PI3K inhib 
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  • ||||||||||  Halaven (eribulin mesylate) / Eisai, Aliqopa (copanlisib) / Bayer
    Enrollment open, Enrollment change, Trial completion date, Trial primary completion date, Combination therapy, Metastases:  Testing the Addition of Copanlisib to Eribulin for the Treatment of Advanced-Stage Triple Negative Breast Cancer (clinicaltrials.gov) -  Feb 8, 2023   
    P1/2,  N=106, Recruiting, 
    Suspended --> Recruiting | N=18 --> 106 | Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: Dec 2022 --> Dec 2023
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Compound Kushen injection attenuates angiotensin II‑mediated heart failure by inhibiting the PI3K/Akt pathway. (Pubmed Central) -  Feb 4, 2023   
    Moreover, H9C2 cells were treated with CKI (2 mg/ml) or LY294002 (an inhibitor of the PI3K/Akt pathway; 25 µmol/l) in combination with Ang II (1 µmol/l) for 48 h...On the whole, the present study demonstrates that CKI reduces cardiomyocyte apoptosis, promotes healthy cardiac function and attenuates Ang II‑mediated HF. These ameliorative effects may be associated with the inhibition of the PI3K/Akt pathway.
  • ||||||||||  Journal:  Updates on Diagnosis and Treatment of PIK3CA-Related Overgrowth Spectrum. (Pubmed Central) -  Feb 3, 2023   
    Drugs that inhibit the PI3K pathway offer alternatives to conventional therapies. This article reviews the current knowledge of PROS and summarizes the latest progress in precise treatment, providing new insights into future therapies and research goals.
  • ||||||||||  Sinonasal cancer: Molecular biomarkers for tumor classification and targeted treatment (Hall B1) -  Jan 30, 2023 - Abstract #SarcomaRC2023SARCOMA_RC_14;    
    Candidate therapies include inhibitors of PI3K/MTOR for ITAC, of EGFR and CDK4/6 for SNSCC, of MEK for MMM, of IDH2 for SNUC/SNEC/ONB, and of EZH2 for SNUC/TCS, while DNA repair and FGFR inhibitors may be considered for many of the sinonasal tumor subtypes. Legal entity responsible for the study The author.
  • ||||||||||  Zydelig (idelalisib) / Gilead
    Preclinical, Journal:  Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3Kδ Inhibitors for Hematological Cancer. (Pubmed Central) -  Jan 29, 2023   
    Among them, compound MR3278 showed superior PI3Kδ inhibitory activity (IC = 30 nM), as well as higher inhibitory activity to most of AML cells (e.g., MOLM-16 and Mv-4-11 cells with IC values of 2.6 μM and 3.7 μM, respectively) than Idelalisib...In addition, in silico physicochemical and ADMET evaluation revealed its drug-like properties with satisfactory toxicity profiles. These results indicate that MR3278 can be identified as a promising new lead compound to the current PI3Kδ inhibitor and is worthy of further profiling.
  • ||||||||||  Journal:  Faulty TRPM4 channels underlie age-dependent cerebral vascular dysfunction in Gould syndrome. (Pubmed Central) -  Jan 25, 2023   
    Acute inhibition of PI3K activity and blockade of transforming growth factor-beta (TGF-β) receptors also rescued the myogenic response, suggesting that hyperactivity of TGF-β signaling pathways stimulates PI3K to deplete PIP and impair TRPM4 channels. We conclude that age-related cerebral vascular dysfunction in Col4a1 mice is caused by the loss of depolarizing TRPM4 currents due to PIP depletion, revealing an age-dependent mechanism of cSVD.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Mechanisms of epigenetic regulation and therapeutic response in hormone-driven tumors (Tangerine Ballroom 1 (WF1) - Convention Center) -  Jan 25, 2023 - Abstract #AACR2023AACR_471;    
    40-60% of these cancers also harbor alterations in the phosphoinositide 3-kinase (PI3K) pathway and the PI3K inhibitor alpelisib is approved in combination with anti-ER therapy...In addition, we have discovered the histone lysine methyltransferase KMT2D as an important regulator of ER-PI3K crosstalk in breast cancer. In this talk, I will discuss recent progress in our understanding of the chromatin-based mechanisms of breast tumorigenesis, how these mechanisms affect therapeutic response to standard of care treatment and suggest new strategies towards therapeutic intervention to overcome resistance.
