delpazolid (LCB01-0371) / LigaChem Biosci, HaiHe Biopharma - LARVOL DELTA

Study to Evaluate the Efficacy of Delpazolid as Add-on Therapy in Refractory Mycobacterium Abscessus Complex (clinicaltrials.gov) - P2 | N=24 | Completed | Sponsor: LigaChem Biosciences, Inc. | Active, not recruiting ➔ Completed | Trial completion date: Dec 2026 ➔ Jun 2026

Trial completion • Trial completion date • Infectious Disease • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases

MDR-ENDPlus: A 6-Month MDR-END Plus Regimen for Rifampicin-Resistant Tuberculosis (clinicaltrials.gov) - P3 | N=294 | Not yet recruiting | Sponsor: Seoul National University Hospital

New P3 trial • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis • CD4

Inhalable nanohybrid of delpazolid enhances antimicrobial host defense against mycobacterial pulmonary infection. (PubMed, J Control Release) - "DZD@DLC treatment preserved the hematopoietic stem cell pool and maintained a homeostatic, non-inflammatory myeloid profile in the bone marrow. By uncoupling therapeutic efficacy from systemic toxicity, the DZD@DLC nanohybrid represents a highly promising platform for developing safer and more effective inhalation therapies against challenging mycobacterial lung infections."

Journal • Immunology • Infectious Disease • Inflammation • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases • LYZ

Annual progress in chemotherapy for tuberculosis in 2025 (PubMed, Zhonghua Jie He He Hu Xi Za Zhi) - "New agents such as Telacebec, Quabodepistat, Sutezolid, and Delpazolid exhibit potent bactericidal activity and lower toxicity, laying the foundation for regimen shortening and combination optimization...In addition, 9-month (Bedaquiline-Linezolid-Fluoroquinolone-based) and 6-9-month all-oral regimens with varied combinations have shown comparable efficacy across different resistance patterns and resource settings, providing feasible alternatives in regions where Pretomanid availability is limited...Future progress is expected to focus on four key directions: discovery of new mechanisms and innovative regimen combinations; precision pharmacological management guided by pharmacokinetic/pharmacodynamic principles and therapeutic drug monitoring; safety assessment and stratified strategies for special populations; and the generation of robust real-world evidence to support globally harmonized yet locally adapted implementation. This review systematically summarizes advances..."

Journal • Review • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Current Status and Perspectives of Antibacterial Agents Belonging to 2-Oxazolidinones. (PubMed, Pharmaceuticals (Basel)) - "Tedizolid phosphate was the second commercially available oxazolidinone antibiotic approved, followed by other oxazolidinones (contezolid, radezolid, ranbezolid, sutezolid, delpazolid, cadazolid, TBI-233 and MK-7762) that are in clinical study. Three literature databases, i.e., PubMed/MEDLINE, Google Scholar and Scopus, were used for the literature search, particularly focusing on the last five years, and screened using different keywords. The design of new drugs belonging to this class may be of considerable interest to researchers and clinicians, contributing to the discovery of new antibiotics that retain antibacterial activity but have fewer side effects."

Journal • Review • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Structural modification of oxazolidinone antibiotics alters nascent peptide stalling preference and peptide trajectory through the ribosome. (PubMed, bioRxiv) - "Delpazolid, which shares the C5 hydroxymethyl moiety with tedizolid, shows a similar preference. Structural analysis of the ribosome with tedizolid and a stalled nascent peptide showed a compacted, helical conformation of the nascent chain induced by the drug. Our findings reveal that stalling preferences of oxazolidinones can be modulated by structural modifications within this antibiotic class."

Journal

Preclinical and clinical evaluation of vancomycin plus delpazolid combination therapy for MRSA bacteremia: a multicenter, double-blinded, randomized, parallel design, phase IIa clinical trial. (PubMed, Microbiol Spectr) - P2 | "Synergistic effects of delpazolid with vancomycin or daptomycin were evaluated in vitro using checkerboard and time-kill assays, and in vivo using a Galleria mellonella model. While overall cure rates and bacteremia clearance were numerically higher in the combination group, these differences were not statistically significant. These preliminary findings underscore the need for larger, adequately powered clinical trials to clarify the clinical role of delpazolid combination therapy in MRSA infections."

Journal • P2a data • Preclinical • Infectious Disease

HIV-associated drug-resistant TB: expanded treatment options and emerging threats. (PubMed, Curr Opin HIV AIDS) - "Treatment options for DR-TB have improved dramatically with less toxic, more effective regimens, but managing HIV-associated DR-TB continues to require careful attention to drug-drug interactions and HIV related co-morbidities. Research into novel DR-TB regimens, especially for people with bedaquiline resistance, and host-directed therapies are critical to realize continued improvement in HIV-associated DR-TB outcomes."

