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Enmetazobactam
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Looking for Enmetazobactam API 1001404-83-6?
- Description:
- Here you will find a list of producers, manufacturers and distributors of Enmetazobactam. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
- API | Excipient name:
- Enmetazobactam
- Synonyms:
- (2s,3s,5r)-3-methyl-3-((3-methyltriazol-3-ium-1-yl)methyl)-4,4,7-trioxo-4^6-thia-1-azabicyclo(3.2.0)heptane-2-carboxylate , 1h-1,2,3-triazolium, 3-(((2s,3s,5r)-2-carboxy-3-methyl-4,4-dioxido-7-oxo-4-thia-1-azabicyclo(3.2.0)hept-3-yl)methyl)-1-methyl-, inner salt
- Cas Number:
- 1001404-83-6
- DrugBank number:
- DB18716
- Unique Ingredient Identifier:
- 80VUN7L00C
General Description:
Enmetazobactam, identified by CAS number 1001404-83-6, is a notable compound with significant therapeutic applications. Enmetazobactam is a penicillanic acid sulfone extended-spectrum beta (β)-lactamase (ESBL) inhibitor. Because ESBL enzymes can hydrolyze important antibiotics such as penicillins, broad-spectrum cephalosporins and monobactams, ESBL-producing bacteria poses challenges in the treatment of serious infections. The combination product of enmetazobactam and was first approved by the FDA on February 23, 2024, for the treatment of complicated urinary tract infections. Enmetazobactam is used as cefepime-sparing therapy by preventing its breakdown by ESBL.
Indications:
This drug is primarily indicated for: In combination with , enmetazobactam is indicated for the treatment of adults with complicated urinary tract infections (cUTI) including pyelonephritis caused by designated susceptible microorganisms. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Metabolism:
Enmetazobactam undergoes metabolic processing primarily in: Enmetazobactam is minimally metabolized. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.
Absorption:
The absorption characteristics of Enmetazobactam are crucial for its therapeutic efficacy: The mean (SD) Cmax is 19.8 (6.3) µg/mL in patients with cUTI and eGFR greater than or equal to 60 mL/min. The mean AUC0-last is 75.3 (30.8) μgxh/mL. The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Half-life:
The half-life of Enmetazobactam is an important consideration for its dosing schedule: The mean (SD) half-life is 2.6 (1.1) hours in patients with cUTI and eGFR greater than or equal to 60 mL/min. This determines the duration of action and helps in formulating effective dosing regimens.
Protein Binding:
Enmetazobactam exhibits a strong affinity for binding with plasma proteins: The percent protein binding of enmetazobactam is negligible. This property plays a key role in the drug's pharmacokinetics and distribution within the body.
Route of Elimination:
The elimination of Enmetazobactam from the body primarily occurs through: About 90% of enmetazobactam is excreted unchanged in urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.
Volume of Distribution:
Enmetazobactam is distributed throughout the body with a volume of distribution of: Mean (SD) steady state volume of distribution (Vss) is 25.26 (9.97) L in patients with cUTI and eGFR greater than or equal to 60 mL/min.. This metric indicates how extensively the drug permeates into body tissues.
Clearance:
The clearance rate of Enmetazobactam is a critical factor in determining its safe and effective dosage: The mean (SD) clearance is 7.6 (2.9) L/h in patients with cUTI and eGFR greater than or equal to 60 mL/min. It reflects the efficiency with which the drug is removed from the systemic circulation.
Pharmacodynamics:
Enmetazobactam exerts its therapeutic effects through: Enmetazobactam is an antibacterial agent that is active against most gram-positive and gram-negative bacteria. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Enmetazobactam functions by: Extended-spectrum beta-lactamases (ESBLs) are a group of bacterial serine beta-lactamases that hydrolyze third-generation cephalosporins (3GC), leading to the development of 3GC-resistant bacteria. When used in combination with cefepime, enmetazobactam protects cefepime from degradation by ESBLs and prevents antibiotic resistance. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Toxicity:
Categories:
Enmetazobactam is categorized under the following therapeutic classes: Anti-Bacterial Agents, Anti-Infective Agents, Aza Compounds, Beta-Lactam Antibacterials, beta-Lactamase Inhibitors, Cytochrome P-450 CYP2E1 Inhibitors, Cytochrome P-450 CYP2E1 Inhibitors (strength unknown), Cytochrome P-450 Enzyme Inhibitors, Enzyme Inhibitors, Extended-spectrum beta-lactamase inhibitors. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.
Enmetazobactam is a type of Anti-infective Agents
Anti-infective agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various infectious diseases. These agents play a crucial role in combating bacterial, viral, fungal, and parasitic infections. The demand for effective anti-infective APIs has grown significantly due to the increasing prevalence of drug-resistant microorganisms.
Anti-infective APIs encompass a wide range of substances, including antibiotics, antivirals, antifungals, and antiparasitics. Antibiotics are particularly important in fighting bacterial infections and are further categorized into different classes based on their mode of action and target bacteria. Antivirals are designed to inhibit viral replication and are essential in the treatment of viral infections such as influenza and HIV. Antifungals combat fungal infections, while antiparasitics are used to eliminate parasites that cause diseases like malaria and helminthiasis.
The development and production of high-quality anti-infective APIs require stringent manufacturing processes and adherence to regulatory standards. Pharmaceutical companies invest heavily in research and development to discover new and more effective anti-infective agents. Additionally, ensuring the safety, efficacy, and stability of these APIs is of utmost importance.
The global market for anti-infective APIs is driven by factors such as the rising incidence of infectious diseases, the emergence of new and drug-resistant pathogens, and the growing demand for improved healthcare infrastructure. Continuous advancements in pharmaceutical technology and the development of innovative drug delivery systems further contribute to the expansion of this market.
In conclusion, anti-infective agents are a critical category of pharmaceutical APIs that play a pivotal role in treating infectious diseases. Their effectiveness in combating various types of infections makes them essential components in the arsenal of modern medicine.
