- |||||||||| prexasertib (ACR-368) / Acrivon Therap
Journal, PARP Biomarker, PD(L)-1 Biomarker, IO biomarker: MYC amplification sensitizes TNBC to CHK1 inhibitors. (Pubmed Central) - Apr 13, 2025 Our subsequent results revealed that the novel second-generation CHK1 inhibitor, prexasertib, exhibited a more pronounced inhibitory effect in MYC-overexpressed TNBC cells compared to other DNA damage repair inhibitors, including ATR, WEE1, and PARP inhibitors...In conclusion, our findings demonstrated that MYC overexpression characterizes an aggressive TNBC subtype, enabling synergistic lethality with CHK1 inhibitors. CHK1 inhibitors will be a potential therapeutic strategy in TNBC patients with MYC overexpression.
- |||||||||| Review, Journal: Newly developed antibiotics against multidrug-resistant and carbapenem-resistant Gram-negative bacteria: action and resistance mechanisms. (Pubmed Central) - Apr 2, 2025
Porin modifications reduce the influx of antibiotics, whereas overexpression of efflux pumps, particularly those in the resistance-nodulation-cell division (RND) family, actively expels antibiotics from bacterial cells, significantly lowering intracellular drug concentrations and leading to treatment failure.This review examines the mechanisms of action, resistance profiles, and pharmacokinetic/pharmacodynamic characteristics of newly developed antibiotics designed to combat infections caused by MDR and carbapenem-resistant Gram-negative pathogens. The antibiotics discussed include ceftazidime-avibactam, imipenem-relebactam, ceftolozane-tazobactam, meropenem-vaborbactam, aztreonam-avibactam, delafloxacin, temocillin, plazomicin, cefiderocol, and eravacycline.
- |||||||||| prexasertib (ACR-368) / Acrivon Therap
Journal: Antitumor Activity of Radiation Therapy Combined with Checkpoint Kinase Inhibition in SHH/p53-Mutated Human Medulloblastoma. (Pubmed Central) - Mar 27, 2025 Here, we investigated the potential radiosensitizing effects of the checkpoint kinase inhibitors (Chk-is) prexasertib (Chk1/2) and SAR-020106 (Chk1) in human SHH/p53-mutated MB in vitro and in vivo...However, high-dose Chk-is may compromise the RT effect, possibly through anti-proliferative activity. Furthermore, we demonstrate, for the first time, the intracranial antitumor activity of the Chk1-specific inhibitor SAR-020106.
- |||||||||| tetracycline / Generic mfg.
Journal: C10-Benzoate Esters of Anhydrotetracycline Inhibit Tetracycline Destructases and Recover Tetracycline Antibacterial Activity. (Pubmed Central) - Mar 14, 2025 The best inhibitors recovered tetracycline antibiotic activity at concentrations as low as 2 ?M, producing synergistic scores <0.5 in the fractional inhibitory concentration index (FICI) against TDase-expressing strains of E. coli and clinical P. aeruginosa. The C10-benzoate ester derivatives of aTC reported here are promising new leads for the development of tetracycline drug combination therapies to overcome TDase-mediated antibiotic resistance.
- |||||||||| Journal: New Kids on the Block: Estimating Use of Next-generation Gram-negative Antibiotics Across Greater Than 700 Hospitals in the United States. (Pubmed Central) - Mar 5, 2025
In recent years, new broad-spectrum antibiotics targeting Gram-negative organisms have been introduced, including cefiderocol, ceftazidime-avibactam, ceftolozane-tazobactam, eravacycline, imipenem-relebactam, omadacycline, and meropenem-vaborbactam...In contrast, piperacillin-tazobactam was prescribed in 731 719 (18.8%) and colistin in 570 (0.01%) admissions...Ceftazidime-avibactam and ceftolozane-tazobactam remain the most frequently prescribed new antibiotics, with uptake of subsequently approved agents trailing. New antibiotics are most commonly used as treatment for sepsis among patients with multiple comorbidities.
- |||||||||| Journal: Comparative phenotypic and genotypic antimicrobial susceptibility surveillance in Achromobacter spp. through whole genome sequencing. (Pubmed Central) - Feb 27, 2025
In general, the species other than A. xylosoxidans showed lower MIC50 and MIC90, especially to carbapenems and ?-lactamase inhibitor combinations like piperacillin-tazobactam, meropenem-vaborbactam, and imipenem-relebactam...Our study provides phenotypic data regarding identification and susceptibility testing and correlates this with the genotypic characterization of 109 clinical isolates belonging to Achromobacter spp. This comprehensive study sheds light on the phenotypic and genotypic character of this bacteria, that is of increasing clinical relevance in hospital-acquired infections.
- |||||||||| prexasertib (ACR-368) / Acrivon Therap
Trial completion, Trial completion date, Trial primary completion date: A Study of the Drugs Prexasertib, Irinotecan, and Temozolomide in People With Desmoplastic Small Round Cell Tumor and Rhabdomyosarcoma (clinicaltrials.gov) - Feb 20, 2025 P1/2, N=21, Completed, This comprehensive study sheds light on the phenotypic and genotypic character of this bacteria, that is of increasing clinical relevance in hospital-acquired infections. Active, not recruiting --> Completed | Trial completion date: Sep 2025 --> Feb 2025 | Trial primary completion date: Sep 2025 --> Feb 2025
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva, colistin sulphate / Generic mfg.
