^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    PI3K inhibitor

    Related drugs:
    1d
    Chidamide Promotes Osteogenic Differentiation of Bone Marrow Mesenchymal Stromal Cells from Patients with Myelodysplastic Syndromes (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
    Chidamide can inhibit HDAC activity in MSC, upregulate the expression of the osteogenic transcription factor RUNX2, and promote the osteogenic differentiation of MDS-MSC.
    Journal • Stroma
    |
    RUNX2 (RUNX Family Transcription Factor 2)
    |
    Epidaza (chidamide)
    1d
    Ribosomal S6 kinase 2-forkhead box protein O4 signaling pathway plays an essential role in melanogenesis. (PubMed, Sci Rep)
    Unexpectedly, LY294002, a PI3K inhibitor, increased melanogenesis without UV or α-MSH stimulation, suggesting that the PI3K/AKT signaling pathway may not be a major signaling pathway for melanogenesis...In addition, FOXO4-wt overexpression showed that FOXO4 enhance melanin synthesis. Overall, the RSK2-FOXO4 signaling pathway plays a key role in modulating melanogenesis.
    Journal
    |
    RPS6KA3 (Ribosomal Protein S6 Kinase A3)
    |
    LY294002
    2d
    Jiedu Xiaozheng Yin Inhibits the Progression of Colitis Associated Colorectal Cancer by Stimulating Macrophage Polarization Towards an M1 Phenotype via the TLR4 Pathway. (PubMed, Integr Cancer Ther)
    Subsequently, after antagonizing the TLR4 pathway with antagonists (TAK242, PDTC, KG501, SR11302, LY294002), the expression of IL-6, TNF-α, iNOS, and IL-1β mRNA were detected by RT-qPCR. Furthermore, JXY inhibited M1-related molecules such as IL-6, TNF-α, iNOS, and IL-1β after antagonizing the TLR4 pathway. Obviously, JXY could exhibit inhibitory effects on the development of colon tumors in mice with CAC by promoting M1 polarization through TLR4-mediated signaling and impeding M2 polarization of macrophages.
    Journal
    |
    IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL10 (Interleukin 10) • IL1B (Interleukin 1, beta) • MRC1 (Mannose Receptor C-Type 1) • CD80 (CD80 Molecule) • CD86 (CD86 Molecule)
    |
    IL6 expression
    |
    LY294002
    3d
    Astaxanthin suppresses the malignant behaviors of nasopharyngeal carcinoma cells by blocking PI3K/AKT and NF-κB pathways via miR-29a-3p. (PubMed, Genes Environ)
    Astaxanthin significantly suppresses NPC cell proliferation, cell cycle arrest, migration, invasion while promoting cell apoptosis by inactivating PI3K/AKT and NF-κB pathways. The study first reveals the anticancer role of astaxanthin in NPC, providing a potential candidate for NPC treatment.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • MIR29A (MicroRNA 29a)
    |
    LY294002
    4d
    ENGAGE: A Trial of Enzastaurin Plus Temozolomide During and Following Radiation Therapy in Patients With Newly Diagnosed Glioblastoma With or Without the Novel Genomic Biomarker, DGM1 (clinicaltrials.gov)
    P3, N=260, Completed, Denovo Biopharma LLC | Active, not recruiting --> Completed | Trial completion date: Jun 2025 --> Feb 2024 | Trial primary completion date: Jun 2025 --> Feb 2024
    Trial completion • Trial completion date • Trial primary completion date
    |
    MGMT (6-O-methylguanine-DNA methyltransferase)
    |
    MGMT promoter methylation
    |
    temozolomide • Kinenza (enzastaurin)
    6d
    Knockdown of SETD5 Inhibits Colorectal Cancer Cell Growth and Stemness by Regulating PI3K/AKT/mTOR Pathway. (PubMed, Biochem Genet)
    Mechanistically, by blocking PI3K/AKT/mTOR pathway with BEZ235, the effects of SETD5 overexpression on cell viability and Nanog and Sox2 protein expression were reversed. Our results substantiated that SETD5 functioned as an oncogene by promoting cell growth and stemness in colorectal cancer cells through activating the PI3K/AKT/mTOR signaling pathway.