  • ||||||||||  leniolisib (CDZ173) / Pharming Group
    Journal:  Phosphatidyl Inositol 3-Kinase (PI3K)-Inhibitor CDZ173 protects against LPS-induced osteolysis. (Pubmed Central) -  Jan 24, 2023   
    Lastly, CDZ173 inhibited the differentiation and function of osteoclasts by weakening the signal axis of PI3K-AKT/MAPK-NFATc1 in osteoclasts. In conclusion, our results highlight the potential pharmacological role of CDZ173 in preventing osteoclast-mediated inflammatory osteolysis and its potential clinical application.
  • ||||||||||  sorafenib / Generic mfg.
    Journal:  A novel polypeptide encoded by the circular RNA ZKSCAN1 suppresses HCC via degradation of mTOR. (Pubmed Central) -  Jan 24, 2023   
    These results reveal that a novel circZKSCAN1-encoded peptide acts as a tumor suppressor on PI3K/AKT/mTOR pathway, and sensitizes HCC cells to sorafenib via ubiquitination of mTOR. These findings demonstrated that circZKSaa has the potential to serve as a therapeutic target and biomarker for HCC treatment.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Review, Journal:  Targeting PI3K/AKT/mTOR Pathway in Breast Cancer: From Biology to Clinical Challenges. (Pubmed Central) -  Jan 22, 2023   
    This review aims to highlight the central role of PI3K-mTORC1/C2 mutations in the different BC subtypes, in terms of clinical outcomes and treatment efficacy. The broad base of knowledge in tumor biology is a key point for personalized BC therapy in the precision medicine era.
  • ||||||||||  LY294002 / Eli Lilly
    Preclinical, Journal:  GPR30 Alleviates Pressure Overload-Induced Myocardial Hypertrophy in Ovariectomized Mice by Regulating Autophagy. (Pubmed Central) -  Jan 22, 2023   
    In summary, our results demonstrate that G1 can attenuate cardiac hypertrophy and fibrosis and improve the cardiac function of mice in the OVX + TAC group through AKT/mTOR mediated inhibition of autophagy. Thus, this study demonstrates a potential option for the drug treatment of pressure overload-induced cardiac hypertrophy in postmenopausal women.
  • ||||||||||  Estybon (rigosertib) / Onconova, SymBio Pharma, Knight Therap
    Journal:  Another Brick to Confirm the Efficacy of Rigosertib as Anticancer Agent. (Pubmed Central) -  Jan 22, 2023   
    The alterations in the cell cycle and in cell-cycle-related proteins were observed in A549 at lower concentrations than U87-MG. In conclusion, with this article we have demonstrated that Rigosertib has different efficacy depending on the cell line considered and that it could be a potential antineoplastic agent against lung cancer in humans.
  • ||||||||||  emavusertib (CA-4948) / Curis, Dr. Reddy's
    Journal, IO biomarker:  Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors. (Pubmed Central) -  Jan 22, 2023   
    Emavusertib exerted its activity via inhibition of NF-κB signaling and induction of apoptosis. Considering the early safety data from clinical trials, our study identifies the IRAK4 inhibitor emavusertib as a novel compound to be explored in trials for patients with MYD88-mutated indolent B cell lymphomas as single agent and as combination partner with BTK or PI3K inhibitors in unselected populations of patients.
  • ||||||||||  cisplatin / Generic mfg.
    Journal:  Label-free-based quantitative proteomic analysis of the inhibition of cisplatin-resistant ovarian cancer cell proliferation by cucurbitacin B. (Pubmed Central) -  Jan 22, 2023   
    Our study confirmed that cucurbitacin B inhibits the PI3K/Akt/mTOR signaling pathway, targets mTOR, suppresses the proliferation of cisplatin-resistant ovarian cancer cells.And we also found that cucurbitacin B induces DNA damage, activates cGASA and recruits IKBα,playing a crucial role in eliciting anti-tumor immunity. We herein uncovered a new use for CuB in inhibiting tumor-drug resistance, providing a novel approach to overcoming chemotherapeutic drug resistance in ovarian cancer.
  • ||||||||||  Journal:  Harmine suppresses the malignant phenotypes and PI3K activity in breast cancer. (Pubmed Central) -  Jan 20, 2023   
    Moreover, harmine injection also suppressed the tumorigenesis of breast cancer cells. Our results suggested that Hermine could suppress multiple malignant phenotypes and inhibit PI3K signaling, which supports that harmine might be a potential tumor-suppressive natural compound against breast cancer.
