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[CAS NO. 117467-28-4] CefditorenPivoxil

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Catalog:	HY-17452A
Brand:	MCE
CAS:	117467-28-4

Overview

MDL	MFCD00933166
Molecular Weight	620.72
Molecular Formula	C25H28N6O7S3
SMILES	O=C(C(N12)=C(/C=C\C3=C(C)N=CS3)CS[C@]2([H])[C@H](NC(/C(C4=CSC(N)=N4)=N\OC)=O)C1=O)OCOC(C(C)(C)C)=O

For research use only. We do not sell to patients.

Summary

Cefditoren Pivoxil (ME 1207) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren Pivoxil has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren Pivoxil can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections ^[1] ^[2] .

In Vitro

Cefditoren (Pivoxil) shows good activity against pneumoniae , S. pyogenes , Staphylococcus aureus , H. influenzae and H. parainfluenzae , M. catarrhalis ^[1] .

Organism	MIC50 (mg/L)	MIC90 (mg/L)	susceptible (%)
Gram-positive organisms
Streptococcus pneumoniae (untyped) ^a	0.015-0.25	0.12-1
PS	≤0.008-0.03	0.015-0.25	99-100
PI	0.06-0.5	0.25-0.5	94-100
PR	0.25-1	0.5-2	7-100
S. pyogenes	≤0.008-0.03	0.015-0.03	100
Staphylococcus aureus (MS)	0.12-0.5	0.5-1	50-100
Gram-negative organisms
Haemophilus	≤0.008-≤0.03	0.015-0.13
influenzae (untyped) ^b
β-Lactamase +	≤0.008-0.03	0.015-0.06	100
β-Lactamase -	≤0.008-0.03	0.015-0.06	100
H. parainfluenzae ^b	≤0.03	0.06
Moraxella	0.03-0.5	0.25-1	96
catarrhalis (untyped) ^b
β-Lactamase +	≤0.03-0.25	0.12-0.5	100
β-Lactamase -	≤0.008-0.03	0.015-0.06	100

^a Including PS, PI and PR strains.
^b Including both β-lactamase-positive and -negative strains.
MIC _50/90 =mean minimum inhibitory concentrations required to inhibit the growth of 50% or 90% of bacterial strains; MS =susceptible to meticillin; PI =intermediate susceptibility to penicillin; PR =resistant to penicillin; PS =susceptible to penicillin.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pharmacokinetics in mice ^[1] ：

Cefditoren (mg/kg)	C ₀ (µg/ml)	t1/2 (h)	AUC _last (µg× h/ml)	T _last (h)
6.25	53.0	0.9	30.4	6
12.5	168.4	1.1	64.1	8
25	232.5	0.9	101.3	8
50	290.6	1.1	124.4	8

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01553006	Thammasat University	Rhinosinusitis	January 2012	Phase 4
NCT04709172	Meiji Pharma Spain S.A.	COVID-19 Pneumonia	January 5, 2021	Phase 4
NCT00598403	Tedec-Meiji Farma, S.A.	Urinary Tract Infections	November 2007	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 161.10 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6110 mL	8.0552 mL	16.1103 mL
5 mM	0.3222 mL	1.6110 mL	3.2221 mL
10 mM	0.1611 mL	0.8055 mL	1.6110 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Wellington K, et al. Cefditoren pivoxil: a review of its use in the treatment of bacterial infections. Drugs. 2004;64(22):2597-618.
[2] Cafini F, et al. Enhanced in vivo activity of cefditoren in pre-immunized mice against penicillin-resistant S. pneumoniae (serotypes 6B, 19F and 23F) in a sepsis model. PLoS One. 2010 Aug 10;5(8):e12041.

Synonyms

5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetyl]amino]-3-[(1Z)-2-(4-methyl-5-thiazolyl)ethenyl]-8-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester, (6R,7R)-

5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[2-(4-methyl-5-thiazolyl)ethenyl]-8-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester, [6R-[3(Z),6α,7β(Z)]]-

5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2Z)-(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[(1Z)-2-(4-methyl-5-thiazolyl)ethenyl]-8-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester, (6R,7R)-

ME 1207

Cefditoren pivoxil

Cefditoren pivoxyl

Meiact

Spectracef

CCRIS 7768

Cefditoren pivaloyloxymethyl ester

Cefditorin

Zostum-O

Cefditran

Ceftorin

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