Biomaterial Database

Imipenem/Cilastatin/Relebactam: A Review in Gram-Negative Bacterial Infections. 2021

Young-A Heo

Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. demail@springer.com.

Imipenem/cilastatin/relebactam (Recarbrio™) is an intravenously administered combination of the carbapenem imipenem, the renal dehydropeptidase-I inhibitor cilastatin, and the novel β-lactamase inhibitor relebactam. Relebactam is a potent inhibitor of class A and class C β-lactamases, conferring imipenem activity against many imipenem-nonsusceptible strains. Imipenem/cilastatin/relebactam is approved in the USA and EU for the treatment of hospital-acquired bacterial pneumonia (HABP) and ventilator-associated bacterial pneumonia (VABP) in adults and other gram-negative infections, including complicated urinary tract infections (cUTIs) [including pyelonephritis] and complicated intra-abdominal infections (cIAIs), in adults with limited or no alternative treatment options. In pivotal phase II and III trials, imipenem/cilastatin/relebactam was noninferior to piperacillin/tazobactam in patients with HABP/VABP and to imipenem/cilastatin in patients with cUTIs and cIAIs. It was also effective in imipenem-nonsusceptible infections. Imipenem/cilastatin/relebactam was generally well tolerated, with a safety profile consistent with that of imipenem/cilastatin. Available evidence indicates that imipenem/cilastatin/relebactam is an effective and generally well tolerated option for gram-negative infections in adults, including critically ill and/or high-risk patients, and a potential therapy for infections caused by carbapenem-resistant pathogens.

UI	MeSH Term	Description	Entries
D007275	Injections, Intravenous	Injections made into a vein for therapeutic or experimental purposes.	Intravenous Injections,Injection, Intravenous,Intravenous Injection
D004338	Drug Combinations	Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.	Drug Combination,Combination, Drug,Combinations, Drug
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000900	Anti-Bacterial Agents	Substances that inhibit the growth or reproduction of BACTERIA.	Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D001618	beta-Lactamases	Enzymes found in many bacteria which catalyze the hydrolysis of the amide bond in the beta-lactam ring. Well known antibiotics destroyed by these enzymes are penicillins and cephalosporins.	beta-Lactamase,beta Lactamase,beta Lactamases
D015377	Cilastatin	A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.	Cilastatin Monosodium Salt,Cilastatin Sodium,MK 0791,MK-791,MK0791,MK 791,MK791,Monosodium Salt, Cilastatin,Salt, Cilastatin Monosodium,Sodium, Cilastatin
D015378	Imipenem	Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.	Imipemide,N-Formimidoylthienamycin,Imipenem Anhydrous,Imipenem, Anhydrous,MK-0787,MK0787,Anhydrous Imipenem,Anhydrous, Imipenem,MK 0787,N Formimidoylthienamycin
D016905	Gram-Negative Bacterial Infections	Infections caused by bacteria that show up as pink (negative) when treated by the gram-staining method.	Bacterial Infections, Gram-Negative,Infections, Gram-Negative Bacterial,Bacterial Infection, Gram-Negative,Gram Negative Bacterial Infections,Gram-Negative Bacterial Infection,Infection, Gram-Negative Bacterial
D053961	Azabicyclo Compounds	Bicyclic bridged compounds that contain a nitrogen which has three bonds. The nomenclature indicates the number of atoms in each path around the rings, such as [2.2.2] for three equal length paths. Some members are TROPANES and BETA LACTAMS.	Azabicyclo(1.1.0)Butanes,Azabicyclo(2.2.2)Octanes,Azabicyclo(3.3.1)Nonanes,Azabicyclo(4.3.0)Nonanes,Azabicyclo(5.2.2)Undecanes
D065093	beta-Lactamase Inhibitors	Endogenous substances and drugs that inhibit or block the activity of BETA-LACTAMASES.	beta Lactamase Inhibitor,beta Lactamase Inhibitors,beta-Lactamase Inhibitor,beta Lactamase Antagonists,Antagonists, beta Lactamase,Inhibitor, beta Lactamase,Inhibitor, beta-Lactamase,Inhibitors, beta Lactamase,Inhibitors, beta-Lactamase,Lactamase Antagonists, beta,Lactamase Inhibitor, beta,Lactamase Inhibitors, beta