Journal • Human Immunodeficiency Virus • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Synergistic activity of fosfomycin combined with old and new oxazolidinones (linezolid, contezolid, delpazolid, and sutezolid) against bloodstream isolates of vancomycin-resistant Enterococcus faecium. (PubMed, Eur J Clin Microbiol Infect Dis) - "Our findings provide preclinical evidence supporting the use of fosfomycin in combination with novel oxazolidinones as a promising therapeutic strategy against VR E. faecium infections."

Journal • Infectious Disease

Updates in the clinical management of Tuberculous meningitis. (PubMed, Expert Rev Anti Infect Ther) - "Emphasis is placed on high-dose rifampicin, linezolid, and novel oxazolidinones such as sutezolid and delpazolid...Steroids like dexamethasone are already used, while drugs like aspirin and thalidomide are being studied. Children, pregnant women, and people with HIV are at special risk and need extra care. With faster tests, stronger drugs, and safer treatment plans, there is new hope that more people will survive and recover well."

Journal • Review • CNS Disorders • Human Immunodeficiency Virus • Infectious Disease • Pain • Pulmonary Disease • Respiratory Diseases • Tuberculosis • Vascular Neurology

PanACEA - STEP2C -01 (clinicaltrials.gov) - P2 | N=390 | Recruiting | Sponsor: Michael Hoelscher | N=270 ➔ 390 | Trial completion date: Feb 2025 ➔ Dec 2027 | Trial primary completion date: Feb 2025 ➔ Oct 2027

Enrollment change • Trial completion date • Trial primary completion date • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Delpazolid in combination with bedaquiline, delamanid, and moxifloxacin for pulmonary tuberculosis (PanACEA-DECODE-01): a prospective, randomised, open-label, phase 2b, dose-finding trial. (PubMed, Lancet Infect Dis) - P2 | "The pharmacokinetic-pharmacodynamic modelling results suggest that delpazolid adds efficacy on top of bedaquiline, delamanid, and moxifloxacin; and that a dose of 1200 mg once daily would result in exposures with maximum efficacy. That dose was shown to be safe, raising hope that linezolid toxicities could be averted in long-term treatment. Delpazolid is a promising drug for future tuberculosis treatment regimens and could be widely usable if safety and efficacy are confirmed in larger trials."

Journal • P2b data • Gastrointestinal Disorder • Hematological Disorders • Human Immunodeficiency Virus • Infectious Disease • Leukopenia • Neutropenia • Optic Neuritis • Pain • Pulmonary Disease • Respiratory Diseases • Thrombocytopenia • Tuberculosis

Study to Evaluate the Efficacy of Delpazolid as Add-on Therapy in Refractory Mycobacterium Abscessus Complex (clinicaltrials.gov) - P2 | N=20 | Active, not recruiting | Sponsor: LigaChem Biosciences, Inc. | Recruiting ➔ Active, not recruiting | Trial completion date: May 2026 ➔ Dec 2026 | Trial primary completion date: Jul 2025 ➔ Nov 2025

Enrollment closed • Trial completion date • Trial primary completion date • Infectious Disease • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases

Cardiac safety of bedaquiline, delamanid and moxifloxacin co-administered with or without varying doses of sutezolid or delpazolid for the treatment of drug-susceptible TB. (PubMed, J Antimicrob Chemother) - "The drug regimens containing standard doses of bedaquiline, delamanid and moxifloxacin, and varying doses of sutezolid or delpazolid were not found to pose a high cardiac risk in a population without further QTc-relevant risk factors. However, close monitoring of the QTc interval remains essential in patients with TB treated with combination drug therapy with known QTc-prolonging drugs."

Journal • Cardiovascular

Establishing Structure-Activity Relationships in Heterogeneous Catalysis of Three-Component Organic Coupling Reactions by Lewis Acidic Metal Sites and Polar Moieties. (PubMed, ACS Appl Mater Interfaces) - "A wide spectrum of substrates with diverse electronic, steric, and polarizing effects is tested to obtain bioactive precursors, particularly tedizolid and delpazolid, achieving high conversion rates (65-94%) and turnover numbers. The postcatalysis analysis of both Co-bpaipa and Ni-bpaipa demonstrates their structural stability and nonleachability, even after multiple catalytic runs."

