Ceftobiprole 500mg powder for solution for infusion vials
Requires a prescription from a doctor or prescriber
Ceftobiprole is a fifth-generation semisynthetic cephalosporin antibacterial which is available commercially as the prodrug [ceftobiprole medocaril].
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Suspected adverse reactions reported for Ceftobiprole
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Zevtera 500mg powder for concentrate for solution for infusion vials
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 19 · Randomised trials: 7 · 2005–2026
Showing the 50 most relevant studies, sorted by most relevant.
Gary J. Noel, Karen Bush, Partha Bagchi, et al.
Clinical Infectious Diseases, 2008
- Ceftazidime
- Cephalosporins
- Gram-Negative Bacteria
Gary J. Noel, Richard Strauß, Karen Amsler, et al.
Antimicrobial Agents and Chemotherapy, 2007
- Anti-Bacterial Agents
- Cephalosporins
- Gram-Positive Bacteria
Susan Nicholson, Tobias Welte, Thomas M. File, et al.
International Journal of Antimicrobial Agents, 2012
- Hospitalization
- Linezolid
- Acetamides
Wissal Jame, B. Başgut, A. Abdi
Diagnostic microbiology and infectious disease, 2024
- Cephalosporins
- Anti-Bacterial Agents
- Gram-Negative Bacteria
Yu. M. Gomon, A. S. Petrichenko
Реальная клиническая практика: данные и доказательства, 2025
Khalid Eljaaly, Haytham Wali, Ahmed Basilim, et al.
International Journal of Antimicrobial Agents, 2019
- Ceftaroline
- Anti-Bacterial Agents
- Ceftriaxone
Li Wang, Xinnan Zheng, Linghui Chen, et al.
Canadian Journal of Infectious Diseases and Medical Microbiology, 2026
Shao-Huan Lan, Hong-Zin Lee, Chih-Cheng Lai, et al.
Expert Review of Anti-infective Therapy, 2021
J. Scott Overcash, Charles Kim, Richard Keech, et al.
Clinical Infectious Diseases, 2020
- Skin Diseases, Bacterial
- Methicillin-Resistant Staphylococcus aureus
- Anti-Bacterial Agents
Abdullah A. Alhifany, Nisrin Bifari, Yasser Alatawi, et al.
Saudi Pharmaceutical Journal : SPJ, 2022
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
194 found
Half-life
3.3 hours
Mechanism
[Ceftobiprole], the active moiety of ceftobiprole medocaril, exhibits its bacter…
Food interactions
None known
Human targets
None mapped
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
100%
[L50472]…
Half-life
3.3 hours
[L50442][L50472]
Protein binding
16%
[L50442][L50472]
Volume of distribution
15.5-18.0 L
Metabolism
4%
[L50472]…
Elimination
89%
[L50472]…
Clearance
4.98 L/h
[L50442][L50472]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
The EMA's Committee for Medicinal Products for Human Use (CHMP) adopted a negative opinion of ceftobiprole medocaril in February 2010, recommending the refusal of its marketing authorization in the European Union primarily due to data quality issues in pivotal clinical studies.[L50467] It received its first approval in Canada in October 2017 for use in certain patients with bacterial pneumonia,[L50472] and was subsequently approved in the United States with additional indications for skin and skin structure infections and bacteremia in April 2024.[L50442][L50457]
[L50442]
It is additionally indicated in adult patients with acute bacterial skin and skin structure infections (ABSSSI).
[L50442]
It is indicated in adult and pediatric patients ≥3 months of age for the treatment of community-acquired bacterial pneumonia (CABP).
[L50442]
In Canada, it is additionally indicated for the treatment of hospital-acquired pneumonia (excluding ventilator-associated pneumonia).
[L50472]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 854 interactions
[L50442]
Ceftobiprole has demonstrated in vitro activity against both Gram-positive and Gram-negative bacteria.[L50442] In Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Ceftobiprole binds to PBP2a.[L50472] Ceftobiprole also binds to PBP2b in Streptococcus pneumoniae (penicillin-intermediate), PBP2x in S. pneumoniae (penicillin resistant), and to PBP5 in Enterococcus faecalis.[L50472]
It is not active against Gram-negative bacteria producing extended-spectrum beta-lactamases (ESBLs) from the TEM, SHV, or CTX-M families, serine carbapenemases (such as KPC), class B metallo-beta-lactamases, class C (AmpC cephalosporinases) if expressed at high levels, and Ambler class D beta-lactamases including carbapenemases.[L50442]
Ceftobiprole is not indicated for use in patients with ventilator-associated bacterial pneumonia (VABP) - in clinical trials, a statistically significant increase in mortality was seen in patients with VABP treated with ceftobiprole medocaril as compared to comparator-treated patients.[L50442]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[L50472]
The mean Cmax and AUC0-8h of ceftobiprole after multiple-dose administration are 33.0 µg/mL and 102 µg*h/mL, respectively.
[L50472]
[L50442][L50472]
[L50442][L50472]
[L50442][L50472]
[L50472]
Ceftobiprole itself is minimally metabolized to a microbiologically inactive open-ring metabolite, which accounts for approximately 4% of the parent exposure in subject with a normal renal function.
[L50472]
[L50472]
Approximately 89% of the administered dose is recovered in the urine as active ceftobiprole (83%), the open-ring metabolite (5%) and ceftobiprole medocaril (<1%).
[L50472]
[L50442][L50472]
Proteins that transport this drug across cell membranes
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
PMID:10220572 PMID:10421658 PMID:11500505 PMID:16332456
Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification .
PMID:10421658
Also mediates hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 .
PMID:11500505
Transports sulfated bile salt such as taurolithocholate sulfate .
PMID:16332456
Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors .
PMID:10220572 PMID:11500505 PMID:12441801
Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine PMID:10220572 PMID:11500505
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Ceftobiprole
Additional database identifiers
Drugs Product Database (DPD)
20326
ChemSpider
23350302
ZINC
ZINC000004424091
GenBank Gene Database
AB063172
UniProt Accession
Q7DHH4_STAAU
GenBank Gene Database
AE005672
UniProt Accession
PBPX_STRPN
GenBank Gene Database
X16022
GenBank Protein Database
984233
UniProt Accession
PBP2_STRR6
GenBank Gene Database
X16367
GenBank Protein Database
47392
UniProt Accession
PBPX_STRR6
GenBank Gene Database
K00137
UniProt Accession
FTSI_ECOLI
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10959
GenAtlas
SLCO1B1
GeneCards
SLCO1B1
GenBank Gene Database
AF060500
GenBank Protein Database
5051630
Guide to Pharmacology
1220
UniProt Accession
SO1B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10961
GeneCards
SLCO1B3
GenBank Gene Database
AJ251506
GenBank Protein Database
9187497
Guide to Pharmacology
1221
UniProt Accession
SO1B3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:53
GenAtlas
ABCC2
GeneCards
ABCC2
GenBank Gene Database
U63970
GenBank Protein Database
1764162
Guide to Pharmacology
780
UniProt Accession
MRP2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:42
GenAtlas
ABCB11
GeneCards
ABCB11
GenBank Gene Database
AF091582
GenBank Protein Database
3873243
Guide to Pharmacology
778
UniProt Accession
ABCBB_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q27284724), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication.