Delving into the Latest Updates on Ceftobiprole Medocaril Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ceftobiprole medocaril free acid, ceftobiprole, ceftobiprole medocaril

+ [12]

Target

PBPs

Action

inhibitors

Mechanism

PBPs inhibitors(Bacterial penicillin-binding protein inhibitors)

Therapeutic Areas

Infectious DiseasesRespiratory DiseasesCongenital Disorders+ [1]

Active Indication

Community Acquired PneumoniaHospital-acquired pneumoniaNeonatal Sepsis

Inactive Indication

Bacterial InfectionsCommunity-acquired bacterial pneumoniaFever+ [14]

Originator Organization

Basilea Pharmaceutica AG

Active Organization

Basilea Pharmaceutica AGBasilea Pharmaceuticals Deutschland GmbH

Avir Pharma, Inc.Startup

Inactive Organization

Janssen Pharmaceutical Unlimited Co.Johnson & Johnson Pharmaceutical Research & Development LLCBasilea Pharmaceutica International Ltd.

Drug Highest PhaseApproved

First Approval Date

Canada (20 Mar 2018),

Community Acquired PneumoniaHospital-acquired pneumonia

RegulationFast Track (United States), Qualified Infectious Disease Product (United States), Priority Review (United States)

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Structure/Sequence

Molecular FormulaC26H26N8NaO11S2

InChIKeyBYUIXTXYXHAECA-LCJFHXTKSA-N

CAS Registry252188-71-9

View All Structures (2)

A Phase 1, Single-center, Open-label, Non-randomized, Fixed-sequence, Drug-drug Interaction Study to Assess the Effect of Repeated Doses of Intravenous Ceftobiprole on the Pharmacokinetics of Oral Pitavastatin (OATP1B Substrate) and on Plasma Levels of Coproporphyrin I (OATP1B Biomarker) in Healthy Subjects

The goal of this clinical study is to determine the effect of the test drug ceftobiprole (a drug approved for the treatment of bacterial infections) on the elimination of pitavastatin (a drug approved for the treatment of increased levels of cholesterol in blood) from the body. This interaction will be investigated by pharmacokinetic (PK) assessments.
The PK of pitavastatin will be assessed when administered alone and when administered together with ceftobiprole in a study design including two treatment periods.
The clinical study will also investigate the safety of ceftobiprole and how well ceftobiprole is tolerated by healthy subjects when it is administered in combination with pitavastatin. In addition, the effect of ceftobiprole on a specific marker, called coproporphyrin I, will be assessed in the blood.
The duration of the study will be a maximum of 38 days.

Start Date17 Jan 2025

Sponsor / Collaborator

Basilea Pharmaceutica AG

[+1]

ChiCTR2500096047

/ RecruitingEarly Phase 1IIT

Pharmacokinetic Characteristics and Blood-Brain Barrier Penetration of Ceftobiprole in Patients with Proposed or Confirmed Central Nervous System Infection

Start Date28 Oct 2024

Sponsor / Collaborator-

NCT05856227

/ CompletedPhase 3

A Multicenter, Open-label, Single-arm, Multiple-dose Study to Evaluate the Safety, Pharmacokinetics, and Efficacy of Ceftobiprole Medocaril in Term and Pre-term Neonates and Infants up to 3 Months of Age With Late-onset Sepsis

This study will evaluate the safety, pharmacokinetics and efficacy of ceftobiprole in term and pre-term newborn babies and infants up to 3 months of age with late-onset sepsis (LOS). Ceftobiprole is an antibiotic which belongs to a group of medicines called 'cephalosporin antibiotics'. It is approved for its use to treat adults and children with pneumonia in many European and non-European countries.

