Tebipenem pivoxil, sold under the brand name Orapenem among others, is a beta-lactam antibiotic medication used for the treatment of complicated urinary tract infections, including pyelonephritis. It is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of beta-lactam antibiotics. It was developed as a novel drug to combat bacteria that had acquired antibiotic resistance to commonly used antibiotics. Tebipenem is the first carbapenem whose prodrug form is orally available. The most common side effects include diarrhea, headache, nausea, abdominal pain, increased liver enzymes, and Clostridioides difficile infection.
Medical uses Tebipenem pivoxil is indicated for the treatment of complicated urinary tract infections, including pyelonephritis, caused by the following susceptible microorganisms: Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae species complex, Klebsiella oxytoca, and Enterococcus faecalis in adults who have limited or no alternative oral treatment options. In Japan, tebipenem pivoxil is approved for the treatment of haemophilus infections and streptococcal infections.
Side effects The most common side effects include diarrhea, headache, nausea, abdominal pain, increased liver enzymes, and Clostridioides difficile infection.
History The efficacy of tebipenem pivoxil was evaluated in adults with cUTI, including pyelonephritis, in a global, randomized, double-blind, double-dummy, noninferiority trial (NCT06059846). In this trial, 1,690 hospitalized participants were randomly assigned to receive tebipenem pivoxil 600 mg orally every 6 hours or imipenem-cilastatin 500 mg intravenously every 6 hours for 7 to 10 days. A total of 929 participants were considered the “intent-to-treat” population.
Society and culture
Legal status Tebipenem pivoxil was approved for medical use in Japan in April 2009, and in the United States in June 2026.
Names Tebipenem pivoxil is the international nonproprietary name. Tebipenem pivoxil is sold under the brand names Orapenem and Utebzi.
Research Tebipenem pivoxil is under development for the treatment of Shigella infections.
References
Further reading Jain A, Utley L, Parr TR, Zabawa T, Pucci MJ (July 2018). "Tebipenem, the first oral carbapenem antibiotic". Expert Review of Anti-infective Therapy. 16 (7): 513–522. doi:10.1080/14787210.2018.1496821. PMID 30014729. McEntee L, Johnson A, Farrington N, Unsworth J, Dane A, Jain A, et al. (August 2019). "Pharmacodynamics of Tebipenem: New Options for Oral Treatment of Multidrug-Resistant Gram-Negative Infections". Antimicrobial Agents and Chemotherapy. 63 (8). doi:10.1128/AAC.00603-19. PMC 6658774. PMID 31109982. Sun Z, Su L, Cotroneo N, Critchley I, Pucci M, Jain A, et al. (May 2022). "Evaluation of Tebipenem Hydrolysis by β-Lactamases Prevalent in Complicated Urinary Tract Infections". Antimicrobial Agents and Chemotherapy. 66 (5): e0239621. doi:10.1128/aac.02396-21. PMC 9112902. PMID 35491852.
External links Clinical trial number NCT06059846 for "A Study of Oral Tebipenem Pivoxil Hydrobromide (TBP-PI-HBr) Compared to Intravenous Imipenem-cilastatin in Participants With Complicated Urinary Tract Infection (cUTI) or Acute Pyelonephritis (AP) (PIVOT-PO)" at ClinicalTrials.gov