zosurabalpin (RG6006) / Roche - LARVOL DELTA

In silico analysis of zosurabalpin-LptB2FG binding in Acinetobacter spp., Klebsiella pneumoniae, and Shigella flexneri: mechanisms underlying its differential efficacy. (PubMed, In Silico Pharmacol) - "These findings underscore the need for tailored zosurabalpin derivatives to enhance efficacy against a broader spectrum of Gram-negative bacteria. The online version contains supplementary material available at 10.1007/s40203-025-00343-3."

Journal • Infectious Disease • Pneumonia

In vitro activity of zosurabalpin against carbapenem-resistant-A. baumannii (CRAB) clinical isolates from diverse origins (ESCMID Global 2025) - No abstract available

Late-breaking abstract • Preclinical

Preliminary zosurabalpin (5µg) disk diffusion quality control ranges using clinical and laboratory standards institute M23 criteria (ESCMID Global 2025) - No abstract available

Clinical

Antibacterial effect of zosurabalpin using simulated human doses against carbapenem resistant Acinetobacter baumannii studied in an in vitro model of infection (ESCMID Global 2025) - No abstract available

Preclinical • Infectious Disease

Antimicrobial activity of zosurabalpin against a diverse collection of aerobic and anaerobic bacterial and yeast isolates (ESCMID Global 2025) - No abstract available

Assessment of zosurabalpin activity in combination with other antibiotics (ESCMID Global 2025) - No abstract available

Combination therapy

Effect of zosurabalpin, a pathogen-focused antibiotic, on the gut microbiome of healthy participants (ESCMID Global 2025) - No abstract available

Clinical

Determination of optimal disk diffusion mass for zosurabalpin (ESCMID Global 2025) - No abstract available

Acinetobacter baumannii Complex Infections: New Treatment Options in the Antibiotic Pipeline. (PubMed, Microorganisms) - "Furthermore, many older agents, such as polymyxin and colistin, have limited lung penetration and are associated with significant toxicities. In order to place these newer molecules in context and to help clinicians appreciate the emerging potential drug development pipeline, we describe the in vitro activity, mechanisms of action, and clinical trial data not only for the commercially now available alternatives, such as cefiderocol and sulbactam-durlobactam, but also review these topics for molecules undergoing phase II and III clinical trials. Specifically, we discuss and analyze data related to four novel drugs from ABC: BV-100, cefepime-zidebactam, zosurabalpin, and OMN6."

Journal • Review • Infectious Disease • Pneumonia • Respiratory Diseases • Septic Shock

Potentially effective antimicrobial treatment for pneumonia caused by isolates of carbapenem-resistant and extensively drug-resistant Acinetobacter baumannii complex species: what can we expect in the future? (PubMed, Expert Rev Anti Infect Ther) - "Doubling the routine intravenous maintenance dosages of conventional tigecycline (100 mg every 12 h) and minocycline (200 mg every 12 h) might be recommended for the effective treatment of pneumonia caused by CR/XDR-Abc. Nebulized polymyxin E, novel parenteral rifabutin BV100, and new polymyxin derivatives (SPR206, MRX-8, and QPX9003) could be considered supplementary combination options with other antibiotic classes. Regarding other novel antibiotics, the potency of sulbactam-durlobactam (1 g/1 g infused over 3 h every 6 h intravenously) combined with imipenem-cilastatin, and the β-lactamase inhibitor xeruborbactam, is promising. Continuous infusion of full-dose cefiderocol is likely an effective treatment regimen for CR/XDR-Abc pneumonia. Zosurabalpin exhibits potent anti-CR/XDR-Abc activity in vitro, but its practical use in clinical therapy remains to be evaluated. The clinical application of antimicrobial peptides and bacteriophages requires validation."

Journal • Review • Infectious Disease • Pneumonia • Respiratory Diseases

Zosurabalpin like petrichor: A novel antibiotic class with unprecedented target towards Acinetobacter baumannii. (PubMed, Sci Bull (Beijing)) - No abstract available

Journal

Zosurabalpin: a novel tethered macrocyclic peptide antibiotic that kills carbapenem-resistant Acinetobacter baumannii. (PubMed, MedComm (2020)) - No abstract available

Journal

Unveiling the Secrets of Acinetobacter baumannii: Resistance, Current Treatments, and Future Innovations. (PubMed, Int J Mol Sci) - "Among the most promising alternatives under investigation are the combination sulbactam/durlobactam, cefepime/zidebactam, imipenem/funobactam, xeruborbactam, and the newest molecules such as novel polymyxins or zosurabalpin. Furthermore, the potential of phage therapy, as well as deep learning and artificial intelligence, offer a complementary approach that could be particularly useful in cases where traditional strategies fail. The fight against A. baumannii is not confined to the microcosm of microbiological research or hospital wards; instead, it is a broader public health dilemma that demands a coordinated, global response."

Journal • Review • Infectious Disease

Assessment of zosurabalpin activity in combination with other antibiotics (ECCMID 2024) - No abstract available

Combination therapy

MIC distributions and activity of the novel anti-Acinetobacter agent zosurabalpin (RG6006) (ECCMID 2024) - No abstract available

Target identification and mode of action studies of zosurabalpin (ECCMID 2024) - No abstract available

Pharmacokinetics and safety in ICU patients and healthy participants following single dose administration of zosurabalpin (RG6006), a novel pathogen-specific antibiotic for the treatment of serious Acinetobacter infections (ECCMID 2024) - No abstract available

Clinical • PK/PD data • Infectious Disease

Preliminary zosurabalpin broth microdilution quality control ranges using Clinical and Laboratory Standards Institute M23 criteria (ECCMID 2024) - No abstract available

Clinical

Mechanism of in vitro resistance to zosurabalpin (RG6006) in Acinetobacter baumannii (ECCMID 2024) - No abstract available

Preclinical

Clinical crusade: zosurabalpin's charge against antibiotic resistance. (PubMed, Trends Mol Med) - "describe a novel tethered macrocyclic peptide (MCP) antibiotic, zosurabalpin, that disrupts the essential function of the LptB2FGC complex in Gram-negative bacteria and demonstrates efficacy against carbapenem-resistant Acinetobacter baumannii (CRAB). Its preclinical success suggests a substantial shift in treating antibiotic resistance, pending clinical trials to validate its effectiveness, pharmacokinetics, and resistance management."

Journal • Infectious Disease

A Study to Investigate the Pharmacokinetics of RO7223280 in Critically Ill Participants With Bacterial Infections (clinicaltrials.gov) - P1 | N=48 | Completed | Sponsor: Hoffmann-La Roche | Recruiting ➔ Completed

Trial completion • Infectious Disease

A novel antibiotic class targeting the lipopolysaccharide transporter. (PubMed, Nature) - "A clinical candidate derived from the MCP class, zosurabalpin (RG6006), effectively treats highly drug-resistant contemporary isolates of CRAB both in vitro and in mouse models of infection, overcoming existing antibiotic resistance mechanisms. This chemical class represents a promising treatment paradigm for patients with invasive infections due to CRAB, for whom current treatment options are inadequate, and additionally identifies LptBFGC as a tractable target for antimicrobial drug development."

Journal • Infectious Disease

Discovery and characterization of Zosurabalpin (RG6006), a Tethered Macrocyclic Peptide Targeting Acinetobacter baumannii (IDWeek 2023) - No abstract available

Infectious Disease

Activity of the Novel Antibiotic Zosurabalpin (RG6006) against Clinical Acinetobacter Isolates from China (IDWeek 2023) - No abstract available

Clinical • Infectious Disease

Safety, Tolerability, and Pharmacokinetics (PK) in Healthy Participants Following Single Dose Administration of Zosurabalpin, a Novel Pathogen-Specific Antibiotic for the Treatment of Serious Acinetobacter Infections (IDWeek 2023) - No abstract available

Clinical • PK/PD data • Infectious Disease