- |||||||||| bevantolol (SOM3355) / SOM Biotech
Clinical, Journal: Prognostic value of estimated plasma volume in patients with chronic systolic heart failure. (Pubmed Central) - Feb 2, 2022 ePVS determined using hemoglobin and hematocrit was independently associated with clinical outcomes for patients with stable CHF. Our study thus further strengthens the evidence that ePVS has important prognostic value in patients with stable CHF.Trial registration number ChiCTR-ONC-14004463.
- |||||||||| prexasertib (LY2606368) / Eli Lilly, SOM Biotech, Ewha Womans University
Journal: MMB-FOXM1-driven premature mitosis is required for CHK1 inhibitor sensitivity. (Pubmed Central) - Jan 27, 2022 To identify genes whose loss confers resistance to CHK1 inhibitors, we perform genome-wide CRISPR-Cas9 screens in non-small-cell lung cancer (NSCLC) cell lines treated with the CHK1 inhibitor prexasertib (CHK1i)...Activation of a feedback loop between the MMB-FOXM1 complex and CDK1 is required for CHK1i-induced premature mitosis in Late S phase and subsequent replication catastrophe, indicating that dysregulation of the S to M transition is necessary for CHK1 inhibitor sensitivity. These findings provide mechanistic insights into small molecule inhibitors currently studied in clinical trials and provide rationale for combination therapies.
- |||||||||| prexasertib (LY2606368) / Eli Lilly, SOM Biotech, Ewha Womans University
Journal: Acquired small cell lung cancer resistance to Chk1 inhibitors involves Wee1 up-regulation. (Pubmed Central) - Jan 15, 2022 As the cell cycle checkpoint kinase 1 (Chk1) plays a key role in DNA damage response to chemotherapeutic drugs, we explored the mechanisms of acquired drug resistance to the Chk1 inhibitor prexasertib in SCLC...We also show that bypass activation of the p38MAPK signaling pathway may contribute to acquired resistance to Chk1 inhibition. The combination of Chk1 and Wee1 inhibitors may provide a new therapeutic strategy for the treatment of SCLC.
- |||||||||| doxorubicin hydrochloride / Generic mfg.
EXPLORING THE ATR-CHK1 PATHWAY IN THE RESPONSE OF DOXORUBICIN-INDUCED DNA DAMAGES IN ACUTE LYMPHOBLASTIC LEUKEMIA CELLS () - Dec 25, 2021 - Abstract #SIE2021SIE_128; Indeed, the inhibition of the G2/M checkpoint led to a significant increment of normal and aberrant mitotic cells, including those showing tripolar spindles, metaphases with lagging chromosomes and massive chromosomes fragmentation. In conclusion, we found that the ATR-CHK1 pathway is involved in the response to Dox-induced DNA damages and we demonstrated that our new in vitro drug schedule that combines Dox followed by ATR/CHK1 inhibitors can increase Dox cytotoxicity against ALL cells, while using lower drug doses.
- |||||||||| prexasertib (LY2606368) / Eli Lilly, SOM Biotech, Ewha Womans University
Preclinical, Journal: Preclinical efficacy of prexasertib in acute lymphoblastic leukemia. (Pubmed Central) - Dec 18, 2021 A proof-of-concept study was conducted to confirm that SOM3355 effectively reduces Huntington’s chorea and has a good safety profile. No abstract available
- |||||||||| Preclinical, Journal: In vitro activity of cefiderocol, cefepime/zidebactam, cefepime/enmetazobactam, omadacycline, eravacycline, and other comparative agents against carbapenem-nonsusceptible Enterobacterales: Results from the Surveillance of Multicenter Antimicrobial Resistance in Taiwan (SMART) in 2017-2020. (Pubmed Central) - Dec 16, 2021
The MICs of omadacycline were significantly higher than those of eravacycline and tigecycline. In summary, cefiderocol, ceftazidime/avibactam, and cefepime/zidebactam were more effective against CNS E. coli and K. pneumoniae, than other drugs; highlighting their potential as valuable therapeutics.
