Identification

Name
Posaconazole
Accession Number
DB01263
Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Description

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

Structure
Thumb
Synonyms
Not Available
External IDs
Sch 56592 / SCH-56592 / SCH56592 / Schering 56592
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NoxafilSuspension40 mg/mlOralMerck Sharp & Dohme Limited2005-10-25Not applicableEu
NoxafilTablet, coated100 mg/1OralMerck Sharp & Dohme Limited2013-11-25Not applicableUs00085 4324 02 nlmimage10 24411278
NoxafilTablet, delayed release100 mgOralMerck Sharp & Dohme Limited2005-10-25Not applicableEu
NoxafilSuspension40 mg/1mLOralMerck Sharp & Dohme Limited2006-09-15Not applicableUs
NoxafilTablet, delayed release100 mgOralMerck Sharp & Dohme Limited2005-10-25Not applicableEu
NoxafilSolution18 mg/1mLIntravenousMerck Sharp & Dohme Limited2014-03-13Not applicableUs
NoxafilInjection, solution, concentrate300 mgIntravenousMerck Sharp & Dohme Limited2005-10-25Not applicableEu
PosanolSuspension40 mgOralMerck Ltd.2007-06-06Not applicableCanada
PosanolSolution18 mgIntravenousMerck Ltd.2014-11-24Not applicableCanada
PosanolTablet, delayed release100 mgOralMerck Ltd.2014-05-21Not applicableCanada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Posaconazole SpPosaconazole (40 mg/ml)SuspensionOralSchering Plough Europe2005-10-252009-08-03Eu
Categories
UNII
6TK1G07BHZ
CAS number
171228-49-2
Weight
Average: 700.7774
Monoisotopic: 700.329708282
Chemical Formula
C37H42F2N8O4
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-ylmethyl)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][C@@](C)(O)[C@]([H])(CC)N1N=CN(C1=O)C1=CC=C(C=C1)N1CCN(CC1)C1=CC=C(OC[C@]2([H])CO[C@](CN3C=NC=N3)(C2)C2=C(F)C=C(F)C=C2)C=C1

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
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
ALanosterol 14-alpha demethylase
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)]
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
DrugInteraction
16-BromoepiandrosteroneThe serum concentration of 16-Bromoepiandrosterone can be increased when it is combined with Posaconazole.
19-norandrostenedioneThe serum concentration of 19-norandrostenedione can be increased when it is combined with Posaconazole.
5-androstenedioneThe serum concentration of 5-androstenedione can be increased when it is combined with Posaconazole.
AbemaciclibThe risk or severity of adverse effects can be increased when Posaconazole is combined with Abemaciclib.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Posaconazole.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Posaconazole.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Posaconazole.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Posaconazole.
AcetazolamideThe metabolism of Posaconazole can be decreased when combined with Acetazolamide.
Acetyl sulfisoxazoleThe metabolism of Posaconazole can be decreased when combined with Acetyl sulfisoxazole.
Food Interactions
Not Available

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]
External Links
KEGG Drug
D02555
PubChem Compound
468595
PubChem Substance
46508639
ChemSpider
411709
BindingDB
50181473
ChEBI
64355
ChEMBL
CHEMBL1397
Therapeutic Targets Database
DAP001101
PharmGKB
PA151958574
HET
X2N
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Posaconazole
ATC Codes
J02AC04 — 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
0RecruitingBasic SciencePharmacokinetics1
1Active Not RecruitingOtherInfections, Fungal1
1Active Not RecruitingPreventionInfections, Fungal1
1CompletedNot AvailableNeoplasms1
1CompletedPreventionInfections, Fungal3
1CompletedPreventionNeutropenias1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Infections, Fungal1
1TerminatedTreatmentInfections, Fungal1
1WithdrawnTreatmentInvasive Aspergillosis1
1, 2Active Not RecruitingTreatmentAcute Myelogenous Leukaemia (AML) / Myelogenous Leukemia / Treatment Naive AML1
2CompletedPreventionChronic Granulomatous Disease (CGD)1
2CompletedTreatmentChagas Disease2
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Oral Candidiasis1
2CompletedTreatmentInfections, Fungal / Leukemias1
2CompletedTreatmentMycoses2
2CompletedTreatmentOnychomycosis1
2RecruitingPreventionAplastic Anaemia (AA) / Infections, Fungal / Myelodysplastic Syndromes1
3CompletedPreventionLeukemia, Myelocytic, Acute / Myelodysplastic Syndromes / Neutropenias1
3CompletedPreventionLeukopenia1
3CompletedPreventionMycoses1
3CompletedTreatmentAspergillosis1
3CompletedTreatmentChronic Granulomatous Disease (CGD) / Hyper IgE Syndromes / Infection NOS1
3CompletedTreatmentCoccidioidomycosis1
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Oral Candidiasis1
3CompletedTreatmentInfections, Fungal1
3CompletedTreatmentInvasive Fungal Infections / Malignancies, Hematologic1
3CompletedTreatmentMycoses3
3RecruitingTreatmentInfections, Fungal1
4CompletedBasic ScienceObesity, Morbid1
4CompletedBasic ScienceSystemic Fungal Infections1
4CompletedPreventionAcute Myelogenous Leukaemia (AML) / Infections, Fungal / Neutropenias1
4CompletedTreatmentAcute Myelogenous Leukaemia (AML) / Myelodysplastic Syndrome1
4Not Yet RecruitingPreventionAplastic Anaemia (AA) / Leukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndromes / Transplantation, Bone Marrow1
4RecruitingPreventionAllogeneic Stem Cell Transplant / Graft Versus Host Disease, Acute / Leukemia Acute Myeloid Leukemia (AML) / Myelo Dysplastic Syndrome1
4RecruitingPreventionAspergillosis; Pulmonary, Invasive (Etiology)1
4TerminatedPreventionInfections, Fungal2
4WithdrawnTreatmentClinical Infection1
Not AvailableCompletedNot AvailableInfections, Fungal1
Not AvailableCompletedNot AvailableMycoses2
Not AvailableNot Yet RecruitingNot AvailableCystic Fibrosis (CF)1
Not AvailableRecruitingNot AvailableInvasive Fungal Infections1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Patheon Inc.
  • Schering Corp.
  • Schering-Plough Inc.
Dosage forms
FormRouteStrength
Injection, solution, concentrateIntravenous300 mg
SolutionIntravenous18 mg/1mL
SuspensionOral40 mg/1mL
SuspensionOral40 mg/ml
Tablet, coatedOral100 mg/1
SolutionIntravenous18 mg
SuspensionOral40 mg
Tablet, delayed releaseOral100 mg
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)
US5703079No1994-08-262014-08-26Us
CA2305803No2009-12-222018-10-05Canada
CA2179396No2001-04-172014-12-20Canada
US5661151No1999-07-192019-07-19Us
US6958337No1998-10-052018-10-05Us
US8263600No2002-04-012022-04-01Us
US9023790No2011-07-042031-07-04Us
US8410077No2009-03-132029-03-13Us
US9493582No2013-02-272033-02-27Us
US9358297No2011-06-242031-06-24Us
US9750822No2009-03-132029-03-13Us

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

Taxonomy

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
Phenylpiperazine / N-arylpiperazine / Phenyltriazole / Phenyl-1,2,4-triazole / Aminophenyl ether / Phenoxy compound / Phenol ether / Tertiary aliphatic/aromatic amine / Aniline or substituted anilines / Dialkylarylamine
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)

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
Human
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]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
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]

Drug created on May 16, 2007 11:41 / Updated on October 16, 2018 08:36