Ceftaroline Fosamil
CAS: 229016-73-3
Category: Antibiotics
| Purity | Reagent Grade ≥95%, Standard Grade ≥98%, High-Purity Grade ≥99%, Pharmaceutical Grade ≥99.5% |
| Molecular Formula | C22H21N8O8PS4 |
| Molecular Weight | 684.68 |
| Appearance | White to pale yellowish-white crystalline powder or solid |
| Packaging | 5 mg/glass vial, 10 mg/glass vial, 25 mg/glass vial, 50 mg/glass vial, 100 mg/glass vial, 250 mg/glass vial, 1 g/glass vial, 5 g/glass vial, or 25 g/HDPE bottle |
| Testing Indicators | Appearance — Visual inspection (white to pale yellowish-white crystalline powder); Purity — HPLC-UV (≥95–99.5%, C18 column, acetonitrile:buffer gradient, λ=254 nm); Related substances — HPLC (impurity profiling including ceftaroline, des-fosamyl ceftaroline, and other degradation products); Assay — RP-HPLC (linearity validated, recovery 98.0–102.0%); Loss on drying — Gravimetric (≤3.0% for monoacetate monohydrate, corresponding to 1 mol H2O and 1 mol acetic acid); Residue on ignition — Gravimetric (≤0.1%); Heavy metals — Colorimetric/ICP-MS (≤20 ppm); Chloride content — Not applicable (inner salt/zwitterion); Identification — FTIR (characteristic peaks: beta-lactam C=O ~1780 cm⁻¹, amide C=O ~1670 cm⁻¹, C=N ~1600 cm⁻¹, P=O ~1200 cm⁻¹, P–O–C ~1050 cm⁻¹, thiazole ring ~1400 cm⁻¹, pyridinium C–H ~3100 cm⁻¹); ¹H NMR (DMSO-d₆: δ 1.20 ppm triplet CH₃CH₂O, δ 3.90 ppm quartet CH₂CH₂O, δ 4.20 ppm singlet N⁺–CH₃, δ 5.10 ppm doublet C6–H, δ 5.80 ppm doublet C7–H, δ 6.80–8.50 ppm multiplet aromatic/thiazole protons); Mass spectrometry — ESI-MS (m/z 685 [M+H]⁺ for inner salt; m/z 763 [M+H]⁺ for monoacetate monohydrate); Water content — Karl Fischer titration (EP 2.5.12, ~2.4% w/w for monohydrate); pH — Potentiometry (reconstituted solution pH 4.8–6.5 with L-arginine); Specific optical rotation — Polarimetry ([α]D ~+50 to +60°, c=1 in water); Sterility — Membrane filtration (EP 2.6.1/USP <71>); Bacterial endotoxins — LAL test (EP 2.6.14/USP <85>); Beta-lactam ring integrity — HPLC or bioassay. |
| Storage Notes | Store in a cool, dry, well-ventilated area at 2–8°C. Protect from light, moisture, and air. Keep container tightly sealed. Store powder at -20°C for long-term stability (up to 3 years); at 4°C for 2 years. Light-sensitive and hygroscopic material; avoid prolonged exposure to light and humid conditions. The anhydrous free acid form is not stable and is typically supplied as the monoacetate monohydrate salt (CAS 866021-48-9) or formulated with L-arginine for enhanced stability and solubility. Store away from strong oxidizing agents and incompatible substances. |
| Lead Time | 10 days |
Ceftaroline Fosamil is a semi-synthetic, broad-spectrum, N-phosphono prodrug of the cephalosporin class of beta-lactam antibiotics. It is rapidly converted in vivo to the microbiologically active ceftaroline (T-91825) by plasma phosphatases. It exhibits potent activity against both Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, and Citrobacter freundii. Used as a pharmaceutical intermediate, active pharmaceutical ingredient (API), and reference standard for the development and quality control of injectable formulations (e.g., Teflaro®/Zinforo®). Approved for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP). Also employed in analytical method development, method validation (AMV), forced degradation studies, and abbreviated new drug application (ANDA) support.