macrolide analogs / Melinta Therap - LARVOL DELTA

Untargeted Metabolomic Analysis and Cytotoxicity of Extracts of the Marine Dinoflagellate Amphidinium eilatiense Against Human Cancer Cell Lines. (PubMed, Toxins (Basel)) - "Untargeted metabolomic analysis of cytotoxic fractions by liquid chromatography coupled with high-resolution mass spectrometry (LC-HRMS) revealed a much richer chemical diversity profile than previous toxigenicity studies on Amphidinium that exclusively focused on linear and cyclic polyethers and their macrolide analogs as putative cytotoxins. This untargeted metabolomic study showed substantial differences in chemical composition between the biologically active and non-active fractions. Preliminary biological and chemical characterization of these A. eilatiense fractions confirms that this species is a rich source of bioactive natural products with potential applications such as anticancer therapeutics."

Journal • Preclinical • Lung Cancer • Oncology • Solid Tumor

Toward a Template for Synthetic Actin-Targeting Macrolide Analogues That Inhibit Cancer Cell Invasiveness. (PubMed, J Med Chem) - "To develop potent analogues of these compounds that are simpler to synthesize and compatible with cell-specific targeting systems, such as antibodies, we designed over 20 analogues of the acyclic side chain (tail) of the macrolide Mycalolide B. These analogues probed the contributions of five distinct regions of the tail toward actin polymerization inhibition, F-actin depolymerization, and inhibition of ECM invasion by human lung cancer A549 cells. We observed that two of these regions tolerate considerable substituent variability, and we identified a specific combination of substituents that maximally inhibit the ECM invasion activity of A549 cells."

Journal • Lung Cancer • Oncology • Solid Tumor

Solithromycin versus ceftriaxone plus azithromycin for the treatment of uncomplicated genital gonorrhoea (SOLITAIRE-U): a randomised phase 3 non-inferiority trial. (PubMed, Lancet Infect Dis) - P3 | "Solithromycin as a single 1000 mg dose is not a suitable alternative to ceftriaxone plus azithromycin as first-line treatment for gonorrhoea. If insufficient duration of solithromycin exposure at the infection site in a subset of individuals was the reason for treatment failures, this might be adequately addressed with dose adjustment. However, any further trials with longer dosing need to consider the potential risk of gastrointestinal effects and liver enzyme elevations."

Clinical • Head-to-Head • Journal • P3 data