Polymyxin B Sulfate

Identification

Name
Polymyxin B Sulfate
Accession Number
DB00781  (APRD01190)
Type
Small Molecule
Groups
Approved, Vet approved
Description

Polymyxin B sulfate is a mixture of polymyxins B1 and B2, obtained from Bacillus polymyxa strains. They are basic polypeptides of about eight amino acids and have cationic detergent action on cell membranes. Polymyxin B is used for infections with gram-negative organisms, but may be neurotoxic and nephrotoxic. All gram-positive bacteria, fungi, and the gram-negative cocci, N. gonorrhea and N. menigitidis, are resistant. It is appropriate for treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosa.

Structure
Thumb
Synonyms
  • Polimixina B
  • Polymyxin B
  • Polymyxin B Sulphate
  • Polymyxin-B-Sulfat
  • Polymyxine B
  • Polymyxine B (sulfate de)
  • Polymyxini B sulfas
  • Polymyxinum B
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aerosporin Sterile PowderPowder, for solution500000 unitIntramuscular; Intrathecal; Intravenous; Respiratory (inhalation); TopicalGlaxo Wellcome1952-12-311998-07-30Canada
Polymyxin B for Injection USPPowder, for solution50 mgIntramuscular; Intrathecal; Intravenous; OphthalmicSterimax Inc2012-05-03Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicX Gen Pharmaceuticals, Inc.2014-01-15Not applicableUs
Polymyxin BInjection, powder, for solution500000 [iU]/1Intramuscular; Intrathecal; Intravenous; OphthalmicBedford Pharmaceuticals1998-06-012014-03-31Us
Polymyxin BInjection, solution500000 1/1Intramuscular; Intrathecal; Intravenous; OphthalmicBreckenridge Pharmaceutical, Inc.2016-06-012019-03-31Us
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicX Gen Pharmaceuticals, Inc.1994-09-30Not applicableUs
Polymyxin BInjection, powder, lyophilized, for solution500000 1/1Intramuscular; Intrathecal; Intravenous; OphthalmicGland Pharma Limited2016-06-01Not applicableUs
Polymyxin BInjection500000 1/1Intramuscular; Intrathecal; IntravenousXellia Pharmaceuticals ApS2014-01-24Not applicableUs
Polymyxin BInjection, powder, for solution500000 [iU]/1Intramuscular; Intrathecal; Intravenous; OphthalmicSagent Pharmaceuticals2011-08-012014-03-31Us
Polymyxin BInjection, powder, lyophilized, for solution500000 [iU]/1Intramuscular; Intrathecal; Intravenous; OphthalmicAthenex Pharmaceutical Division, Llc.2017-01-01Not applicableUs
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; IntravenousX Gen Pharmaceuticals, Inc.2014-04-25Not applicableUs
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicFresenius Kabi2009-11-17Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
10 Person ANSIPolymyxin B Sulfate (5000 [iU]/1g) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Ibuprofen (200 mg/1) + Lidocaine (0.5 1/100g) + Neomycin sulfate (5 mg/1g) + Water (98.6 mL/100mL)KitGenuine First Aid2010-04-24Not applicableUs
25 Person ANSIPolymyxin B Sulfate (5000 [iU]/1g) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Ethanol (62 g/100g) + Ibuprofen (200 mg/1) + Isopropyl Alcohol (70 mL/100mL) + Lidocaine (0.5 g/100g) + Neomycin sulfate (5 mg/1g) + Water (98.6 mL/100mL)KitGenuine First Aid2010-04-25Not applicableUs
50 Person ANSIPolymyxin B Sulfate (5000 [iU]/1g) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Ethanol (62 g/100g) + Ibuprofen (200 mg/1) + Isopropyl Alcohol (70 mL/100mL) + Lidocaine (0.5 g/100g) + Neomycin sulfate (5 mg/1g) + Water (98.16 mL/100mL)KitGenuine First Aid2010-06-02Not applicableUs
7 Select First Aid Triple AntibioticPolymyxin B Sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Neomycin sulfate (3.5 mg/1g)OintmentTopical7-ELEVEN, INC.2016-12-08Not applicableUs
