Delafloxacin API Manufacturers

General Description:

Delafloxacin, identified by CAS number 189279-58-1, is a notable compound with significant therapeutic applications. Delafloxacin is a fluoroquinolone antibiotic which has been used in trials studying the treatment and basic science of Gonorrhea, Hepatic Impairment, Bacterial Skin Diseases, Skin Structure Infections, and Community Acquired Pneumonia, among others. It was approved in June 2017 under the trade name Baxdela for use in the treatment of acute bacterial skin and skin structure infections.

Indications:

This drug is primarily indicated for: Delafloxacin is indicated for the treatment of acute bacterial skin and skin structure infections caused by the Gram-positive organisms Staphylococcus aureus (including methicillin-resistant and methicillin-susceptible isolates), Staphylococcus haemolyticus, Staphylococcus lugdunensis, Streptococcus agalactiae, Streptococcus anginosus Group (including Streptococcus anginosus, Streptococcus intermedius, and Streptococcus constellatus), Streptococcus pyogenes, and Enterococcus faecalis as well as the Gram-negative organisms Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, and Pseudomonas aeruginosa . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Delafloxacin undergoes metabolic processing primarily in: Delafoxacin is primarily metabolized via glucuronidation mediated by UDP glucuronosyltransferase 1-1, UDP-glucuronosyltransferase 1-3, and UDP-glucuronosyltransferase 2B15 . Less than 1% is metabolized via oxidation. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Delafloxacin are crucial for its therapeutic efficacy: The median time to peak plasma concentration for orally administered Delafloxacin is 0.75 (0.5-4.0) hours after a single dose and 1.00 (0.5-6.0) hours for steady state dosing . The median time to peak plasma concentration for intravenously administered Delafloxacin is 1.00 (1.0-1.2) hours for a single dose and 1.0 (1.0-1.0) hour for steady state dosing. The absolute bioavailability for orally administed Delafloxacin is 58.8%. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Delafloxacin is an important consideration for its dosing schedule: The mean half life of elimination of Delafloxacin is 3.7 hours after a single intravenous administration . The mean half life of elimination for multple oral administrations is 4.2-8.5 hours. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Delafloxacin exhibits a strong affinity for binding with plasma proteins: Delafloxacin is 84% bound to human plasma proteins . It primarily binds to serum albumin. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Delafloxacin from the body primarily occurs through: After a single intravenous dose, 65% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 28% excreted unchanged in the feces . After a single oral dose, 50% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 48% excreted unchanged in the feces. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Delafloxacin is distributed throughout the body with a volume of distribution of: The steady sate volume of distrubution of Delafloxacin is 30-48 liters . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Delafloxacin is a critical factor in determining its safe and effective dosage: The mean total clearance of Delafloxacin is 16.3 liters per hour . Renal clearance accounts for 35-45% of total clearance. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Delafloxacin exerts its therapeutic effects through: Delafloxacin is a fluoroquinolone antibacterial drug which kills bacterial cells . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Delafloxacin functions by: Delafloxacin inhibits the activity of bacterial DNA topoisomerase IV and DNA gyrase (topoisomerase II) . This interferes with bacterial DNA replication by preventing the relaxation of positive supercoils introduced as part of the elongation process . The resultant strain inhibits further elongation. Delafloxacin exerts concentration-dependent bacteriocidal activity . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Delafloxacin belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions, classified under the direct parent group Quinoline carboxylic acids. This compound is a part of the Organic compounds, falling under the Organoheterocyclic compounds superclass, and categorized within the Quinolines and derivatives class, specifically within the Quinoline carboxylic acids subclass.

Categories:

Delafloxacin is categorized under the following therapeutic classes: Anti-Bacterial Agents, Anti-Infective Agents, Antibacterials for Systemic Use, Antiinfectives for Systemic Use, BCRP/ABCG2 Substrates, Cytochrome P-450 CYP2C9 Inducers, Cytochrome P-450 CYP2C9 Inducers (weak), Cytochrome P-450 CYP2E1 Inducers, Cytochrome P-450 CYP2E1 Inducers (weak), Cytochrome P-450 CYP3A Inducers, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (weak), Cytochrome P-450 Enzyme Inducers, Drugs that are Mainly Renally Excreted, Fluoroquinolone Antibacterial, Fluoroquinolones, Heterocyclic Compounds, Fused-Ring, Potential QTc-Prolonging Agents, QTc Prolonging Agents, Quinolines, Quinolones, UGT1A1 Substrates, UGT1A3 substrates. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.