Journal: Genome drafting of nosocomial infection CRE Klebsiella pneumoniae confirming resistance to colistin and eravacycline, carrying bla NDM-1, mcr-1, and bla KPC-2, in neonatology from November to December 2023. (Pubmed Central) - Feb 11, 2025 The plasmid profiles suggest these strains are reservoirs for multidrug-resistant genes, emphasizing the need for strict infection control and ongoing genomic surveillance. For neonatal care, these resistance challenges increase the risk of treatment failures and mortality, underscoring the importance of enhanced infection prevention and novel therapeutic strategies.
- |||||||||| imipenem/relebactam / Merck (MSD), Vabomere (meropenem/vaborbactam) / Melinta Therap, Menarini, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Colistin, meropenem/vaborbactam, imipenem/relebactam, and eravacycline testing in carbapenem-resistant Gram-negative rods: a comparative evaluation of broth microdilution, gradient test, and VITEK 2 (Poster area; A / 7 / 35) - Feb 4, 2025 - Abstract #ESCMIDGlobal2025ESCMID_Global_3727;
- |||||||||| Emblaveo (aztreonam/avibactam) / Pfizer, AbbVie, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
In vitro activities of the essential antimicrobial agents including aztreonam/avibactam, eravacycline, colistin, and other comparators against carbapenem-resistant organisms with different carbapenemase genes: a multicentre study in China, 2021 (Poster area; A / 3 / 6) - Feb 4, 2025 - Abstract #ESCMIDGlobal2025ESCMID_Global_3661;
- |||||||||| Journal, Adverse events: Pharmacovigilance analysis of drug-induced hypofibrinogenemia using the FDA Adverse Event Reporting System. (Pubmed Central) - Jan 31, 2025
This analysis of FAERS data identified 52 drugs associated with hypofibrinogenemia, most (88.5%) of which do not mention this risk in their prescribing information. These findings demonstrate the need for the monitoring of blood fibrinogen and may serve as a reference for the explore of the characteristics and underlying mechanism of drug-induced hypofibrinogenemia in the real world.
- |||||||||| decitabine / Generic mfg.
Decitabine Synergizes with Replication Checkpoint Inhibitors in TP53-Mutated Acute Myeloid Leukemia () - Dec 7, 2024 - Abstract #ASH2024ASH_7862; https://clinicaltrials.gov/, ChiCTR2300078646. Prior reports suggest that DNA methyltransferase inhibitors (DNMTi), such as decitabine and azacitidine, form covalent DNA-DNMT1 adducts and invoke a DNA damage response (DDR) characterized by activation of the ATR-CHK1 pathway, including in TP53MT AML samples...Similar results were obtained from decitabine (EC50 = 300
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Clinical, Preclinical, Journal: In vitro activities of eravacycline against clinical bacterial isolates: a multicenter study in Guangdong, China. (Pubmed Central) - Dec 3, 2024 Eravacycline (ERV), a novel tetracycline derivative, exhibits broad-spectrum antibacterial activity, but data on the bacterial activity against Chinese bacterial isolates are very scarce...Since there were no intermediate breakpoints for the eravacycline, the MIC values measured by the ETEST method might result in lower CA and higher VME and ME. This study provides MIC values of eravacycline against Gram-positive and Gram-negative pathogens in four hospitals in Guangdong Province, and eravacycline is an effective therapeutic candidate for common bacteria.
- |||||||||| imipenem/relebactam / Merck (MSD), Vabomere (meropenem/vaborbactam) / Melinta Therap, Menarini, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Journal, Gram negative: Colistin, Meropenem-Vaborbactam, Imipenem-Relebactam, and Eravacycline Testing in Carbapenem-Resistant Gram-Negative Rods: A Comparative Evaluation of Broth Microdilution, Gradient Test, and VITEK 2. (Pubmed Central) - Nov 27, 2024 VITEK 2 was mostly accurate in measuring ERV MICs, while the corresponding gradient test yielded reliable results exclusively in CREs. It is essential that laboratories are aware of which testing method provides reliable results for each combination of microorganisms and reserve antibiotics.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Journal: Eradication of Pseudomonas aeruginosa Persister Cells by Eravacycline. (Pubmed Central) - Nov 16, 2024 The effects of eravacycline on persister control were further validated in vivo using a lung infection model in mice. Collectively, these results demonstrate the possibility to control persister cells of bacterial pathogens by targeting dormancy.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Journal, Combination therapy: Combination Therapy of Trimethoprim-Sulfamethoxazole (TMP-SMZ) and Eravacycline for Treating Elizabethkingia anophelis-Induced Pulmonary Infections: A Case Report. (Pubmed Central) - Nov 15, 2024 Additionally, this report provides a summary of high-risk factors for E. anophelis infection, clinical manifestations, and therapeutic options. Given the high degree of antimicrobial drug resistance of the organism and the fact that inappropriate empirical antimicrobial therapy constitutes a risk factor for mortality, our case serves as a valuable reference for similar cases, highlighting potential strategies for effective management.
- |||||||||| Emblaveo (aztreonam/avibactam) / Pfizer, AbbVie, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Clinical, Preclinical, Journal: In vitro activities of the essential antimicrobial agents including aztreonam/avibactam, eravacycline, colistin, and other comparators against carbapenem-resistant bacteria with different carbapenemase genes: a multicenter study in China, 2021. (Pubmed Central) - Nov 6, 2024 Using aztreonam/avibactam, eravacycline and colistin to treat infections caused by CRB offers significant advantages. These findings will guide clinical practice and optimize antimicrobial administration.
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