Ruesga MT, Quindos G, Mendrick CA, Hare RS, Loebenberg D, DiDomenico B, McNicholas PM: Changes in susceptibility to posaconazole in clinical isolates of Candida albicans. J Antimicrob Chemother. 2004 Jan;53(1):74-80. Epub 2003 Dec 4. [PubMed:14657086]
  5. Bhattacharya M, Rajeshwari K, Dhingra B: Posaconazole. J Postgrad Med. 2010 Apr-Jun;56(2):163-7. doi: 10.4103/0022-3859.65281. [PubMed:20622401]
  6. Schiller DS, Fung HB: Posaconazole: an extended-spectrum triazole antifungal agent. Clin Ther. 2007 Sep;29(9):1862-86. [PubMed:18035188]
  7. Kwon DS, Mylonakis E: Posaconazole: a new broad-spectrum antifungal agent. Expert Opin Pharmacother. 2007 Jun;8(8):1167-78. [PubMed:17516880]
  8. Groll AH, Walsh TJ: Posaconazole: clinical pharmacology and potential for management of fungal infections. Expert Rev Anti Infect Ther. 2005 Aug;3(4):467-87. [PubMed:16107193]
  9. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
  10. Warrilow AG, Melo N, Martel CM, Parker JE, Nes WD, Kelly SL, Kelly DE: Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B. Antimicrob Agents Chemother. 2010 Oct;54(10):4225-34. doi: 10.1128/AAC.00316-10. Epub 2010 Jul 26. [PubMed:20660663]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Nagappan V, Deresinski S: Reviews of anti-infective agents: posaconazole: a broad-spectrum triazole antifungal agent. Clin Infect Dis. 2007 Dec 15;45(12):1610-7. doi: 10.1086/523576. [PubMed:18190324]
  2. Kharuzhyk SA, Matskevich SA, Filjustin AE, Bogushevich EV, Ugolkova SA: Survey of computed tomography doses and establishment of national diagnostic reference levels in the Republic of Belarus. Radiat Prot Dosimetry. 2010 Apr-May;139(1-3):367-70. doi: 10.1093/rpd/ncq070. Epub 2010 Feb 24. [PubMed:20181649]
  3. Kwon DS, Mylonakis E: Posaconazole: a new broad-spectrum antifungal agent. Expert Opin Pharmacother. 2007 Jun;8(8):1167-78. [PubMed:17516880]
  4. Drug Interactions & Labeling - FDA [Link]
  5. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Nagappan V, Deresinski S: Reviews of anti-infective agents: posaconazole: a broad-spectrum triazole antifungal agent. Clin Infect Dis. 2007 Dec 15;45(12):1610-7. doi: 10.1086/523576. [PubMed:18190324]
  2. Shumaker AC, Bullard HM, Churpek J, Knoebel RW: Posaconazole-digoxin drug-drug interaction mediated by inhibition of P-glycoprotein. J Oncol Pharm Pract. 2019 Oct;25(7):1758-1761. doi: 10.1177/1078155218801055. Epub 2018 Sep 27. [PubMed:30259783]

Drug created on May 16, 2007 11:41 / Updated on October 25, 2020 09:16

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