Kim, Ju Sang published the artcileEarly Bactericidal Activity of Delpazolid (LCB01-0371) in Patients with Pulmonary Tuberculosis., Category: oxazolidine, the publication is Antimicrobial agents and chemotherapy (2022), 66(2), e0168421, database is MEDLINE.
Delpazolid, an oxazolidinone, has been studied in non-clinical studies of efficacy and toxicity and Phase 1 clinical studies. Delpazolid has in vitro activity against Gram-positive bacteria, including Mycobacterium tuberculosis. This study evaluated the bactericidal activity, safety, and pharmacokinetics of delpazolid in patients with pulmonary tuberculosis (TB). Seventy-nine subjects, aged 19 to 75âyears with newly diagnosed smear-positive TB with no prior treatment for the current episode and no confirmed resistance to rifampin or isoniazid, were randomized to receive delpazolid 800âmg once a day (QD), 400âmg twice a day (BID), 800âmg BID or 1,200âmg QD or an active control of isoniazid, rifampin, pyrazinamide, and ethambutol (HRZE) or linezolid 600âmg BID. The primary endpoint was the average daily reduction in log transformed bacterial load, assessed on 7H11 solid-media culture, from days 0 to 14. The average daily decline in log-CFU was 0.044â±â?.016, 0.053â±â?.017, 0.043â±â?.016, and 0.019â±â?.017, for the delpazolid 800âmg QD, 400âmg BID, 800âmg BID, and the 1,200âmg QD groups, respectively. The average daily decline in log-CFU was 0.192â±â?.028 for the HRZE group and 0.154â±â?.023 for the linezolid 600âmg BID group. Three serious adverse events (SAE) were reported, one each in the delpazolid 400âmg BID group (death due to worsening of TB at day 2), the HRZE group (hospitalization due to pleural effusion) and the linezolid group (hyperkalemia); none of the SAEs were assessed as related to study drugs. This study has been registered at ClinicalTrials.gov with registration number NCT02836483.
Antimicrobial agents and chemotherapy published new progress about 1219707-39-7. 1219707-39-7 belongs to oxazolidine, auxiliary class Other Aliphatic Heterocyclic,Oxazolidine,Chiral,Fluoride,Benzene,Amide,Alcohol,Anti-infection, name is (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one, and the molecular formula is C14H17FN4O3, Category: oxazolidine.
Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem