[CAS NO. 117467-28-4] CefditorenPivoxil
PRODUCTS SPECIFICATIONS [117467-28-4]
DESCRIPTION [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 |
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 |
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
DMSO : ≥ 100 mg/mL ( 161.10 mM )
* "≥" means soluble, but saturation unknown.
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 |
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
