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  • ||||||||||  telaglenastat (CB-839) / Calithera
    Journal:  Glutamine anaplerosis is required for amino acid biosynthesis in human meningiomas. (Pubmed Central) -  Apr 5, 2022   
    Grade-I meningiomas possess relatively higher glutamine metabolism providing carbon/nitrogen for the biosynthesis of key nonessential amino acids. GLS1 inhibitor (CB-839) is very effective in downregulating glutamine metabolic pathways in grade-I meningiomas leading to decreased cellular proliferation.
  • ||||||||||  telaglenastat (CB-839) / Calithera
    Journal:  Pharmacological Inhibition of Glutaminase 1 Attenuates Alkali-Induced Corneal Neovascularization by Modulating Macrophages. (Pubmed Central) -  Apr 5, 2022   
    Treatment with a selective oral GLS1 inhibitor, CB-839 (telaglenastat), significantly decreased the distribution of polarized M2 macrophages in the alkali-injured corneas and suppressed the development of CoNV...Our findings revealed that GLS1 inhibition or glutamine deprivation prevented alkali-induced CoNV by inhibiting the infiltration and M2 polarization of macrophages. This work suggests that pharmacological GLS1 inhibition is a feasible and effective treatment strategy for chemical burn-related CoNV in humans.
  • ||||||||||  telaglenastat (CB-839) / Calithera
    Journal:  Identification and characterization of a novel glutaminase inhibitor. (Pubmed Central) -  Apr 1, 2022   
    Several GLS inhibitors have been identified, of which DON (6-diazo-5-oxonorleucine), BPTES (bis-2-(5-phenylacetamido-1, 3, 4-thiadiazol-2-yl) ethyl sulphide), 968 (5-(3-Bromo-4-(dimethylamino)phenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one) and CB839 (Telaglenastat) are the most widely used...Moreover, C19 inhibits anti-CD3/CD28-induced CD4+ T cell proliferation and cytokine production with similar or greater potency as compared to BPTES. Taken together, our data suggest that C19 has the potential to modulate GLS1 activity and alter metabolic activity of T cells.
  • ||||||||||  sapanisertib (CB-228) / Calithera
    Trial termination, Metastases:  MLN0128 Compared to Sorafenib in Advanced or Metastatic Hepatocellular Carcinoma (clinicaltrials.gov) -  Mar 31, 2022   
    P1/2,  N=11, Terminated, 
    Taken together, our data suggest that C19 has the potential to modulate GLS1 activity and alter metabolic activity of T cells. Active, not recruiting --> Terminated; Funder Decision
  • ||||||||||  mivavotinib (CB-659) / Calithera, Ninlaro (ixazomib) / Takeda
    Trial completion date, Trial termination, Trial primary completion date:  Study Augmenting TAK-659 Action in Relapsed/Refractory AML by Addition Ofthe Proteasome Inhibitor Ixazomib (clinicaltrials.gov) -  Mar 31, 2022   
    P1/2,  N=8, Terminated, 
    Active, not recruiting --> Terminated; Funder Decision Trial completion date: Oct 2023 --> Feb 2022 | Active, not recruiting --> Terminated | Trial primary completion date: Oct 2022 --> Sep 2021; Funder requested termination due to halting internal development of TAK-659
  • ||||||||||  Xospata (gilteritinib) / Astellas
    Journal:  Gilteritinib Inhibits Glutamine Uptake and Utilization in FLT3-ITD-positive AML. (Pubmed Central) -  Mar 26, 2022   
    Collectively, this work has identified a previously unrecognized, gilteritinib-sensitive metabolic pathway downstream of SLC38A1 that causes decreased glutaminolysis and disruption of redox homeostasis. These findings provide a rationale for the development and therapeutic exploration of targeted combinatorial treatment strategies for this subset of relapse/refractory AML.
  • ||||||||||  sapanisertib (CB-228) / Calithera
    Enrollment closed, Combination therapy, Metastases:  Sapanisertib and Metformin in Treating Patients With Advanced or Metastatic Relapsed or Refractory Cancers (clinicaltrials.gov) -  Mar 25, 2022   
    P1,  N=50, Active, not recruiting, 
    This study reports a detailed (phospho)proteomic analysis of the response of BRAF mutant glioma to combined MEK and mTOR pathway inhibition and identifies new targets for the development of rational combination therapies for BRAF-driven tumors. Recruiting --> Active, not recruiting
  • ||||||||||  sapanisertib (CB-228) / Calithera
    Journal:  The mTORC1-eIF4F axis controls paused pluripotency. (Pubmed Central) -  Mar 15, 2022   
    Inhibition of mechanistic target of rapamycin (mTOR) by the kinase inhibitor INK128 is known to induce paused pluripotency in mESCs cultured with traditional serum/LIF medium (SL), but the underlying mechanisms remain unclear...Interestingly, eIF4F also regulates maintenance of pluripotency in an mTORC1-independent but MEK/ERK-dependent manner in SL, indicating that translation of pluripotency genes is controlled differently in SL and 2iL. Our study reveals a detailed picture of how mTOR governs self-renewal in mESCs and uncovers a context-dependent function of eIF4F in pluripotency regulation.
  • ||||||||||  Bylantra (devimistat) / Rafael Pharma, Ono Pharma
    Inhibition of glutaminolysis overcomes metabolic adaptation to devimistat treatment (Section 6) -  Mar 9, 2022 - Abstract #AACR2022AACR_5578;    
    Most importantly, the addition of a GLS1 inhibitor CB-839 to devimistat treatment abrogates the metabolic dependency of HNSCC cells on glutamine, achieving a synergistic anticancer effect in glutamine-addicted HNSCC. These novel and significant findings could lay a scientific foundation for developing more effective treatments targeting the metabolic requirements of HNSCC.
  • ||||||||||  VPS4A inhibitor / Calithera
    Identification of novel VPS4A inhibitors for the treatment of VPS4B-deleted cancers (Section 23) -  Mar 9, 2022 - Abstract #AACR2022AACR_4028;    
    We have discovered a novel series of VPS4A inhibitors and are advancing this inhibitor series through lead optimization. Potent, selective, and pharmacologically active VPS4A inhibitors are expected to be well tolerated and have strong single-agent activity in tumors bearing VPS4B homozygous deletions.
  • ||||||||||  telaglenastat (CB-839) / Calithera, sapanisertib (CB-228) / Calithera
    Targeting amino acid uptake in lung squamous cell carcinomas to improve response to targeted therapies (Section 23) -  Mar 9, 2022 - Abstract #AACR2022AACR_3285;    
    Resistance to targeted therapies is a major hurdle to achieving effective therapies in multiple cancer types. Identifying ways to overcome resistance to targeted therapies would allow for longer therapeutic response for larger number of patients, ultimately leading to longer survival and better quality of life.
  • ||||||||||  telaglenastat (CB-839) / Calithera
    Enrollment closed, Combination therapy, Metastases:  Glutaminase Inhibitor CB-839 and Azacitidine in Treating Patients With Advanced Myelodysplastic Syndrome (clinicaltrials.gov) -  Feb 28, 2022   
    P1/2,  N=40, Active, not recruiting, 
    These findings uncover the critical role of GLS1-mediated glutaminolysis in CPI-613 treatment and suggest that the CB-839 and CPI-613 combination may potentiate synergistic anticancer activity for HNSCC therapeutic gain. Recruiting --> Active, not recruiting
  • ||||||||||  sapanisertib (CB-228) / Calithera
    Enrollment closed, Metastases:  Study of TAK-228 In Patients With Previously Treated Metastatic Renal Cell Carcinoma (clinicaltrials.gov) -  Feb 24, 2022   
    P2,  N=39, Active, not recruiting, 
    Active, not recruiting --> Completed | Trial completion date: Dec 2022 --> Dec 2021 | Trial primary completion date: Dec 2022 --> Dec 2021 Recruiting --> Active, not recruiting
  • ||||||||||  telaglenastat (CB-839) / Calithera
    Journal, Heterogeneity:  Heterogeneity of glutamine metabolism in acquired-EGFR-TKI-resistant lung cancer. (Pubmed Central) -  Feb 19, 2022   
    Trial completion date: Jan 2022 --> Dec 2023 | Trial primary completion date: Dec 2021 --> Dec 2022 These findings suggest that glutamine dependency in acquired EGFR-TKI-resistant lung cancer is heterogeneous and that inhibition of glutamine metabolism by CB-839 may serve as a therapeutic tool for acquired EGFR-TKI-resistant lung cancer.
  • ||||||||||  sirolimus / Generic mfg.
    Review, Journal:  Deficiency in the Treatment Description of mTOR Inhibitor Resistance in Medulloblastoma, a Systematic Review. (Pubmed Central) -  Feb 12, 2022   
    The second-generation mTOR, AZD8055 and sapanisertib, suppressed medulloblastoma cell growth; however, limited studies have investigated possible resistance pathways...This systematic review highlights the mechanisms of resistance of mTOR inhibitors in medulloblastoma and includes IDO1, T cells, Mnk2, and eIF4E, as they prolong malignant cell survival. The findings promote the importance of combination therapy in medulloblastoma due to its highly resistant nature.