ACME FIRST AID Contains 404 PIECESPolymyxin B Sulfate (5000 [iU]/1g) + Acetylsalicylic acid (81 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Isopropyl Alcohol (70 mL/100mL) + Lidocaine (0.5 g/100g) + Neomycin sulfate (5 mg/1g) + Water (98.16 mL/100mL)KitAcme United Corporation2010-04-27Not applicableUs
Acme Home/Office/Auto KitPolymyxin B Sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Isopropyl Alcohol (0.70 mL/1mL) + Lidocaine hydrochloride (0.5 g/100g) + Neomycin sulfate (3.5 mg/1g)KitDukal Corporation2010-05-01Not applicableUs
ACME Small Cuts and BurnsPolymyxin B Sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Lidocaine (0.5 g/100g) + Neomycin sulfate (5 mg/1g)KitAcme United Corporation2010-04-30Not applicableUs
Adventure First Aid .5 TinPolymyxin B Sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzocaine (0.6 mg/100mL) + Ethanol (60 mL/100mL) + Isopropyl Alcohol (700 mg/1mL) + Neomycin sulfate (5 mg/1g)KitOral; TopicalTender Corporation2015-10-01Not applicableUs
Adventure Medical Kits 1-2 Person First AidPolymyxin B Sulfate (5000 [iU]/1g) + Acetaminophen (500 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Diphenhydramine hydrochloride (25 mg/1) + Ethanol (60 mL/100mL) + Ibuprofen (200 mg/1) + Neomycin sulfate (5 mg/1g)KitTopicalTender Corp Dba Adventure Medical Kits2010-08-26Not applicableUs
Adventure Medical Kits 1-2 Person National Ski Patrol First AidPolymyxin B Sulfate (5000 [iU]/1g) + Acetaminophen (500 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Ibuprofen (200 mg/1) + Neomycin sulfate (5 mg/1g)KitTender Corp Dba Adventure Medical Kits2010-08-26Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Neomycin and Polymyxin B Sulfates and Bacitracin Zinc with Hydrocortisone AcetatePolymyxin B Sulfate (10000) + Bacitracin zinc (400) + Hydrocortisone acetate (10 mg/1g) + Neomycin sulfate (3.5 mg/1g)OintmentOphthalmicE. FOUGERA and CO.2006-09-12Not applicableUs
NeosporinPolymyxin B Sulfate (10000) + Bacitracin zinc (400) + Neomycin sulfate (3.5 ug/1g)OintmentOphthalmicBurroughs Wellcome2006-10-03Not applicableUs
StatrolPolymyxin B Sulfate (10000) + Neomycin sulfate (3.5 mg/1g)OintmentOphthalmicALCON LABORATORIES, INC.2006-05-12Not applicableUs
StatrolPolymyxin B Sulfate (16250 1/1mL) + Neomycin sulfate (3.5 mg/1mL)SolutionOphthalmicAlcon2006-05-12Not applicableUs
StatrolPolymyxin B Sulfate (16250) + Neomycin sulfate (3.5 mg/1mL)SolutionOphthalmicALCON (Puerto Rico) INC.2006-05-12Not applicableUs
International/Other Brands
Aerosporin (GlaxoSmithKline) / Metamyxin (Pola Pharma) / Polomyxin B (Fuji Yakuhin) / Poly-Rx (X-Gen) / Polyfax (Intra) / Polyxx (Celon)
Categories
UNII
19371312D4
CAS number
1405-20-5
Weight
Average: 1203.4767
Monoisotopic: 1202.749927302
Chemical Formula
C56H98N16O13
InChI Key
WQVJHHACXVLGBL-UHFFFAOYSA-N
InChI
InChI=1S/C56H98N16O13/c1-7-32(4)13-11-12-16-44(75)63-36(17-23-57)51(80)72-46(34(6)74)56(85)68-39(20-26-60)48(77)67-41-22-28-62-55(84)45(33(5)73)71-52(81)40(21-27-61)65-47(76)37(18-24-58)66-53(82)42(29-31(2)3)69-54(83)43(30-35-14-9-8-10-15-35)70-49(78)38(19-25-59)64-50(41)79/h8-10,14-15,31-34,36-43,45-46,73-74H,7,11-13,16-30,57-61H2,1-6H3,(H,62,84)(H,63,75)(H,64,79)(H,65,76)(H,66,82)(H,67,77)(H,68,85)(H,69,83)(H,70,78)(H,71,81)(H,72,80)
IUPAC Name
N-[3-amino-1-({1-[(3-amino-1-{[6,9,18-tris(2-aminoethyl)-15-benzyl-3-(1-hydroxyethyl)-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl]carbamoyl}propyl)carbamoyl]-2-hydroxypropyl}carbamoyl)propyl]-6-methyloctanamide
SMILES
CCC(C)CCCCC(=O)NC(CCN)C(=O)NC(C(C)O)C(=O)NC(CCN)C(=O)NC1CCNC(=O)C(NC(=O)C(CCN)NC(=O)C(CCN)NC(=O)C(CC(C)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CCN)NC1=O)C(C)O

