e-Drug3D

977

COLISTIMETHATE


INN
COLISTIMETHATE

(has an active metabolite)

cas 8068-28-8
CLASS

ANTIINFECTIVES
ANTIBACTERIAL
GRAM-NEGATIVE BACILLI

ROUTE (list)

INJECTION

ATC code

A07AA10
J01XB01

PK parameters

VD 5.8 LITER (65 KILOGRAM)
Cl 13.7 LITER / HOUR (PMID19433570)
t1/2 2.5 HOUR

Target

TARGET MEMBRANE

DrugCentral

CELL MEMBRANE INHIBITOR CHEMBL2364031 CELL MEMBRANE BACTERIA

Download SDF file pentasodium [[4-[[3-hydroxy-1-[[1-[[3-(1-hydroxyethyl)-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-6,9,18-tris[2-(sulfonatomethylamino)ethyl]-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]-1-oxo-4-(sulfonatomethylamino)butan-2-yl]amino]-1-oxobutan-2-yl]amino]-3-(6-methyloctanoylamino)-4-oxobutyl]amino]methanesulfonate

Formula:
C57H108N16O28S5

Calculated chemical properties:

MW 1625.94
NB_atoms 106
XLogP -8.45
PSA 675.784
NB_HD 23
NB_HA 44
fsp3 0.81
Lipinski(0=no;1=yes) 0

FDA
NDA 050108 (label) INN (COLISTIMETHATE SODIUM) COLY-MYCIN M (PH HEALTH) APPROVAL= AP YEAR= 1970 DISCONTINUED
NDA 064216 (pdf not found) INN (COLISTIMETHATE SODIUM) COLISTIMETHATE SODIUM (PHARMOBEDIENT) APPROVAL= AP YEAR= 1999 DISCONTINUED
NDA 065177 (pdf not found) INN (COLISTIMETHATE SODIUM) COLISTIMETHATE SODIUM (NEXUS) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 065364 (pdf not found) INN (COLISTIMETHATE SODIUM) COLISTIMETHATE SODIUM (FRESENIUS KABI USA) APPROVAL= AP YEAR= 2008
NDA 202359 (pdf not found) INN (COLISTIMETHATE SODIUM) COLISTIMETHATE SODIUM (AVET LIFESCIENCES) APPROVAL= AP YEAR= 2012
NDA 201365 (pdf not found) INN (COLISTIMETHATE SODIUM) COLISTIMETHATE SODIUM (SAGENT PHARMS INC) APPROVAL= AP YEAR= 2014
NDA 205356 (pdf not found) INN (COLISTIMETHATE SODIUM) COLISTIMETHATE SODIUM (XELLIA PHARMS APS) APPROVAL= AP YEAR= 2015

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1312

COLISTIN


INN
COLISTIN

(is an active metabolite)

cas 1066-17-7
CLASS

ANTIINFECTIVES
ANTIBIOTIC
ANTIBACTERIAL
POLYMYXIN E
DISRUPTS THE BACTERIAL CELL MEMBRANE

ROUTE (list)

ORAL OTIC

ATC code

A07AA10
J01XB01

PK parameters

Cmax 1.99 MICROMOLAR (PMID19433570)
VD 189 LITER (PMID19433570)
Cl 13.7 LITER / HOUR (PMID19433570)
t1/2 14.4 HOUR (PMID19433570)

Target

TARGET MEMBRANE

DrugCentral

Unknown

Download SDF file N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-3-(1-hydroxyethyl)-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-5-methylheptanamide

Formula:
C52H98N16O13

Calculated chemical properties:

MW 1155.46
NB_atoms 81
XLogP -5.83
PSA 443.846
NB_HD 23
NB_HA 29
fsp3 0.79
Lipinski(0=no;1=yes) 0

FDA
NDA 050355 (pdf not found) INN (COLISTIN SULFATE) COLY-MYCIN S (PARKE DAVIS) APPROVAL= - YEAR= 0 DISCONTINUED
NDA 050356 (label) INN (COLISTIN SULFATE ; HYDROCORTISONE ACETATE ; NEOMYCIN SULFATE ; THONZONIUM BROMIDE) COLY-MYCIN S (PH HEALTH) APPROVAL= AP YEAR= 1962

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL