| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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Cefixime (FR-17027; Unixime; Cefiximum; Cefixima; FK-027; CL-284635) is a novel and potent third generation cephalosporin antibiotic with activity against a variety of Gram-negative bacteria, including E. coli, K. pneumoniae, and H. influenzae. Cefixime binds to penicillin-binding proteins and is stable to many penicillinases and β-lactamases. It is an effective, orally-active cephalosporin with applications in acute otitis media, respiratory tract infections, and urinary tract infections.
| Targets |
β-lactam
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|---|---|
| ln Vitro |
With a MIC90 value of 0.25 μg/mL, cefixime exhibits strong antibacterial activity against clinical isolates of Salmonella typhi. It also exhibits antibacterial activity against strains that are resistant to amoxicillin (HY-B0467A) and produce β-lactamase.
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| ln Vivo |
Mice challenged with FA1090 (ESC-susceptible strain) have lower bacterial burdens when cefixime (0.75–60 mg/kg) is administered orally[4].
Cefixime (50 or 150 mg/kg, oral gavage) alters the composition and diversity of the C57BL/6J mice's gut microbiota, resulting in a decrease in the microbial community's diversity and a shift toward a predominate Firmicutes phylum[5].
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| Animal Protocol |
Pharmacokinetic (PK) Study Protocol:** Uninfected, estradiol-treated female BALB/c mice were administered a single oral dose of cefixime at concentrations ranging from 0.19 to 120 mg/kg. Venous blood samples were collected from the retro-orbital sinus at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 hours post-dose. Blood was collected from each mouse at two time points (n=4 mice/time point). Samples were processed to K3EDTA plasma and stored at ≤ -70°C until analysis by liquid chromatography-tandem mass spectrometry (LC-MS/MS) to determine cefixime concentrations [4].
* **In Vivo Efficacy Study Protocol (Susceptible Strain):** Female BALB/c mice were implanted with a 17β-estradiol pellet and treated with antibiotics to promote gonococcal infection. Mice were then inoculated vaginally with *N. gonorrhoeae* strain FA1090. On day 0 post-inoculation, a single dose of cefixime (0.19, 0.75, 3, 12, or 60 mg/kg) was administered by oral gavage. Cefixime was prepared in sterile endotoxin-free PBS (pH 6.0) with 0.1M NaHCO3 (1:10). Infection was monitored for 8 days post-treatment by daily quantitative culture of vaginal swab specimens [4]. * **In Vivo Efficacy Study Protocol (Resistant Strain):** Using the same mouse model, mice were inoculated with the resistant strain H041. Cefixime was administered by oral gavage in various fractionated dosing regimens over 24 hours to attempt to achieve therapeutic times above the elevated MIC (8 μg/ml). Regimens tested included single doses (QD) of 120 mg/kg and 300 mg/kg, two doses (BID, every 12 hours) of 60 mg/kg and 150 mg/kg, and three doses (TID, every 8 hours) of 40 mg/kg and 100 mg/kg. Gentamicin (i.p., 48 mg/kg, 5 doses, QD) was used as a positive control. Infection was monitored for 8 days post-treatment by daily quantitative culture of vaginal swab specimens [4]. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Oral cefixime, whether taken on an empty stomach or with food, has an absorption rate of approximately 40%-50%. However, when taken with food, the time to peak concentration is prolonged by about 0.8 hours. In healthy male volunteers, a single oral dose of 200 mg cefixime tablets resulted in a peak plasma concentration (Cmax) of 3.25 mg/L and a time to peak concentration (Tmax) of 4 hours. In healthy volunteers, an oral dose of 200 mg cefixime solution resulted in a peak plasma concentration (Cmax) of 3.22 μg/mL; while doses of 200 mg and 400 mg cefixime capsules resulted in peak plasma concentrations (Cmax) of 2.92 μg/mL and 4.84 μg/mL, respectively. Following administration of cefixime via 200 mg intravenous injection, 200 mg oral solution, 200 mg capsules, and 400 mg capsules, the mean area under the curve (AUC) was 47.0 μg·h/mL, 26.0 μg·h/mL, 23.6 μg·h/mL, and 39.4 μg·h/mL, respectively. Approximately 50% of absorbed cefixime is excreted unchanged in the urine within 24 hours. The mean volume of distribution of orally administered cefixime is 0.1 L/kg body weight. In children aged 6 to 13 years with urinary tract infections, the mean apparent total clearance of cefixime suspension administered orally at a dose of 8 mg/kg was 4.74 ml/min/kg. Metabolites/Metabolites: There is currently no evidence that cefixime is metabolized in the body. Biological Half-Life The average serum half-life of cefixime in healthy subjects is 3 to 4 hours, regardless of dosage form. In some healthy volunteers, the half-life can reach 9 hours. In patients with severe renal impairment (creatinine clearance of 5 to 20 mL/min), the average half-life of cefixime is prolonged to 11.5 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation While there is currently no information regarding the use of cefixime during lactation, it is generally believed that cephalosporins do not have adverse effects on breastfed infants. There are reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Cefixime is safe for use by breastfeeding women. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Protein Binding Approximately 65% of cefixime binds to serum proteins, and the serum protein binding rate is independent of drug concentration. |
| References |
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| Additional Infomation |
Pharmacodynamics
Cefixime is a broad-spectrum antibiotic, belonging to the class of orally effective third-generation semi-synthetic cephalosporins. Like other cephalosporins, cefixime's antibacterial action derives from the inhibition of cell wall synthesis. Also like other cephalosporins, cefixime remains stable in the presence of certain β-lactamases, meaning that some microorganisms resistant to penicillin and some cephalosporins due to the presence of β-lactamases may be sensitive to cefixime. Use of cefixime may cause hypersensitivity reactions, including anaphylactic/hypersensitivity reactions and Clostridium difficile-associated diarrhea (CDAD); it may also cause a decrease in prothrombin activity. The dosage of cefixime should be adjusted in patients with impaired renal function, as well as those undergoing continuous ambulatory peritoneal dialysis (CAPD) and hemodialysis (HD); patients undergoing dialysis should be monitored while taking cefixime. |
| Molecular Formula |
C16H15N5O7S2
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|---|---|
| Molecular Weight |
453.45
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| Exact Mass |
453.041
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| Elemental Analysis |
C, 42.38; H, 3.33; N, 15.44; O, 24.70; S, 14.14
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| CAS # |
79350-37-1
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| Related CAS # |
Cefixime trihydrate;125110-14-7
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| PubChem CID |
5362065
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| Appearance |
Off-white to slightly yellow solid powder.
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| Density |
1.9±0.1 g/cm3
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| Melting Point |
218-225°C
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| Index of Refraction |
1.811
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| LogP |
1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
861
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(C1=C(C=C)CS[C@@H]2[C@@H](C(N12)=O)NC(=O)/C(/C1=CSC(N)=N1)=N\OCC(=O)O)(=O)O
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| InChi Key |
OKBVVJOGVLARMR-VINNURBNSA-N
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| InChi Code |
InChI=1S/C16H15N5O7S2/c1-2-6-4-29-14-10(13(25)21(14)11(6)15(26)27)19-12(24)9(20-28-3-8(22)23)7-5-30-16(17)18-7/h2,5,10,14H,1,3-4H2,(H2,17,18)(H,19,24)(H,22,23)(H,26,27)/b20-9+/t10-,14-/m1/s1
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| Chemical Name |
(6R,7R)-7-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-(carboxymethoxyimino)acetyl]amino]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
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| Synonyms |
Cefixima; FR17027; Suprax; Trihydrate, Cefixime; FK 027; FK-027; FK027; FR 17027; FR-17027;Cefixim; Cefixoral; Unixime; Cefiximum;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 90~100 mg/mL ( 198.47~220.53 mM )
Ethanol : ~1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (5.51 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2053 mL | 11.0266 mL | 22.0531 mL | |
| 5 mM | 0.4411 mL | 2.2053 mL | 4.4106 mL | |
| 10 mM | 0.2205 mL | 1.1027 mL | 2.2053 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04958122 | RECRUITING | Drug: Cefixime 400mg Drug: benzathine penicillin |
Human Immunodeficiency Virus Syphilis |
University of Southern California | 2021-06-20 | Phase 3 |
| NCT02708992 | COMPLETED | Drug: Azithromycin Drug: Cefixime |
Gonorrhoea | National Institute of Allergy and Infectious Diseases (NIAID) | 2016-04-28 | Phase 1 |
| NCT03660488 | COMPLETEDWITH RESULTS | Drug: Cefixime 400 milligram Oral Capsule [Suprax] Drug: Benzathine Penicillin G |
Early Syphilis Syphilis |
University of California, Los Angeles | 2018-09-03 | Phase 2 |
| NCT03329547 | WITHDRAWN | Drug: Cefixime test capsule Drug: Cefixime reference capsule |
Infections, Bacterial | GlaxoSmithKline | 2018-01-11 | Phase 1 |
| NCT04982861 | COMPLETED | Drug: Cefixime Trihydrate 100 mg/5 mL Dry Syrup Drug: Suprax 100 MG in 5 mL Oral Suspension |
Drug Use | PT Bernofarm | 2020-06-15 | Not Applicable |
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