Pharmacology

Indication

For treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosa.

Associated Conditions
Pharmacodynamics

Polymyxin B sulfate is a mixture of polymyxins B1 and B2, obtained from Bacillus polymyxa strains. They are basic polypeptides of about eight amino acids and have cationic detergent action on cell membranes. Polymyxin B is used for infections with gram-negative organisms, but may be neurotoxic and nephrotoxic. All gram-positive bacteria, fungi, and the gram-negative cocci, N. gonorrhea and N. menigitidis, are resistant.

Mechanism of action

Polymyxin B sulfate has a bactericidal action against almost all gram-negative bacilli except the Proteus group. Polymyxin B sulfate interacts with the lipopolysaccharide of the cytoplasmic outer membrane of Gram-negative bacteria, altering membrane permeability and causing cell death. It does not need to enter the cell.

TargetActionsOrganism
ABacterial outer membrane
incorporation into and destabilization
Absorption

Not absorbed from the normal alimentary tract.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination

The drug is excreted slowly by the kidneys.

Half life
Not Available
Clearance
Not Available
Toxicity

Overdose can cause stomach pains, vomiting, and diarrhea.

Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Polymyxin B Sulfate is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when 3,4-Methylenedioxyamphetamine is combined with Polymyxin B Sulfate.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Polymyxin B Sulfate.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Polymyxin B Sulfate.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Polymyxin B Sulfate is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Polymyxin B Sulfate.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Polymyxin B Sulfate.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Polymyxin B Sulfate.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Polymyxin B Sulfate.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Polymyxin B Sulfate.
Food Interactions
Not Available

