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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H22N8O6S2.H2O4S
Molecular Weight 620.636
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of CEFOSELIS SULFATE

SMILES

OS(O)(=O)=O.CO\N=C(/C(=O)N[C@H]1[C@H]2SCC(CN3C=CC(=N)N3CCO)=C(N2C1=O)C(O)=O)C4=CSC(N)=N4

InChI

InChIKey=LZOLCSVRFKCSEM-ZQCAECPKSA-N
InChI=1S/C19H22N8O6S2.H2O4S/c1-33-24-12(10-8-35-19(21)22-10)15(29)23-13-16(30)27-14(18(31)32)9(7-34-17(13)27)6-25-3-2-11(20)26(25)4-5-28;1-5(2,3)4/h2-3,8,13,17,20,28H,4-7H2,1H3,(H2,21,22)(H,23,29)(H,31,32);(H2,1,2,3,4)/b20-11?,24-12-;/t13-,17-;/m1./s1

HIDE SMILES / InChI

Description

Cefoselis sulphate is a new parenteral cephalosporin, which was launched into therapy in Japan on 9 September, 1998, under the brand name Wincef. Cefoselis sulphate, like all the other beta-lactams, exhibits its bactericidal eff ects by binding to penicillinbinding proteins. It has a spectrum of activity that covers aerobic and anaerobic gram-positive and gram-negative bacteria. Cefoselis sulphate has been approved to treat infections caused by Staphylococcus and Pseudomonas especially respiratory and urinary tract infections. The recommended dose of cefoselis is 1 g twice a day as an intravenous infusion. The duration of therapy is from 5 to 14 days. Cefoselis sulfate has a potent antibacterial activity against Gram-positive bacteria involving Staphylococcus, Pneumococcus, and Streptococcus, as well as Gram-negative bacteria involving Pseudomonas, Escherichia coli, Klebsiella, Enterobacter, Serratia, Proteus, Morganella, and Providencia.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
185.0 mM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Wincef
Curative
Wincef

Cmax

ValueDoseCo-administeredAnalytePopulation
83.8 μg/mL
1 g single, oral
CEFOSELIS plasma
Homo sapiens
142.6 μg/mL
2 g single, oral
CEFOSELIS plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
159.7 μg × h/mL
1 g single, oral
CEFOSELIS plasma
Homo sapiens
303.7 μg × h/mL
2 g single, oral
CEFOSELIS plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
2 h
1 g single, oral
CEFOSELIS plasma
Homo sapiens
2 h
2 g single, oral
CEFOSELIS plasma
Homo sapiens

Doses

PubMed

Sample Use Guides

In Vivo Use Guide
1.0 g of for moderate infection or 2.0 g intravenous infusion for severe infection administered at an interval of 12 hours for 7 to 14 days
Route of Administration: Intravenous
In Vitro Use Guide
Cefoselis sulphate inhibited methicillin-susceptible staphylocci at < or = 4 ug/ml. Of 98 isolates of homogenous methicillin-resistant Staphylococcus aureus, 55 (56.1%) were inhibited by 8 ug of FK-037 per ml