- |||||||||| Clinical, Review, Journal: Role of new antibiotics in extended-spectrum β-lactamase-, AmpC- infections. (Pubmed Central) - Dec 16, 2021
New therapeutic agents against ESBL- and AmpC-producing Enterobacterales have distinctive specificities and limitations that require further investigations. Future randomized clinical trials are required to define the best strategy for their use in patients with serious infections due to ESBL- and/or AmpC- infections.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, PAION, Innoviva
Trial completion, Trial completion date, Trial primary completion date: A Safety and PK Study of IV Eravacycline (clinicaltrials.gov) - Dec 3, 2021 P1, N=19, Completed, Future randomized clinical trials are required to define the best strategy for their use in patients with serious infections due to ESBL- and/or AmpC- infections. Recruiting --> Completed | Trial completion date: Nov 2020 --> Mar 2021 | Trial primary completion date: Aug 2020 --> Mar 2021
- |||||||||| carboplatin / Generic mfg.
Journal: The mitotic checkpoint is a targetable vulnerability of carboplatin-resistant triple negative breast cancers. (Pubmed Central) - Nov 21, 2021 We confirmed that pharmacological inhibition of CHEK1 by prexasertib in the presence of carboplatin is well tolerated by mice and suppresses the growth of carboplatin-resistant TNBC xenografts. Thus, abrogation of the mitotic checkpoint by CHEK1 inhibition re-sensitizes carboplatin-resistant TNBCs to carboplatin and represents a potential strategy for the treatment of carboplatin-resistant TNBCs.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION
Journal: A plethora of carbapenem resistance in Acinetobacter baumannii: no end to a long insidious genetic journey. (Pubmed Central) - Nov 17, 2021 Colistin, considered as the most promising antibacterial agent, nevertheless faces adverse effects flaws. Cefiderocol, eravacycline, new β-lactam antibiotics, non-β-lactam-β-lactamase inhibitors, polymyxin B-derived molecules and bacteriophages are some other new treatment options streamlined.
- |||||||||| vancomycin / Generic mfg.
Journal: Therapeutic Options for Infections due to vanB Genotype Vancomycin-Resistant Enterococci. (Pubmed Central) - Nov 6, 2021 In addition, new drugs have been developed (e.g., dalbavancin, telavancin, and tedizolid), new molecules will soon be available (e.g., eravacycline, omadacycline, and oritavancin), and new treatment strategies are progressively being used in clinical practice (e.g., combination therapies and bacteriophages). The aim of this article is to discuss the pathogenesis of infections due to enterococci harboring the vanB operon (vanBVRE) and their therapeutic, state-of-the-art, and future treatment options and provide a comprehensive and easy to use review for clinical purposes.
- |||||||||| ATR/CHK1/WEE1 Dependency in SRSF2-Mutated MDS/AML (GWCC - Hall B5, Level 1) - Nov 5, 2021 - Abstract #ASH2021ASH_5353;
Cell line models indicate that sensitivity is similar across mutant alleles and dependent on allelic copy number. Several ATR/CHK1 and WEE1 inhibitors are in development, and our results suggest that these compounds could be effective treatments for SRSF2 -mutated MDS and AML.
- |||||||||| Nuzyra (omadacycline) / Paratek, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION
Clinical, Journal: Antimicrobial susceptibility of bacteremic vancomycin-resistant Enterococcus faecium to eravacycline, omadacycline, lipoglycopeptides, and other comparator antibiotics: Results from the 2019/2020 Nationwide Surveillance of Multicenter Antimicrobial Resistance in Taiwan (SMART). (Pubmed Central) - Oct 30, 2021 Moreover, the susceptibility rates of quinupristin/dalfopristin, tedizolid, and linezolid were 59.1%, 84.2%, and 77.4%, respectively...Compared to several large worldwide antimicrobial susceptibility surveillance programs, the susceptibility rates of VREfm isolates in Taiwan to synthetic tetracyclines and daptomycin were slightly lower, and their susceptibility rates to oxazolidinone-class antibiotics were much lower than those in other parts of the world. Continuous monitoring of VREfm resistance to novel antibiotics, including synthetic tetracyclines, oxazolidinone-class antibiotics, and daptomycin in Taiwan is needed.