References

General References
  1. Yuan Z, Tam VH: Polymyxin B: a new strategy for multidrug-resistant Gram-negative organisms. Expert Opin Investig Drugs. 2008 May;17(5):661-8. doi: 10.1517/13543784.17.5.661 . [PubMed:18447592]
  2. Zavascki AP, Goldani LZ, Li J, Nation RL: Polymyxin B for the treatment of multidrug-resistant pathogens: a critical review. J Antimicrob Chemother. 2007 Dec;60(6):1206-15. Epub 2007 Sep 17. [PubMed:17878146]
External Links
Human Metabolome Database
HMDB0014919
KEGG Drug
D01066
KEGG Compound
C11613
PubChem Compound
4868
PubChem Substance
46507302
ChemSpider
4702
ChEMBL
CHEMBL241797
Therapeutic Targets Database
DAP001323
PharmGKB
PA451027
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Polymyxin_B
ATC Codes
J01XB02 — Polymyxin bS03AA03 — Polymyxin bS01AA18 — Polymyxin bS02AA11 — Polymyxin bA07AA05 — Polymyxin b
AHFS Codes
  • 08:12.28.28 — Polymyxins
MSDS
Download (46.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceAtopic Dermatitis (AD)1
0RecruitingTreatmentOsteomyelitis1
1CompletedTreatmentPlasma Cell Myeloma1
1RecruitingTreatmentRetinoblastoma1
2, 3Unknown StatusTreatmentBacteremia / Healthcare-Associated Pneumonia / Ventilator-Associated Pneumonia (VAP)1
2, 3WithdrawnTreatmentMinor burns1
3CompletedPreventionFlu caused by Influenza1
3CompletedTreatmentCommunity Acquired Infections / Infections, Gram-Positive Bacterial / Pneumonia, Pneumococcal1
3RecruitingTreatmentCritical Illness / Resistant Infection / Traumas1
3Unknown StatusTreatmentAcute / Conjunctivitis, Bacterial1
3Unknown StatusTreatmentHordeolum1
4CompletedBasic ScienceFlu caused by Influenza1
4CompletedPreventionFlu caused by Influenza1
4CompletedPreventionPostoperative Infections1
4CompletedTreatmentConjunctivitis1
4CompletedTreatmentFunctional Dyspepsia / Helicobacter Pylori / Peptic Ulcers1
4CompletedTreatmentHelicobacter Pylori Treatment Failure1
4CompletedTreatmentIndigestion / Peptic Ulcers1
4CompletedTreatmentPyelonephritis1
4CompletedTreatmentVertebral Osteomyelitis1
4RecruitingTreatmentHospital Infection1
4WithdrawnPreventionComplications; Breast Prosthesis, Infection or Inflammation1
Not AvailableCompletedNot AvailableDiverticulitis1
Not AvailableCompletedNot AvailablePenicillin Allergy1
Not AvailableCompletedPreventionInfection NOS1
Not AvailableCompletedTreatmentCorneal Diseases1
Not AvailableCompletedTreatmentDiverticulitis, Colonic1
Not AvailableCompletedTreatmentNasal Carriers of Staphylococcus Aureus1
Not AvailableCompletedTreatmentScleral Buckling1
Not AvailableEnrolling by InvitationTreatmentAppendicitis Acute1
Not AvailableRecruitingTreatmentLiver Cirrhosis / Small Intestinal Bacterial Overgrowth1
Not AvailableWithdrawnNot AvailableCystic Fibrosis (CF)1

