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  • ||||||||||  meropenem / Generic mfg., Daewon Pharmaceutical, Xerava (eravacycline) / Tetraphase, SOM Biotech, Ewha Womans University
    Journal:  Eravacycline: a new treatment option for complicated intra-abdominal infections in the age of multidrug resistance. (Pubmed Central) -  May 9, 2020   
    Safety: Eravacycline is well tolerated, with lower rates of nausea, vomiting and diarrhea than other tetracyclines. Eravacycline is an effective new option for use in complicated intra-abdominal infections, and in particular, for the treatment of extended-spectrum β-lactamase- and carbapenem-resistant Enterobacteriaceae-expressing organisms.
  • ||||||||||  meropenem / Generic mfg., Daewon Pharmaceutical, Xerava (eravacycline) / Tetraphase
    Journal:  Eravacycline: The Tetracyclines Strike Back. (Pubmed Central) -  Apr 24, 2020   
    Eravacycline is a new tetracycline antibiotic with a broad spectrum of activity that has demonstrated efficacy in the treatment of cIAIs. Although it has activity against multidrug-resistant organisms, data are limited for other indications.
  • ||||||||||  relebactam (MK-7655) / Merck (MSD)
    FDA event, Review, Journal:  FDA approved antibacterial drugs: 2018-2019. (Pubmed Central) -  Apr 21, 2020   
    Lefamulin is a semisynthetic pleuromutilin antibiotic for community-acquired bacterial pneumonia, while cefiderocol, a cephalosporin antibiotic is the last antibacterial drug approved in 2019, for the use in complicated urinary tract infections. Despite of these new developments, there is an ongoing need and urgency to develop novel antibiotic strategies and drugs to overrun the bacterial resistance to antibiotics.
  • ||||||||||  tolcapone (CRX-1008) / Corino Therap, SOM Biotech, Tasmar (tolcapone) / Endo, Bausch Health
    The Interaction Between COMT Genotype and Tolcapone on Cerebral Perfusion and Resting-State Functional Connectivity (Americas Hall I & II) -  Apr 17, 2020 - Abstract #SOBP2020SOBP_757;    
    Directionality and regions influenced differ between those affected by COMT genotype compared with those altered by tolcapone. Our findings also extend the evidence for dopaminergic modulation of cerebral perfusion and highlight the importance of considering vascular effects in functional neuroimaging studies.
  • ||||||||||  tolcapone (CRX-1008) / Corino Therap, SOM Biotech, Tasmar (tolcapone) / Endo, Bausch Health
    Catechol-O-Methyltransferase Activity Impacts Smoking Urges and Withdrawal in Women (Americas Hall I & II) -  Apr 17, 2020 - Abstract #SOBP2020SOBP_396;    
    These sex-sensitive findings may shed light on mechanisms contributing to sex differences in barriers to smoking cessation and support the potential benefit COMT inhibitors for smoking cessation in women. Funding Source: R21 DA038253-01 (NIDA; Co PIs: DeVito, Sofuoglu)
  • ||||||||||  tolcapone (CRX-1008) / Corino Therap, SOM Biotech, tolcapone / Generic mfg.
    [VIRTUAL] Proof-Of-Concept Study of Tolcapone in Women Smokers () -  Apr 17, 2020 - Abstract #CPDD2020CPDD_229;    
    Findings supported the hypotheses: tolcapone reduced smoking urges, withdrawal symptoms, smoking behavior and subjective reinforcement from smoking in women. Additional research is needed into tolcapone as a potential cessation aid in women.
  • ||||||||||  tolcapone (CRX-1008) / Corino Therap, SOM Biotech, tolcapone / Generic mfg., Duodopa (levodopa/carbidopa intraduodenal gel infusion) / AbbVie
    [VIRTUAL] Effect of tolcapone on peripheral neuropathy in patients with Parkinson’s disease treated with levodopa/carbidopa intestinal gel (Room: Screen A9) -  Apr 9, 2020 - Abstract #EAN2020EAN_1321;    
    Although tolcapone add-on therapy and vitamin B supplementation decrease HCY and increase vitamin B levels, only patients treated with tolcapone had improved EMG findings – especially improvement in motor CV. This suggests that also other mechanisms connected with COMT function may play role in amelioration of peripheral neuropathy.
  • ||||||||||  prexasertib (ACR-368) / Acrivon Therap
    Trial completion date, BRCA Biomarker, PARP Biomarker:  A Study of Prexasertib (LY2606368) in Platinum-Resistant or Refractory Recurrent Ovarian Cancer (clinicaltrials.gov) -  Mar 18, 2020   
    P2,  N=169, Active, not recruiting, 
    ATRi-resistant cells further exhibit a G1-phase cell cycle arrest response to ATRi and alterations in G1/S phase proteins, including loss of CDC25A. Trial completion date: Mar 2020 --> Sep 2020
  • ||||||||||  Xerava (eravacycline) / Tetraphase
    Journal:  Eravacycline for the treatment of complicated intra-abdominal infections. (Pubmed Central) -  Mar 14, 2020   
    Expert opinion: Eravacycline may be particularly suitable for the treatment of cIAIs. Results from clinical trials and real-world data are now expected in specific subgroups of patients to confirm the safety profile and efficacy observed in registration trials.
