zotiraciclib (TG02) / Cothera Biosci 
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 20 Diseases   1 Trial   1 Trial   104 News 


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  • ||||||||||  zotiraciclib (TG02) / Cothera Biosci
    Review, Journal:  Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications. (Pubmed Central) -  Apr 2, 2024   
    Several potent small molecule inhibitors, exemplified by TG02 (4), have progressed to clinical trials...Our focus extends to various types of inhibitors, including pan-inhibitors, selective inhibitors, dual-target inhibitors, degraders, PPI inhibitors, and natural products. The discussion encompasses chemical structures, structure-activity relationships (SARs), biological activities, selectivity, and therapeutic potential, providing detailed insight into the diverse landscape of CDK9 inhibitors.
  • ||||||||||  bemcentinib (BGB324) / BerGenBio, repotrectinib (TPX-0005) / BMS
    Journal:  The promising impact of Bemcentinib and Repotrectinib on sleep impairment in Alzheimer's disease. (Pubmed Central) -  Nov 4, 2023   
    We report Bemcentinib and Repotrectinib, formerly prescribed for cancer, as potential inhibitors of the CK1 ?. Besides their high binding affinity compared to ATP, they can inhibit all ATP-binding sites and alter the tau binding stability.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  Journal:  An Overview of CDK Enzyme Inhibitors in Cancer Therapy. (Pubmed Central) -  Jun 19, 2023   
    CDKIs are CDK4/6, CDK7, CDK9, and CDK12 inhibitors. Finally, we have looked into the efficacy of CDK inhibitors and PD1/PDL1 antibodies when used together, which could lead to the development of a viable cancer treatment strategy.
  • ||||||||||  zotiraciclib (TG02) / Cothera Biosci
    Targeting the selective vulnerability of IDH-mutant glioma with zotiraciclib (West/Central Hall) -  Sep 28, 2022 - Abstract #SNO2022SNO_510;    
    Low-dose exposure of zotiraciclib induces cell death and suppresses transcriptional process and mitochondrial biogenesis in IDH-mutant glioma, not in IDH-wt tumors. These findings support a clinical trial testing zotiraciclib in IDH-mutated glioma.
  • ||||||||||  zotiraciclib (TG02) / Cothera Biosci
    Trial completion date, Trial primary completion date:  STEAM: Study of TG02 in Elderly Newly Diagnosed or Adult Relapsed Patients With Anaplastic Astrocytoma or Glioblastoma (clinicaltrials.gov) -  Mar 28, 2022   
    P1,  N=71, Active, not recruiting, 
    Once validated, polymorphisms predicting drug metabolism may allow personalized dosing of zotiraciclib. Trial completion date: Jan 2022 --> May 2022 | Trial primary completion date: Jan 2022 --> May 2022
  • ||||||||||  paxalisib (GDC-0084) / Kazia, zotiraciclib (TG02) / Adastra Pharma
    COMBINATORIAL THERAPY TARGETING TRANSCIPTION AND IMMUNO-METABOLISM IN RECURRENT GLIOBLASTOMA () -  Nov 16, 2021 - Abstract #SNO2021SNO_1230;    
    Overall, these data suggest that combining TG02 and GDC-0084 is an effective treatment for recurrent GBMs. Furthermore, our results support the use of a translational research platform consisting of a personalized pharmaco-genomics testing, using patient-derived tumor samples towards designing more effective treatment for recurrent GBM patients.
  • ||||||||||  zotiraciclib (TG02) / Cothera Biosci
    Enrollment closed, Trial completion date, Trial primary completion date:  STEAM: Study of TG02 in Elderly Newly Diagnosed or Adult Relapsed Patients With Anaplastic Astrocytoma or Glioblastoma (clinicaltrials.gov) -  Sep 21, 2021   
    P1,  N=71, Active, not recruiting, 
    Furthermore, our results support the use of a translational research platform consisting of a personalized pharmaco-genomics testing, using patient-derived tumor samples towards designing more effective treatment for recurrent GBM patients. Recruiting --> Active, not recruiting | Trial completion date: Aug 2020 --> Jan 2022 | Trial primary completion date: Aug 2020 --> Jan 2022
  • ||||||||||  zotiraciclib (TG02) / Adastra Pharma
    [VIRTUAL] New therapies under investigation: What is TG02? (Channel 1) -  Aug 20, 2021 - Abstract #EANO2021EANO_65;    
    Given the lack of standard therapy for ATRTs, these findings help fill an unmet need and support further study of TG02 as a potential therapeutic option for patients with this deadly disease. There is no abstract associated with this presentation.