Pharmacoeconomics

Manufacturers
  • Glaxosmithkline
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • X gen pharmaceuticals inc
  • Paddock laboratories inc
Packagers
  • Abraxis BioScience Inc.
  • Accutome Inc.
  • Advanced Pharmaceutical Services Inc.
  • AG Marin Pharmaceuticals
  • Akorn Inc.
  • Alba Pharmacal
  • Alcon Laboratories
  • A-S Medication Solutions LLC
  • Bausch & Lomb Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • C.O. Truxton Inc.
  • Carlisle Laboratories Inc.
  • Clipper Distributing Co. LLC
  • Darby Dental Supply Co. Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • DSM Corp.
  • E. Fougera and Co.
  • Eye Care and Cure Corp.
  • Eye Supply Usa Inc.
  • Falcon Pharmaceuticals Ltd.
  • Gonberetica
  • H and H Laboratories
  • H.J. Harkins Co. Inc.
  • Hurst Pharmaceutical
  • Keltman Pharmaceuticals Inc.
  • King Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Major Pharmaceuticals
  • Marlop Pharmaceuticals Inc.
  • Medisca Inc.
  • Monarch Pharmacy
  • MWI Veterinary Supply Co.
  • Nycomed Inc.
  • Ocusoft
  • OMJ Pharmaceuticals
  • Paddock Labs
  • Palmetto Pharmaceuticals Inc.
  • Pfizer Inc.
  • Pharmaforce Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Qualitest
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Rx Veterinary Products
  • Stat Rx Usa
  • Stat Scripts LLC
  • Teral Laboratories
  • Toku E Company
  • United Research Laboratories Inc.
  • Vedco Inc.
  • Wa Butler Co.
  • Watson Pharmaceuticals
  • Wilson Ophthalmic Corp.
  • X-Gen Pharmaceuticals
Dosage forms
FormRouteStrength
KitOral; Topical
Kit
KitTopical
Powder, for solutionIntramuscular; Intrathecal; Intravenous; Respiratory (inhalation); Topical500000 unit
Solution / dropsOphthalmic
Ointment; swabTopical
SolutionAuricular (otic)
SuspensionTopical
SwabTopical
LozengeBuccal
StickTopical
LiquidAuricular (otic)
SuspensionOphthalmic
SolutionIrrigation
Suspension / dropsAuricular (otic)
Suspension / dropsOphthalmic
SolutionAuricular (otic); Ophthalmic
IrrigantIrrigation
SolutionUrethral
OintmentOphthalmic
SuspensionAuricular (otic)
GelTopical
LiquidOphthalmic
LiquidAuricular (otic); Ophthalmic
InjectionIntramuscular; Intrathecal; Intravenous500000 1/1
Injection, powder, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [iU]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [iU]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 1/1
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous500000 [USP'U]/1
Injection, solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 1/1
Powder, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic50 mg
PowderTopical
CreamTopical
Solution / dropsAuricular (otic); Ophthalmic
Solution / dropsAuricular (otic)
OintmentOphthalmic; Topical
OintmentTopical
SolutionOphthalmic
LozengeOral
Prices
Unit descriptionCostUnit
Polymyxin b 100 million unit4039.2USD each
Polymyxin b sulfate vial13.65USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility25 mg/mLNot Available
logP-4.861Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0744 mg/mLALOGPS
logP-0.89ALOGPS
logP-7.2ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)11.57ChemAxon
pKa (Strongest Basic)10.23ChemAxon
Physiological Charge5ChemAxon
Hydrogen Acceptor Count18ChemAxon
Hydrogen Donor Count18ChemAxon
Polar Surface Area490.66 Å2ChemAxon
Rotatable Bond Count29ChemAxon
Refractivity313.22 m3·mol-1ChemAxon
Polarizability129.71 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.884
Blood Brain Barrier-0.9879
Caco-2 permeable-0.7581
P-glycoprotein substrateSubstrate0.8438
P-glycoprotein inhibitor INon-inhibitor0.8392
P-glycoprotein inhibitor IINon-inhibitor0.8657
Renal organic cation transporterNon-inhibitor0.9411
CYP450 2C9 substrateNon-substrate0.8693
CYP450 2D6 substrateNon-substrate0.7766
CYP450 3A4 substrateNon-substrate0.5151
CYP450 1A2 substrateNon-inhibitor0.9159
CYP450 2C9 inhibitorNon-inhibitor0.9365
CYP450 2D6 inhibitorNon-inhibitor0.9187
CYP450 2C19 inhibitorNon-inhibitor0.9012
CYP450 3A4 inhibitorNon-inhibitor0.6778
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9869
Ames testNon AMES toxic0.8798
CarcinogenicityNon-carcinogens0.8926
BiodegradationNot ready biodegradable0.9829
Rat acute toxicity3.0984 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9788
hERG inhibition (predictor II)Non-inhibitor0.7856
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.
Kingdom
Organic compounds
Super Class
Organic Polymers
Class
Polypeptides
Sub Class
Not Available
Direct Parent
Polypeptides
Alternative Parents
Cyclic peptides / N-acyl-alpha amino acids and derivatives / Macrolactams / Alpha amino acid amides / N-acyl amines / Benzene and substituted derivatives / Secondary carboxylic acid amides / Secondary alcohols / Lactams / Azacyclic compounds
show 5 more
Substituents
Polypeptide / Cyclic alpha peptide / Macrolactam / N-acyl-alpha amino acid or derivatives / Alpha-amino acid amide / N-substituted-alpha-amino acid / Alpha-amino acid or derivatives / Monocyclic benzene moiety / Fatty amide / N-acyl-amine
show 23 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Targets

1. Bacterial outer membrane
Kind
Group
Organism
Not Available
Pharmacological action
Yes
Actions
Incorporation into and destabilization
References
  1. Yuan Z, Tam VH: Polymyxin B: a new strategy for multidrug-resistant Gram-negative organisms. Expert Opin Investig Drugs. 2008 May;17(5):661-8. doi: 10.1517/13543784.17.5.661 . [PubMed:18447592]
  2. Zavascki AP, Goldani LZ, Li J, Nation RL: Polymyxin B for the treatment of multidrug-resistant pathogens: a critical review. J Antimicrob Chemother. 2007 Dec;60(6):1206-15. Epub 2007 Sep 17. [PubMed:17878146]

Drug created on June 13, 2005 07:24 / Updated on September 25, 2018 03:08