Relebactam API Manufacturers

General Description:

Relebactam, identified by CAS number 1174018-99-5, is a notable compound with significant therapeutic applications. Relebactam is a diazabicyclooctane beta-lactamase inhibitor, similar in structure to . It includes a piperidine ring which reduces export from bacterial cells by producing a positive charge. It is currently available in a combination product which includes and to treat complicated urinary tract infections (UTIs), pyelonephritis, and complicated intra-abdominal infections in adults. It is considered to be a last-line treatment option and gained FDA approval as part of the combination product RecarbrioⓇ in July 2019.

Indications:

This drug is primarily indicated for: Relebactam is indicated in combination with and for the treatment of complicated urinary tract infections (including pyelonephritis), and complicated intra-abdominal infections caused by susceptible organisms in adults. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Relebactam undergoes metabolic processing primarily in: Relebactam does not undergo significant metabolism and can be found mostly unchanged in human plasma. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Relebactam are crucial for its therapeutic efficacy: Currently, relebactam is only available as an intravenous product; therefore, there is no relevant absorption data in the literature. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Relebactam is an important consideration for its dosing schedule: Relebactam has a half-life of 1.2 hours as per official FDA labeling. Values reported in pharmacokinetic studies vary from 1.35-1.8 hours. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Relebactam exhibits a strong affinity for binding with plasma proteins: Relebactam is approximately 22% plasma protein bound. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Relebactam from the body primarily occurs through: Approximately 90-100% of relebactam is renally eliminated. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Relebactam is distributed throughout the body with a volume of distribution of: Relebactam has a volume of distribution of approximately 19 L with both single and steady state dosing. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Relebactam is a critical factor in determining its safe and effective dosage: Relebactam has a reported total clearance of approximately 130-150 mL/min (8 L/h). About 30% of the total drug clearance can be attributed to active tubular secretion. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Relebactam exerts its therapeutic effects through: Relebactam prevents the hydrolysis of , allowing it to exert its bactericidal effect. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Relebactam functions by: Relebactam is a beta-lactamase inhibitor known to inhibit many types of beta-lactamases including Ambler class A and Ambler class C enzymes, helping to prevent from degrading in the body. Similar to the structurally-related , first, relebactam binds non-covalently to a beta-lactamase binding site, then, it covalently acylates the serine residue in the active site of the enzyme. In contrast to some other beta-lactamase inhibitors, once relebactam de-acylates from the active site, it can reform it's 5 membered ring and is capable of rebinding to target enzymes. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Relebactam belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids, classified under the direct parent group Alpha amino acid amides. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Amino acids, peptides, and analogues subclass.

Categories:

Relebactam is categorized under the following therapeutic classes: Antibacterials for Systemic Use, Antiinfectives for Systemic Use, Aza Compounds, beta-Lactamase Inhibitors, Enzyme Inhibitors, MATE 1 Substrates, MATE 2 Substrates, MATE substrates, OAT3/SLC22A8 Substrates. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.