  • ||||||||||  Copiktra (duvelisib) / Secura Bio, Yakult Honsha
    Journal:  Duvelisib attenuates bleomycin-induced pulmonary fibrosis via inhibiting the PI3K/Akt/mTOR signalling pathway. (Pubmed Central) -  Jan 19, 2023   
    In vitro and in vivo pharmacological experiments showed that Duvelisib dose-dependently suppressed lung fibroblast activation and improved autophagy inhibition by inhibiting the phosphorylation of PI3K, Akt and mTOR. Our results indicate that Duvelisib can alleviate the severity of pulmonary fibrosis and provide potential drugs for the treatment of pulmonary fibrosis.
  • ||||||||||  Preclinical, Journal, IO biomarker:  Myrislignan Induces Apoptosis in Gastric Cancer Cell Line Through PI3K/AKT Signaling Pathway (Pubmed Central) -  Jan 18, 2023   
    However, PI3K activator attenuated MYR-induced apoptosis in gastric cancer cells and MYR's regulation of PI3K, AKT, BAX, Caspase-3, and Caspase-9 protein expression ( P<0.05). MYR induces the expression of BAX, Caspase-3, and Caspase-9 proteins by inhibiting the PI3K/AKT signaling pathway, thereby promoting the apoptosis of gastric cancer cells.
  • ||||||||||  Journal:  Synthetic methodologies and SAR of quinazoline derivatives as PI3K inhibitors. (Pubmed Central) -  Jan 18, 2023   
    Lapatinib, afatinib, gefitinib, erlotinib, idelalisib and copanlisib are quinazoline-based, FDA-approved PI3K inhibitors, while compounds like NVPBYL719, GDC-0032, AZD8186, AZD-6482, etc. are under different stages of clinical trials. In light of the above-mentioned facts, in the present study, we have reported different synthetic approaches, mechanisms of anticancer action, and structure-activity relationship analysis of reported quinazoline derivatives as PI3K inhibitors to help researchers working in the field in designing better and isoform-selective PI3K inhibitors.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Journal:  The PIK3CA-E545K-SIRT4 signaling axis reduces radiosensitivity by promoting glutamine metabolism in cervical cancer. (Pubmed Central) -  Jan 17, 2023   
    Moreover, the PI3K inhibitor BYL719, but not mTOR inhibitors, exerted remarkable synergistic effects with radiotherapy by inhibiting glutamine metabolism in vitro and in vivo. Collectively, this study reveals the role of PIK3CA-E545K-SIRT4 axis in regulating glutamine metabolism and the radioresistance in cervical cancer, which provides a necessary preliminary basis for clinical research of PI3K inhibitors as radiosensitizing agents.
  • ||||||||||  Piqray (alpelisib) / Novartis
    PK/PD data, Review, Journal:  Pharmacokinetics and Pharmacodynamic of Alpelisib. (Pubmed Central) -  Jan 13, 2023   
    The first, if not fully contra-indicated in (pre-)diabetic patients, warrants a close follow up when treatment is started and a potential dose reduction when needed. Because of its safety profile, alpelisib require stringent patient selection and close follow-up.
  • ||||||||||  Piqray (alpelisib) / Novartis, MK-8776 / Merck (MSD)
    Integrated analyses prioritize therapies for -mutant breast cancer and reveal a pro-survival role for p21 in drug resistance () -  Jan 13, 2023 - Abstract #LCC2023LCC_22;    
    Importantly, targeted inhibition of the check-point inhibitor CHK1 with MK-8776 effectively caused death of p21-high T47D cells thus establishing a new vulnerability of BYL719-resistant breast cancer cells. Together, our integrated studies uncover hidden molecular mediators causing resistance to PI3Ka inhibition and provide a framework to prioritize combination therapies for PI3K mutant breast cancer.
  • ||||||||||  Review, Journal:  The therapeutic potential of arctigenin against multiple human diseases: A mechanistic review. (Pubmed Central) -  Jan 12, 2023   
    Inhibition of PI3K/AKT pathway and activation of AMPK signaling play the pivotal roles in the therapeutic effects of ATG. PI3K/AKT and AMPK signaling widely link to other signaling pathways, modulating various biological processes such as anti-inflammation, anti-oxidative stress, anti-fibrosis, anti-ER stress, anti-steatosis and pro-apoptosis, which constitute the curative mechanisms of ATG against multiple human diseases.