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Safety, bactericidal activity, and pharmacokinetics of the antituberculosis drug candidate BTZ-043 in South Africa (PanACEA-BTZ-043-02): an open-label, dose-expansion, randomised, controlled, phase 1b/2a trial.

Lancet Microbe

December 2024

Institute of Infectious Diseases and Tropical Medicine, LMU University Hospital, LMU Munich, Germany; German Center for Infection Research, Munich Partner Site, Munich, Germany; Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Immunology, Infection, and Pandemic Research, Munich, Germany; Unit Global Health, Helmholtz Zentrum München, German Research Center for Environmental Health, Neuherberg, Germany. Electronic address:

Background: The broad use of bedaquiline and pretomanid as the mainstay of new regimens to combat tuberculosis is a risk due to increasing bedaquiline resistance. We aimed to assess the safety, bactericidal activity, and pharmacokinetics of BTZ-043, a first-in-class DprE1 inhibitor with strong bactericidal activity in murine models.

Methods: This open-label, dose-expansion, randomised, controlled, phase 1b/2a trial was conducted in two specialised tuberculosis sites in Cape Town, South Africa.

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Objectives: For investigating an influence on butylphthalide sodium chloride injection combined with edaravone dextromethorphan on neurological function, serum free radical levels, and serum inflammatory factor levels in sufferers having acute progressive cerebral infarction (APCI).

Methods: A cohort of 200 patients, afflicted by APCI and admitted to our healthcare institution between December 2018 through July 2023, were incorporated into this longitudinal prospective analysis. Employing a random number table methodology, the patient cohort was bifurcated into a control group ( = 100) and an observation group ( = 100).

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Dextromethorphan inhibits collagen and collagen-like cargo secretion to ameliorate lung fibrosis.

Sci Transl Med

December 2024

Cell Biology and Biophysics Unit, European Molecular Biology Laboratory, 69117 Heidelberg, Germany.

Excessive deposition of fibrillar collagen in the interstitial extracellular matrix (ECM) of human lung tissue causes fibrosis, which can ultimately lead to organ failure. Despite our understanding of the molecular mechanisms underlying the disease, no cure for pulmonary fibrosis has yet been found. We screened a drug library and found that dextromethorphan (DXM), a cough expectorant, reduced the amount of excess fibrillar collagen deposited in the ECM in cultured primary human lung fibroblasts, a bleomycin mouse model, and a cultured human precision-cut lung slice model of lung fibrosis.

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Post-stroke effects of IC87201 on neurobehavioral function and brain injuries: A stereological study.

IBRO Neurosci Rep

December 2024

Histomorphometry and Stereology Research Center and Department of Anatomical Sciences, Shiraz University of Medical Sciences, Shiraz, Iran.

Article Synopsis
  • Stroke is a major global health issue, mainly causing neuron death through NMDA receptor overactivation, and this study explores IC87201 as a potential treatment to reduce brain damage from ischemic strokes.
  • In an experiment with 24 male rats subjected to cerebral ischemia, researchers compared the effects of IC87201 and Dextromethorphan hydrobromide (DXM) on post-stroke brain recovery.
  • Results indicate that IC87201 significantly improved neurobehavioral functions and reduced brain damage more effectively than DXM, particularly enhancing cell survival in the striatum area of the brain.
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Article Synopsis
  • * Brexpiprazole is the only approved drug for agitation in Alzheimer's, but its effectiveness is questioned, and there are no approved treatments for psychosis, emphasizing the urgent need for new therapies.
  • * The review identifies three promising compounds in phase 3 trials for treating these symptoms: xanomeline-trospium for psychosis, and dextromethorphan-bupropion and dexmedetomidine for agitation; it also suggests incorporating biomarkers in clinical trials to improve drug testing efficiency.
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