Start Date06 Aug 2023

Sponsor / Collaborator

Basilea Pharmaceutica AG

100 Clinical Results associated with Ceftobiprole Medocaril Sodium

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100 Translational Medicine associated with Ceftobiprole Medocaril Sodium

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100 Patents (Medical) associated with Ceftobiprole Medocaril Sodium

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448

Literatures (Medical) associated with Ceftobiprole Medocaril Sodium

01 Apr 2025·International Journal of Antimicrobial Agents

Safety of ceftobiprole in patients with impaired renal, hepatic or immune function: A multinational retrospective hospital chart review (RETRACE study)

Article

Author: Francisci, Daniela ; de Novales, Francisco Javier Membrillo ; Fernández-Hidalgo, Nuria ; Jemmely, Noëlle ; Falcone, Marco ; Estébanez, Miriam ; Durante-Mangoni, Emanuele ; Cedar, Eve ; Quevedo, Juan ; Gentile, Ivan ; Soriano, Alex

Ceftobiprole, an advanced-generation cephalosporin with broad bactericidal activity, is approved for community-acquired and hospital-acquired pneumonia (excluding ventilator-associated pneumonia). We aimed to evaluate, in a real-world setting, the safety profile of ceftobiprole in patients with risk conditions (severe renal impairment, hepatic impairment, and immunocompromised status), groups excluded from clinical trials. In this retrospective study (NCT04170309), 396 consecutive charts of patients treated with ceftobiprole during 2016-2022 in 15 centers in France, Italy, and Spain were analyzed: 62 had severe renal impairment, 51 had hepatic impairment, 120 were immunocompromised, and 203 had no predefined risk condition (controls). Ceftobiprole was used for off-label indications in 110/396 (27.8%) patients; 46/396 (11.6%) patients received a higher-than-recommended dose. Treatment-emergent adverse events (TEAEs) considered as ceftobiprole-related occurred in 44 patients, more frequently in the risk groups compared to controls (severe renal impairment: 8/62 [12.9%]; hepatic impairment: 7/51 [13.7%]; immunocompromised: 19/120 [15.8%]; controls: 15/203, [7.4%]); in 7/44 patients, these events were serious. Compared to controls, liver-related AEs occurred more frequently in the impaired hepatic function (17/51 [33.3%] vs 22/203 [10.8%], odds ratio [OR:]: 4.11; 95% confidence interval [CI]: 1.98-8.55) and immunocompromised (30/120 [25.0%] vs 22/203 [10.8%], OR: 2.74; 95%CI: 1.50-5.02) groups. Hyponatremia was also more frequent in immunocompromised patients than controls (14/120 [11.7%] vs 9/203 [4.4%], OR: 2.85; 95%CI: 1.19-6.80). Underlying disease, concomitant medications and the poor health status of the patients likely affected these imbalances. Overall, no new safety concerns related to ceftobiprole use in real-world patients with severe renal impairment, hepatic impairment or immunocompromised status were identified.

13 Feb 2025·Antimicrobial Agents and Chemotherapy

Ceftobiprole activity against multidrug-resistant Staphylococcus aureus clinical isolates collected in the United States from 2016 through 2022

Article

Author: Castanheira, Mariana ; Sader, Helio S. ; Smart, Jennifer I. ; Mendes, Rodrigo E.

ABSTRACT Ceftobiprole was recently approved by the United States (US) Food and Drug Administration (FDA) for the treatment of adult patients with Staphylococcus aureus bacteremia, including right-side endocarditis, acute bacterial skin and skin structure infections, and community-acquired bacterial pneumonia in adults and pediatrics. Ceftobiprole is an advanced-generation cephalosporin approved in many countries for the treatment of adults with community-acquired pneumonia and hospital-acquired pneumonia, excluding ventilator-associated pneumonia. We evaluated the activities of ceftobiprole and comparators against methicillin-resistant S. aureus (MRSA) and multidrug-resistant (MDR) S. aureus clinical isolates. A total of 19,764 S . aureus isolates were collected from patients with various infection types at 37 US medical centers from 2016 to 2022. Susceptibility testing was performed by broth microdilution according to Clinical and Laboratory Standard Institutes (CLSI) standards. Isolates were categorized as MDR if they were nonsusceptible by CLSI criteria to ≥3 antimicrobials. Ceftobiprole was highly active against MRSA ( n = 8,184; MIC 50/90 , 1/2 mg/L; 99.3% susceptible [S]) and MDR ( n = 2,789; MIC 50/90 , 1/2 mg/L; 98.1%S) isolates and retained activity against 87.3% of ceftaroline-nonsusceptible isolates ( n = 433; MIC 50/90 , 2/4 mg/L). Ceftobiprole demonstrated greater susceptibility rates than ceftaroline against all resistant subsets. Ceftobiprole was highly active against isolates nonsusceptible to clindamycin (98.0%S), daptomycin (100.0%S), doxycycline (98.2%S), erythromycin (99.5%S), gentamicin (98.1%S), levofloxacin (99.1%S), tetracycline (99.1%S), tigecycline (100.0%S), and trimethoprim-sulfamethoxazole (99.4%S) and isolates with decreased susceptibility to vancomycin (98.3%S).

01 Feb 2025·The Nurse Practitioner

Recent drug approvals, winter 2025 edition

Article

Author: Drake, Evan S. ; Anderson, James Layton ; Marino, Adriane B. ; Theroux, Jenna D. ; Self, Destiny S.

ABSTRACTIn the first half of 2024, the US FDA approved several new drugs that have relevance for those practicing in primary care. This article, the winter 2025 edition of the journal's biannual Drug Update, highlights the following new medications: sotatercept-csrk (Winrevair), aprocitentan (Tryvio), resmetirom (Rezdiffra), berdazimer (Zelsuvmi), ceftobiprole medocaril sodium (Zevtera), sofpironium (Sofdra), and ensifentrine (Ohtuvayre).

94

News (Medical) associated with Ceftobiprole Medocaril Sodium

14 Mar 2025

·www.globenewswire.com

Strong Cresemba® (isavuconazole) sales performance in Asia Pacific and China triggers milestone payment to Basilea

Allschwil, Switzerland, March 14, 2025 Basilea Pharmaceutica Ltd, Allschwil (SIX: BSLN), a commercial-stage biopharmaceutical company committed to meeting the needs of patients with severe bacterial and fungal infections, announced today that the continued strong sales performance of the antifungal Cresemba® (isavuconazole) by its license partner Pfizer Inc. in the Asia Pacific region and China exceeded the sales threshold triggering a USD 2.5 million milestone payment. David Veitch, Basilea’s Chief Executive Officer, stated: “We are pleased with the strong sales performance from our partner Pfizer, resulting in this first sales milestone for the Asia Pacific and China region this year, which significantly surpasses previous sales milestones for the region. This underscores the continued progress in making Cresemba available to increasing numbers of patients suffering from life-threatening invasive mold infections in this region.” The license agreement between Basilea and Pfizer for Cresemba covers Europe (excluding the Nordic countries) as well as China and 16 countries in the Asia Pacific region. Cresemba is marketed in more than 70 countries. According to the latest available market data, total global in-market sales of Cresemba in the twelve-month period between October 2023 and September 2024 amounted to USD 533 million, a 20 percent growth year-on-year, making it the largest branded antifungal for invasive fungal infections worldwide.1 About Cresemba® (isavuconazole) Cresemba, with the active ingredient isavuconazole, is an intravenous (i.v.) and oral azole antifungal. Basilea has entered into several license and distribution agreements for Cresemba covering approximately 115 countries. In China, the oral and intravenous formulations are approved for the treatment of adult patients with invasive aspergillosis and invasive mucormycosis. Isavuconazole is also approved in the European Union2, the United Kingdom3, the United States (US)4 and several additional countries including in the Asia Pacific region.5 About Basilea Basilea is a commercial-stage biopharmaceutical company founded in 2000 and headquartered in Switzerland. We are committed to discovering, developing and commercializing innovative drugs to meet the needs of patients with severe bacterial or fungal infections. We have successfully launched two hospital brands, Cresemba for the treatment of invasive fungal infections and Zevtera for the treatment of bacterial infections. In addition, we have preclinical and clinical anti-infective assets in our portfolio. Basilea is listed on the SIX Swiss Exchange (SIX: BSLN). Please visit basilea.com. Disclaimer This communication expressly or implicitly contains certain forward-looking statements, such as "believe", "assume", "expect", "forecast", "project", "may", "could", "might", "will" or similar expressions concerning Basilea Pharmaceutica Ltd, Allschwil and its business, including with respect to the progress, timing and completion of research, development and clinical studies for product candidates. Such statements involve certain known and unknown risks, uncertainties and other factors, which could cause the actual results, financial condition, performance or achievements of Basilea Pharmaceutica Ltd, Allschwil to be materially different from any future results, performance or achievements expressed or implied by such forward-looking statements. Basilea Pharmaceutica Ltd, Allschwil is providing this communication as of this date and does not undertake to update any forward-looking statements contained herein as a result of new information, future events or otherwise. For further information, please contact: Peer Nils Schröder, PhD Head of Corporate Communications & Investor RelationsBasilea Pharmaceutica International Ltd, Allschwil Hegenheimermattweg 167b4123 AllschwilSwitzerland Phone +41 61 606 1102 E-mail media_relations@basilea.cominvestor_relations@basilea.com This press release can be downloaded from www.basilea.com. References IQVIA Analytics Link, September 2024. In-market sales reported as moving annual total (MAT) in US dollar.European Public Assessment Report (EPAR) Cresemba: https://www.ema.europa.eu/en/medicines/human/EPAR/cresemba [Accessed: March 13, 2025]Summary of Product Characteristics (SmPC) Cresemba: https://www.medicines.org.uk/emc/search?q=cresemba [Accessed: March 13, 2025]Full US prescribing information: https://www.astellas.us/docs/cresemba.pdf [Accessed: March 13, 2025]The registration status and approved indications may vary from country to country. Attachment Press release (PDF)

License out/inDrug Approval

18 Feb 2025

·www.fiercebiotech.com

Basilea opts not to take MRSA antibiotic into clinic due to \'stringent risk-return criteria\'

“This decision demonstrates that we are focused on stringent risk-return criteria when making portfolio decisions,” Basilea Pharmaceutica said.\n Basilea Pharmaceutica has cited its “stringent risk-return criteria” as a reason for not taking up its option to bring a MRSA antibiotic into clinical development.Basilea secured the license option for the endolysin antibiotic, called tonabacase, from Korea’s iNtRON Biotechnology in 2023. Basilea had been conducting a preclinical evaluation of the asset throughout 2024 ahead of a decision on whether to secure the exclusive rights to take tonabacase into human trials.When it signed the agreement with iNtRON, Basilea pointed to preclinical evidence of tonabacase’s activity against methicillin-resistant and methicillin-susceptible Staphylococcus aureus (MRSA and MSSA) as well as coagulase-negative staphylococci.“There continues to be a high medical need for new treatment options for patients with persistent infections caused by Gram-positive bacteria and tonabacase is an exciting and innovative asset for us to evaluate over the coming months,” Basilea Chief Medical Officer Marc Engelhardt, M.D., said back in 2023. “If the outcome of our evaluation is positive and we enter into a full license agreement, we may be able to start directly a phase 2 clinical study in 2025.” That trial is now off the menu, as Basilea has completed its own preclinical profiling of the medicine and “taken the decision not to pursue further development,” the Swiss company said in its full-year earnings report.“This decision demonstrates that we are focused on stringent risk-return criteria when making portfolio decisions,” the company added.Basilea currently markets Cresemba for invasive fungal infections and Zevtera for bacterial infections. The low return on investment means many of the biggest biopharmas have given up working on new antifungals or antibiotics in recent years—although GSK in particular has continued to sign deals and post encouraging clinical results against infections like gonorrhea.Meanwhile, Basilea has swum against the tide, pivoting away from cancer toward anti-infectives last year. The company’s clinical pipeline is headed up by fosmanogepix, an antifungal licensed from Amplyx Pharmaceuticals that Basilea is planning to enter into its second phase 3 study against mold infections.Basilea’s work developing new antifungals received a significant boost last September from the U.S. Department of Health and Human Services, which signed off on up to $268 million of funding to the biopharma over more than a decade.

$Basilea opts not to take MRSA antibiotic into clinic due to \'stringent risk-return criteria\'$

License out/inPhase 3

08 Feb 2025

·www.globenewswire.com

Strong launch for Cresemba in Japan triggers first sales milestone payment from AKP to Basilea

Basilea Pharmaceutica Ltd, Allschwil (SIX: BSLN), a commercial-stage biopharmaceutical company committed to meeting the needs of patients with severe bacterial and fungal infections, reported today that the sales of the antifungal Cresemba® (isavuconazole) in Japan exceeded the threshold triggering the first sales milestone payment from its partner Asahi Kasei Pharma (AKP), amounting to approximately CHF 1.2 million. David Veitch, Chief Executive Officer of Basilea, said: “Japan is a key market with significant growth potential for Cresemba. The achievement of the first sales milestone already in the second year of commercialization is a testament of the commercial capability of our partner AKP in this important market. The strong sales ramp-up in the early stage of its life cycle in Japan underscores that Cresemba is meeting critical medical needs of patients with life-threatening fungal infections.” By year-end 2024, Cresemba was marketed in more than 70 countries. According to the latest available market data, total global in-market sales of Cresemba in the twelve-month period between October 2023 and September 2024 amounted to USD 533 million, a 20 percent growth year-on-year, making it the largest branded antifungal for invasive fungal infections worldwide.1 Isavuconazole is an intravenous (i.v.) and oral azole antifungal, commercialized under the trade name Cresemba. In Japan, the oral and intravenous formulations are approved for the treatment of adult patients with aspergillosis, mucormycosis, and cryptococcosis.2 Isavuconazole is also approved in the United States (US),3 China, the EU4 and several additional countries in Europe and beyond.5 Basilea is a commercial-stage biopharmaceutical company founded in 2000 and headquartered in Switzerland. We are committed to discovering, developing and commercializing innovative drugs to meet the needs of patients with severe bacterial and fungal infections. We have successfully launched two hospital brands, Cresemba for the treatment of invasive fungal infections and Zevtera for the treatment of bacterial infections. In addition, we have preclinical and clinical anti-infective assets in our portfolio. Basilea is listed on the SIX Swiss Exchange (SIX: BSLN). Please visit basilea.com. References IQVIA Analytics Link, September 2024. In-market sales reported as moving annual total (MAT) in US dollar. PMDA List of Approved Drugs April 2022 to March 2023: https://www.pmda.go.jp/files/000267877.pdf [Accessed: February 04, 2025] Full US prescribing information: https://www.astellas.us/docs/cresemba.pdf [Accessed: February 04, 2025] European Public Assessment Report (EPAR): https://www.ema.europa.eu/en/medicines/human/EPAR/cresemba [Accessed: February 04, 2025] The content above comes from the network. if any infringement, please contact us to modify.

Drug Approval

100 Deals associated with Ceftobiprole Medocaril Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Ceftobiprole Medocaril Sodium	J01DI01	DB14733

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Community Acquired Pneumonia	Canada	Avir Pharma, Inc.Startup	20 Mar 2018
Hospital-acquired pneumonia	Canada	Avir Pharma, Inc.Startup	20 Mar 2018

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Skin Diseases, Infectious	Preclinical	European Union	Janssen Pharmaceutical Unlimited Co.	-
Soft Tissue Infections	Preclinical	European Union	Janssen Pharmaceutical Unlimited Co.	-
Skin and skin structure infections	Discovery	United States	Basilea Pharmaceutica International Ltd.	03 Apr 2024
Staphylococcus aureus bacteraemia	Discovery	United States	Basilea Pharmaceutica International Ltd.	03 Apr 2024
Healthcare-Associated Pneumonia	Discovery	-	Basilea Pharmaceutica AG	01 Apr 2005
Staphylococcal Skin Infections	Discovery	-	Basilea Pharmaceutica AG	01 Oct 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03137173 (FDA_CDER) Manual	Phase 3	Skin and skin structure infections	679	ZEVTERA 667 mg	(sphdkxpxfg) = uklchlkfro anrdkogwmc (ruvqqwuyrb ) View more	Positive	03 Apr 2024
				Vancomycin plus aztreonam	(sphdkxpxfg) = twmrniyltj anrdkogwmc (ruvqqwuyrb ) View more
NCT03138733 (FDA_CDER) Manual	Phase 3	Staphylococcus aureus bacteraemia	387	ZEVTERA	(xldtcgebqt) = xmdjuttwic uzsrichfwe (tvmigdwegc ) View more	Positive	03 Apr 2024
				Daptomycin	(xldtcgebqt) = dqzattfmzj uzsrichfwe (tvmigdwegc ) View more
NCT00326287 \| NCT03439124 (FDA_CDER) Manual	Phase 3	Community-acquired bacterial pneumonia	-	Ceftobiprole medocaril (Adult Patients)	(xelozuxuuz) = bfxnrnvtrw lnlogvdmzv (zxquhljjmg ) View more	Positive	03 Apr 2024
				Ceftriaxone with or without Linezolid (Adult Patients)	(xelozuxuuz) = jdzskjuhvp lnlogvdmzv (zxquhljjmg ) View more
NCT03138733 (ERADICATE, Corporate Publications) Manual	Phase 3	Staphylococcus aureus bacteraemia	390	Ceftobiprole Medocaril Sodium	gmhdaimuno(aedxgvhvff) = pggjebylnd bjkkottmox (whfqbyhzmn ) View more	Non-inferior	24 Oct 2022
				Aztreonam+Daptomycin	gmhdaimuno(aedxgvhvff) = ncqemrsoju bjkkottmox (whfqbyhzmn ) View more
NCT02527681 \| NCT03439124 (Pubmed \| Pediatr Infect Dis J)	Not Applicable	-	-	Ceftobiprole (Neonates and infants up to 3 months of age)	(bvumqpzrtg) = fxskqthubh dwmxwjggli (ygltugukbv ) View more	-	01 Nov 2021
				Ceftobiprole (Patients 3 months to 17 years of age)	(bvumqpzrtg) = vgnowlejrq dwmxwjggli (ygltugukbv ) View more
NCT03137173 (TARGET, Pubmed \| Clin Infect Dis) Manual	Phase 3	Skin and skin structure infections	679	Ceftobiprole Medocaril Sodium	(lxuexgosjl) = zymgoznfln ferzopyodl (obrkaztrcw ) View more	Non-inferior	05 Oct 2021
				Vancomycin Hydrochloride+Aztreonam	(lxuexgosjl) = odsyyfvpvz ferzopyodl (obrkaztrcw ) View more
NCT03439124 (Pubmed \| Pediatr Infect Dis J)	Phase 3	Pneumonia in children	138	Ceftobiprole	(cauuhacdmx) = qxuqiowugd wadmzusmhu (tkcwmljhqt ) View more	Positive	21 Jan 2021
				Standard-of-care IV cephalosporin treatments (ceftazidime or ceftriaxone)	(cauuhacdmx) = cfszpmoshh wadmzusmhu (tkcwmljhqt ) View more
NCT02527681 (CTgov)	Phase 1	Bacterial Infections	15	Ceftobiprole (Ceftobiprole PK Population)	(hltkgzwybs) = eiosogtnat jasaraxmmr (fftxdolxqx, fofpjnxofi - jvoizaqzmp) View more	-	06 Jan 2021
				Ceftobiprole (Ceftobiprole ITT/Safety Population)	aubrkpbnvx(pbpedqnxgo) = yksucokktg dfhrthefel (pdnpuiirjn, izjqaeekuq - dggpmrpled) View more
NCT03439124 (Trial 5, CTgov)	Phase 3	Community Acquired Pneumonia \| Hospital-acquired pneumonia	138	ceftobiprole medocaril (Ceftobiprole Medocaril)	tcwggbsujs(nwhvbdpbzr) = evhmibpzbd glcwtqhhik (grkssaghoy, ihoosjuvwz - jnzsangteo) View more	-	11 Sep 2020
				IV standard-of-care cephalosporin (IV Standard-of-care Cephalosporin)	tcwggbsujs(nwhvbdpbzr) = ayakhrkgqa glcwtqhhik (grkssaghoy, lfkjrxfqwc - vhbfscgsib) View more
NCT03137173 (TARGET \| Trial 2, CTgov)	Phase 3	Skin and skin structure infections	679	ceftobiprole medocaril (Ceftobiprole Medocaril)	(tnflocskmm) = supgqahnxz dvgqgcjcdv (rtajxjbpuw, emujjghdwi - eazzrsjtpz) View more	-	18 May 2020
				aztreonam+vancomycin (Vancomycin+Aztreonam)	(tnflocskmm) = vijsstbqmj dvgqgcjcdv (rtajxjbpuw, ufoenmdxme - xckcdabiam) View more