Heterogeneity • Journal

Comparative In Vitro Drug Susceptibility Study of Five Oxazolidinones Against Mycobacterium tuberculosis in Hainan, China. (PubMed, Pathogens) - "In this study, we aimed to compare the in vitro activity of linezolid (LZD) and four oxazolidinones, including tedizolid (TZD), contezolid (CZD), sutezolid (SZD), and delpazolid (DZD), against multidrug-resistant tuberculosis (MDR-TB) and pre-extensively drug-resistant tuberculosis (pre-XDR-TB) isolates from Hainan. In vitro susceptibility testing indicated that SZD exhibited the strongest antibacterial activity, followed by TZD and LZD, while CZD and DZD demonstrated comparable but weaker effectiveness. Mutations in rplD and mce3R were discovered, but further research is needed to clarify their role in conferring oxazolidinone resistance in MTB."

Clinical • Journal • Preclinical • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Comparative pharmacokinetics study of two tablet formulations of delpazolid, a novel oxazolidinone class antibiotic. (PubMed, Transl Clin Pharmacol) - P1 | "The two different delpazolid formulations showed comparable PK and safety profiles, indicating that the test drug is an appropriate alternative to the reference drug. ClinicalTrials.gov Identifier: NCT04939779."

Journal • PK/PD data • Infectious Disease

Management of Refractory Nontuberculous Mycobacterial Pulmonary Disease (KATRDIC 2024) - "Liposomal amikacin, for example, has shown an additional 20% bacterial conversion in refractory cases. Other new drugs, such as epetraborole, delpazolid, inhaled clofazimine, and omadacycline, have also been utilized for NTM-PD. When bacterial conversion is difficult, the treatment goal may shift to improving quality of life through appropriate antibiotic therapy. This presentation will comprehensively address the causes of treatment-refractory NTM-PD and outline appropriate management strategies."

Nontuberculous mycobacteria • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases

Study to Evaluate the Efficacy of Delpazolid as Add-on Therapy in Refractory Mycobacterium Abscessus Complex (clinicaltrials.gov) - P2 | N=20 | Recruiting | Sponsor: LigaChem Biosciences, Inc. | Active, not recruiting ➔ Recruiting

Enrollment open • Infectious Disease • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases

New Oxazolidinones for Tuberculosis: Are Novel Treatments on the Horizon? (PubMed, Pharmaceutics) - "The search identified sutezolid, tedizolid, delpazolid, eperezolid, radezolid, contezolid, posizolid and TBI-223, in addition to linezolid. Sutezolid, tedizolid, delpazolid and TBI-223 displayed promising preliminary results. Further clinical studies would be required to assess the safety profiles and optimize the dosing regimens."

Journal • Review • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

A Phase 2a Study, Effect of Vancomycin With vs Without Delpazolid (LCB01-0371) in Patients With MRSA Bacteremia (clinicaltrials.gov) - P2 | N=40 | Terminated | Sponsor: LigaChem Biosciences, Inc. | N=100 ➔ 40 | Trial completion date: Nov 2024 ➔ Feb 2024 | Recruiting ➔ Terminated | Trial primary completion date: Nov 2024 ➔ Feb 2024; Early termination; Difficulties in enrolling subjects due to the decrease in patients with MRSA bacteremia

Enrollment change • Monotherapy • Trial completion date • Trial primary completion date • Trial termination

Pharmacokinetic and Pharmacodynamic Modeling Analysis of Delpazolid (LCB01-0371) in Adult Patients with Pulmonary Tuberculosis. (PubMed, J Clin Pharmacol) - "The PK-PD simulation suggested that the bacterial titers are the lowest on the 800 mg bid regimen among the four, consistent with observed data, as all regimens substantially decrease. In the dose-response relationship, the effectiveness of delpazolid was suggested."

Journal • PK/PD data • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

PanACEA DElpazolid Dose-finding and COmbination DEvelopment (DECODE) (clinicaltrials.gov) - P2 | N=76 | Completed | Sponsor: LegoChem Biosciences, Inc | Active, not recruiting ➔ Completed | Phase classification: P2b ➔ P2 | Trial completion date: Mar 2024 ➔ Sep 2023

Phase classification • Trial completion • Trial completion date • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Study to Evaluate the Efficacy of Delpazolid as Add-on Therapy in Refractory Mycobacterium Abscessus Complex (clinicaltrials.gov) - P2 | N=20 | Active, not recruiting | Sponsor: LegoChem Biosciences, Inc | Not yet recruiting ➔ Active, not recruiting | Phase classification: P2a ➔ P2

Enrollment closed • Phase classification • Infectious Disease • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases

A Phase 2a Study, Effect of Vancomycin With vs Without Delpazolid (LCB01-0371) in Patients With MRSA Bacteremia (clinicaltrials.gov) - P2 | N=100 | Recruiting | Sponsor: LegoChem Biosciences, Inc | Phase classification: P2a ➔ P2 | Trial completion date: Nov 2023 ➔ Nov 2024 | Trial primary completion date: Nov 2023 ➔ Nov 2024

Monotherapy • Phase classification • Trial completion date • Trial primary completion date