  • ||||||||||  Review, Journal:  CDK inhibitors in cancer therapy, an overview of recent development. (Pubmed Central) -  Jun 8, 2021   
    These CDKIs include CDK4/6, CDK7, CDK9, and CDK12/13 inhibitors. Finally, the efficacy and discrepancy of combination therapy with CDK inhibitors and PD1/PDL1 antibodies were analyzed, which might give insights into the development of promising strategy for cancer treatment.
  • ||||||||||  zotiraciclib (TG02) / Cothera Biosci
    Trial completion date, Trial primary completion date:  Phase I Clinical Study of Oral TG02 Capsule in the Treatment of Recurrent / Progressive High-grade Glioma Patients (clinicaltrials.gov) -  Apr 13, 2020   
    P1,  N=15, Recruiting, 
    These results set the stage for further investigation of these clinically advanced compounds for treatment of infections caused by the free-living amebae, including treatment of the highly fatal meningoencephalitis. Trial completion date: Dec 2019 --> Oct 2020 | Trial primary completion date: Oct 2019 --> Aug 2020
  • ||||||||||  zotiraciclib (TG02) / Adastra Pharma
    Journal, IO Biomarker:  Interferon-β sensitizes human glioblastoma cells to the cyclin-dependent kinase inhibitor, TG02. (Pubmed Central) -  Mar 30, 2020   
    In summary, these data suggest that type I IFN may be combined with TG02 to limit glioblastoma growth, but that the well characterized effects of IFN and TG02 on apoptotic signaling are dispensable for synergistic tumor growth inhibition. Instead, exploring how IFN signaling primes glioma cells for TG02-mediated direct target inhibition may help to design novel and effective pharmacological approaches to glioblastoma.
  • ||||||||||  zotiraciclib (TG02) / Adastra Pharma
    Interferon-β sensitizes human glioblastoma cells to the cyclin-dependent kinase inhibitor, TG02 (Ballroom Lawn) -  Oct 29, 2019 - Abstract #SNO2019SNO_406;    
    In summary, these data suggest that type I IFN may be combined with TG02 to limit glioblastoma growth but the well characterized effects of IFN and TG02 on apoptotic signaling are dispensable for synergistic control of tumor growth. Instead, exploring how IFN signaling primes glioma cells for TG02-mediated direct target inhibition may help to design novel, more effective pharmacological approaches to glioblastoma.
  • ||||||||||  zotiraciclib (TG02) / Cothera Biosci
    Enrollment change, Trial withdrawal, Metastases:  Study of TG02 Citrate in Patients With Advanced Hepatocellular Carcinoma (clinicaltrials.gov) -  Sep 24, 2019   
    P1,  N=0, Withdrawn, 
    Instead, exploring how IFN signaling primes glioma cells for TG02-mediated direct target inhibition may help to design novel, more effective pharmacological approaches to glioblastoma. N=32 --> 0 | Not yet recruiting --> Withdrawn
  • ||||||||||  zotiraciclib (TG02) / Adastra Pharma
    Clinical, Journal:  Novel Targeting of Transcription and Metabolism in Glioblastoma. (Pubmed Central) -  Sep 14, 2019   
    N=32 --> 0 | Not yet recruiting --> Withdrawn TG02 inhibits multiple survival mechanisms and synergistically decreases energy production with temozolomide, representing a promising therapeutic strategy in GBM, currently under investigation in an ongoing clinical trial.
  • ||||||||||  zotiraciclib (TG02) / Adastra Pharma
    Journal:  TG02 inhibits proteasome inhibitor-induced HSF1 serine 326 phosphorylation and heat shock response in multiple myeloma. (Pubmed Central) -  Jan 4, 2018   
    Initiation date: Dec 2017 --> Apr 2018 | Trial completion date: Jun 2020 --> Aug 2020 | Trial primary completion date: Jun 2020 --> Aug 2020 Proteasome inhibition activates multiple kinases in myeloma cells resulting in the phosphorylation of p53, HSP27, c-JUN, and HSF1.TG02 inhibits proteasome inhibitor (PI)-induced HSF1 pS326, representing a novel mechanism for a TG02 and PI combination.
  • ||||||||||  carfilzomib / Generic mfg., zotiraciclib (TG02) / Adastra Pharma
    Journal:  Dual Inhibition of Mcl-1 by the Combination of Carfilzomib and TG02 In Multiple Myeloma. (Pubmed Central) -  Sep 13, 2017   
    Taken together our data suggest that dual inhibition of Mcl-1 via decreased expression and the induction of its antagonist NOXA by the combination of carfilzomib and TG02 is active in myeloma and warrants further testing preclinically and in clinical trials. Moreover, regulation of Mcl-1 by TG02 is more complex than initially appreciated.