Eravacycline API Manufacturers

General Description:

Eravacycline, identified by CAS number 1207283-85-9, is a notable compound with significant therapeutic applications. Eravacycline, known as _Xerava_ by Tetraphase Pharmaceuticals, is a fully synthetic fluorocycline antibiotic of the tetracycline class with activity against clinically significant gram-negative, gram-positive aerobic, and facultative bacteria. This includes most of those bacteria resistant to cephalosporins, fluoroquinolones, β-lactam/β-lactamase inhibitors, multidrug-resistant strains, and carbapenem-resistant Enterobacteriaceae, and the majority of anaerobic pathogens . It was first approved by the FDA on August 27, 2018 . Eravacycline has demonstrated superior potency to that of antibiotics that are currently being marketed for intraabdominal infections .

Indications:

This drug is primarily indicated for: Eravacycline is a tetracycline class antibacterial indicated for the treatment of complicated intra-abdominal infections in patients 18 years of age and older . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Eravacycline undergoes metabolic processing primarily in: Eravacycline is metabolized primarily by CYP3A4- and FMO-mediated oxidation . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Eravacycline are crucial for its therapeutic efficacy: Following single-dose intravenous administration, eravacycline AUC (area under the curve) and Cmax (maximum concentration) increase dose-proportionally for doses from 1 mg/kg - 3 mg/kg (3 times the approved dose). There is approximately 45% accumulation following intravenous dosing of 1 mg/kg every 12 hours . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Eravacycline is an important consideration for its dosing schedule: The mean elimination half-life is 20 hours . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Eravacycline exhibits a strong affinity for binding with plasma proteins: Protein binding of eravacycline to human plasma proteins increases with increasing plasma concentrations, with 79% to 90% (bound) at plasma concentrations ranging from 100 to 10,000 ng/mL . This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Eravacycline from the body primarily occurs through: Following a single intravenous dose of radiolabeled eravacycline 60 mg, approximately 34% of the dose is excreted in urine and 47% in feces as unchanged eravacycline (20% in urine and 17% in feces) and metabolites . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Eravacycline is distributed throughout the body with a volume of distribution of: The volume of distribution at steady-state is approximately 321 L . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Eravacycline is a critical factor in determining its safe and effective dosage: 17.82 L/min (standard deviation of 3.4) . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Eravacycline exerts its therapeutic effects through: Eravacycline is an antibiotic that disrupts bacterial protein synthesis, treating complicated intraabdominal infections . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Eravacycline functions by: Eravacycline is a fluorocycline antibacterial of the tetracycline class of antibacterial drugs. Eravacycline disrupts bacterial protein synthesis by binding to the 30S ribosomal subunit, preventing the incorporation of amino acid residues into elongating peptide chains. In general, eravacycline is bacteriostatic against gram-positive bacteria (e.g, Staphylococcus aureus and Enterococcus faecalis); however, in vitro bactericidal activity has been shown against certain strains of Escherichia coli and Klebsiella pneumoniae . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Eravacycline belongs to the class of organic compounds known as tetracyclines. These are polyketides having an octahydrotetracene-2-carboxamide skeleton, substituted with many hydroxy and other groups, classified under the direct parent group Tetracyclines. This compound is a part of the Organic compounds, falling under the Phenylpropanoids and polyketides superclass, and categorized within the Tetracyclines class, specifically within the None subclass.

Categories:

Eravacycline is categorized under the following therapeutic classes: Anti-Bacterial Agents, Antibacterials for Systemic Use, Antiinfectives for Systemic Use, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 Substrates, Monoamine Oxidase A Substrates, Naphthacenes, Tetracyclines. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.