    Journal
    |
    SOX2 • NANOG (Nanog Homeobox) • SETD5 (SET Domain Containing 5)
    |
    SETD5 overexpression • SOX2 expression
    |
    dactolisib (RTB101)
    8d
    LncRNA NEAT1 promotes MPP+ induced injury of PC12 cells and accelerates the progression of Parkinson's disease in mice through FUS mediated inhibition of PI3K/AKT/mTOR signalling pathway. (PubMed, Exp Gerontol)
    The brain tissue of NEAT1-silenced PD mice had decreased inflammatory infiltration and apoptosis and increased neurological scores. In conclusion, NEAT1 is involved in PD progression through FUS-mediated inhibition of the PI3K/AKT/mTOR signalling pathway.
    Preclinical • Journal
    |
    SQSTM1 (Sequestosome 1) • NEAT1 (Nuclear Paraspeckle Assembly Transcript 1) • FUS (FUS RNA Binding Protein)
    8d
    LncRNA SNHG1 overexpression alleviates osteoarthritis via activating PI3K/Akt signal pathway and suppressing autophagy. (PubMed, Immunobiology)
    However, rapamycin (RAPA, an autophagy activator) and LY294002 (a PI3K inhibitor) reversed the effects of SNHG1 overexpression on the viability and apoptosis of chondrocytes as well as on the proteins related to PI3K/Akt pathway and autophagy. In OA-modeled mice, SNHG1 overexpression prevented the loss of chondrocytes via the activation of PI3K/Akt pathway and the suppression of autophagy. SNHG1 overexpression might inhibit the apoptosis of chondrocytes by promoting PI3K/Akt pathway and inhibiting autophagy.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • IL1B (Interleukin 1, beta) • SNHG1 (Small Nucleolar RNA Host Gene 1)
    |
    BCL2 expression
    |
    sirolimus • LY294002
    8d
    STX-478-101: First-in-Human Study of STX-478 as Monotherapy and in Combination With Other Antineoplastic Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=400, Recruiting, Scorpion Therapeutics, Inc. | Trial completion date: Apr 2028 --> Feb 2029 | Trial primary completion date: Apr 2026 --> Feb 2027
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    fulvestrant • STX-478
    12d
    Chidamide plus envafolimab as subsequent treatment in advanced non-small cell lung cancer patients resistant to anti-PD-1 therapy: A multicohort, open-label, phase II trial with biomarker analysis. (PubMed, Cancer Med)
    Combination of chidamide and envafolimab showed efficacy signals in certain NSCLC patients. But further identification of beneficial population is necessary for precision treatment.
    P2 data • Clinical Trial,Phase II • Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker • Metastases
    |
    TMB (Tumor Mutational Burden) • HDAC2 (Histone deacetylase 2)
    |
    PD-L1 negative • HDAC2 expression
    |
    Epidaza (chidamide) • Enweida (envafolimab)
    13d
    Connexin 43 Prevents Radiation-Induced Intestinal Damage via the Ca2+-Dependent PI3K/Akt Signaling Pathway. (PubMed, Radiat Res)
    Administration of the PI3K/AKT pathway inhibitor LY294002 inhibited the radioprotective effects in Cx43-overexpressing intestinal epithelial cells. Our study demonstrated that Cx43 expression is decreased by ionizing radiation, which facilitates the radioprotection of intestinal epithelial cells.
    Journal
    |
    GJA1 (Gap Junction Protein Alpha 1)
    |
    GJA1 expression • GJA1 overexpression
    |
    LY294002
    16d
    Enhancing therapeutic efficacy in luminal androgen receptor triple-negative breast cancer: exploring chidamide and enzalutamide as a promising combination strategy. (PubMed, Cancer Cell Int)
    This study confirmed that the combination of histone deacetylase (HDAC) inhibitors and androgen receptor (AR) antagonists possessed greater therapeutic efficacy than monotherapy in LAR TNBC. This finding significantly bolsters the theoretical basis for the clinical translation of this combination therapy and provides an innovative strategy for the targeted treatment of LAR TNBC.