  • ||||||||||  Journal:  Developments on antibiotics for multidrug resistant bacterial Gram-negative infections. (Pubmed Central) -  Mar 14, 2020   
    Recently approved antibiotic formulations; and agents in advanced stages of development, including combinations of β-lactam/β-lactamase inhibitor, novel cephalosporins (cefiderocol), tetracyclines (eravacycline), aminoglycosides (plazomicin), quinolones (delafloxacin and finafloxacin) and pleuromutilins (lefamulin) are discussed in this review...However, most of the new compounds are based on modifications of traditional antibiotic structures challenging their longevity as therapeutic options. More investment is needed for the discovery and clinical development of truly innovative and effective antibiotics without cross resistance to currently used antibiotics.
  • ||||||||||  prexasertib (LY2606368) / Eli Lilly, Pfizer, Lynparza (olaparib) / Merck (MSD), AstraZeneca
    Biomarker, Journal, BRCA Biomarker, PARP Biomarker:  Prexasertib treatment induces homologous recombination deficiency and synergizes with olaparib in triple-negative breast cancer cells. (Pubmed Central) -  Feb 28, 2020   
    Based on these data, RAD51 could be a biomarker for aggressive TNBC and for racial disparity in breast cancer. As positive correlation exists between RAD51 and CHEK1 expression in breast cancer, the in vitro preclinical data presented here provides additional mechanistic insights for further evaluation of the rational combination of prexasertib and olaparib for improved outcomes and reduced racial disparity in TNBC.
  • ||||||||||  prexasertib (LY2606368) / Eli Lilly, Pfizer
    Prexasertib (STARLIGHT BALLROOM) -  Feb 21, 2020 - Abstract #IASLCLCTT2020IASLC_LCTT_301;    
  • ||||||||||  rifampicin / Generic mfg., Xerava (eravacycline) / Tetraphase
    Clinical, Journal:  Mass Balance and Drug Interaction Potential of IV Eravacycline Administered to Healthy Subjects. (Pubmed Central) -  Feb 14, 2020   
    A reduction in total eravacycline exposure (AUC) of approximately 25%-35% and an increase in CL of approximately 50% occurred with concomitant eravacycline and rifampin. The dose of eravacycline should be increased to 1.5 mg/kg Q12H when coadministered with a strong CYP3A inducer.
  • ||||||||||  Review, Journal:  Carbapenem-Sparing Strategies for ESBL Producers: When and How. (Pubmed Central) -  Feb 10, 2020   
    An important point of the review focuses on piperacillin-tazobactam as the agent arousing the most debate. The most available data regarding non-carbapenem β-lactams (i.e., ceftolozane-tazobactam, ceftazidime-avibactam, temocillin, cephamycins and cefepime) are also thoroughly presented as well as non β-lactams (i.e., aminoglycosides, quinolones, tigecycline, eravacycline and fosfomycin).
  • ||||||||||  Nuzyra (omadacycline) / Paratek, Xerava (eravacycline) / Tetraphase
    Journal:  Semisynthetic Analogues of Anhydrotetracycline as Inhibitors of Tetracycline Destructase Enzymes. (Pubmed Central) -  Feb 9, 2020   
    Inhibitor potency was found to vary as a function of enzyme (major) and substrate-inhibitor pair (minor), and anhydrotetracycline analogue stability to enzymatic and nonenzymatic degradation in solution contributes to their ability to rescue tetracycline activity in whole cell Escherichia coli expressing tetracycline destructase enzymes. Taken collectively, these results provide the framework for the rational design of next-generation inhibitor libraries en route to a viable and proactive adjuvant approach to combat the enzymatic degradation of tetracycline antibiotics.
  • ||||||||||  Comtan (entacapone) / Novartis, Orion, Ongentys (opicapone) / Ono Pharma, Neurocrine
    Journal:  Opicapone for the treatment of Parkinson's disease: an update. (Pubmed Central) -  Feb 7, 2020   
    Dyskinesia was the most common complaint. Further comparative studies and broader trial inclusion criteria are needed to help the decision between COMT inhibitors and to expand the patient spectrum where this drug can be applied.
  • ||||||||||  adavosertib (AZD1775) / AstraZeneca, prexasertib (LY2606368) / Eli Lilly, Pfizer
    Journal:  Synthetic Lethal Targeting of Mitotic Checkpoints in HPV-Negative Head and Neck Cancer. (Pubmed Central) -  Feb 6, 2020   
    These phenotypes were accompanied by more significantly reduced activation of CHK1 and its paralog CHK2, and enhanced CDK1 activation, eliminating breaks on the mitotic entry of cells with DNA damage. These data suggest the potential value of dual inhibition of CHK1 and WEE1 in tumors with compromised G1/S checkpoints.