- |||||||||| Clinical, Review, Journal: Emerging Carbapenem-Resistant Enterobacteriaceae Infection, Its Epidemiology and Novel Treatment Options: A Review. (Pubmed Central) - Oct 30, 2021
Meropenem-vaborbactam, imipenem-relebactam, plazomicin, cefiderocol, eravacycline, and aztreonam-avibactam are recently reported to be active against carbapenem-resistant Enterobacteriaceae; and are also in ongoing trials for different populations and combinations with other antibacterial agents. Overall, treatment must be tailored to the patient's susceptibility profile, type and degree of infection, and personal characteristics.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION, Zemdri (plazomicin) / Ionis, Achaogen
Clinical, Journal: New drugs for difficult bugs: management of multidrug-resistant gram-negative infections in solid organ transplant recipients. (Pubmed Central) - Oct 20, 2021 Overall, treatment must be tailored to the patient's susceptibility profile, type and degree of infection, and personal characteristics. This review summarizes therapeutic options for extended-spectrum β-lactamase-producing Enterobacterales, carbapenem-resistant Enterobacterales and Pseudomonas aeruginosa with difficult-to-treat resistance in SOT recipients and emphasizes recently approved antimicrobial agents.
- |||||||||| sulbactam-durlobactam (ETX2514SUL) / Entasis Therap, ZAI Lab, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION
Review, Journal: Contemporary Perspective on the Treatment of Acinetobacter baumannii Infections: Insights from the Society of Infectious Diseases Pharmacists. (Pubmed Central) - Oct 15, 2021 Traditional agents with retained in vitro activity (aminoglycosides, polymyxins, and tetracyclines) are limited by suboptimal pharmacokinetic characteristics, emergence of resistance, and/or toxicity...On balance, cefiderocol and eravacycline demonstrate potent in vitro activity and are well tolerated, but clinical data for patients with CRAB infections do not yet support widespread use...Our preferred regimen for critically ill patients infected, or considered to be at high risk for CRAB, includes meropenem, polymyxin B, and ampicillin/sulbactam...Promising therapies that are in clinical development and/or under investigation include durlobactam-sulbactam, cefiderocol combination regimens, and bacteriophage therapy, which may over time eliminate the need for the continued use of polymyxins. Future goals for CRAB management include pathogen-focused treatment paradigms that are based on molecular mechanisms of resistance, local susceptibility rates, and the availability of well-tolerated, effective treatment options.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION
[VIRTUAL] In Vitro Activity of Eravacycline Against Clinically Significant Bacteria Isolated from Patients with Cancer () - Oct 6, 2021 - Abstract #IDWeek2021IDWeek_2155; Our data demonstrate that eravacycline has promising activity against clinically significant bacterial pathogens isolated from PWC including many drug resistant strains such as CRE and non--fermentative GNB. it might play an important role in the treatment of bacterial infections in PWC and warrants clinical evolution in this setting.
- |||||||||| Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION
[VIRTUAL] Eravacycline in Bacteremia: A Case Series () - Oct 6, 2021 - Abstract #IDWeek2021IDWeek_2138; ERV may be an option for bacteremia as demonstrated by clearance in four of five cases. More studies must be conducted as these reports show variable clinical outcomes.
- |||||||||| imipenem/relebactam / Merck (MSD), Vabomere (meropenem/vaborbactam) / Melinta Therap, Xerava (eravacycline) / SOM Biotech, Ewha Womans University, La Jolla Pharma, PAION
[VIRTUAL] Access to Antimicrobial Susceptibility Testing for Novel Gram-Negative Antibiotics () - Oct 6, 2021 - Abstract #IDWeek2021IDWeek_985; Long TATs exist and a great deal of time is spent per patient for coordinating AST for these novel agents. There is a crucial need for a multidisciplinary, collaborative approach to resolve the challenges in obtaining AST for newly developed antibiotics to provide patient care.
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