    Journal
    |
    AR (Androgen receptor)
    |
    Xtandi (enzalutamide capsule) • Epidaza (chidamide)
    17d
    Exploring the Mechanism of KLF15 on the Biological Activity and Autophagy of Gastric Cancer Cells based on PI3K/Akt/Mtor Signaling Pathway. (PubMed, Comb Chem High Throughput Screen)
    Overexpression of KLF15 can inhibit the proliferation and invasion of Gastric cancer cells and promote cell apoptosis and autophagy, and its mechanism may be related to the regulation of the PI3K/Akt/mTOR signaling pathway.
    Journal
    |
    IGF1 (Insulin-like growth factor 1) • BECN1 (Beclin 1)
    |
    LY294002
    17d
    Gedatolisib in Combination With Darolutamide in Metastatic Castration-Resistant Prostate Cancer (clinicaltrials.gov)
    P1/2, N=54, Recruiting, Celcuity Inc | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    gedatolisib (PF-05212384) • Nubeqa (darolutamide)
    17d
    TFE3/PI3K/Akt/mTOR axis in renal cell carcinoma affects tumor microenvironment. (PubMed, Am J Pathol)
    When RCC cells were treated with a PI3K inhibitor (LY294002), TFE3 expression increased and phospho-Akt expression decreased. TFE3 is related to the PI3K/Akt pathway in RCC, and our results suggest that PI3K/Akt inhibitors may potentially aid in treatment of patients with RCC by affecting tumor microenvironment.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • TFE3
    |
    LY294002
    17d
    Tucidinostat, Azacitidine Combined With CHOP Versus CHOP in Patients With Untreated Peripheral T-cell Lymphoma (clinicaltrials.gov)
    P3, N=107, Recruiting, Peking Union Medical College Hospital | Not yet recruiting --> Recruiting | Trial primary completion date: Oct 2023 --> May 2024
    Enrollment open • Trial primary completion date
    |
    azacitidine • cyclophosphamide • epirubicin • Epidaza (chidamide)
    19d
    Study of a patient with Myelodysplastic/myeloproliferative neoplasm with co-morbid neutrophilia and a novel NCOR1::GLYR1 fusion gene (PubMed, Zhonghua Yi Xue Yi Chuan Xue Za Zhi)
    NCOR1::GLYR1 gene is considered as the pathogenic factor for the MDS/MPN patient with neutropenia.
    Journal • IO biomarker
    |
    NCOR1 (Nuclear Receptor Corepressor 1)
    |
    cytarabine • decitabine • Epidaza (chidamide) • aclarubicin
    21d
    Class I HDAC inhibitors enhance antitumor efficacy and persistence of CAR-T cells by activation of the Wnt pathway. (PubMed, Cell Rep)
    Here, we identify class I histone deacetylase inhibitors (HDACi) as boosters of CAR-T cell function by high-throughput screening of chromatin-modifying drugs, in which M344 and chidamide enhance memory maintenance and resistance to exhaustion of CAR-T cells that induce sustained antitumor efficacy both in vitro and in vivo...Multi-omics analyses from RNA-seq, ATAC-seq, and H3K27ac CUT&Tag-seq show that HDACi upregulate expression of TCF4, LEF1, and CTNNB1, which subsequently activate the canonical Wnt/β-catenin pathway. Collectively, our findings elucidate the functional roles of class I HDACi in enhancing CAR-T cell function, which provides the basis and therapeutic targets for synergic combination of CAR-T cell therapy and HDACi treatment.
    Journal • CAR T-Cell Therapy • IO biomarker
    |
    HDAC1 (Histone Deacetylase 1) • TCF4 (Transcription Factor 4)
    |
    CTNNB1 expression
    |
    Epidaza (chidamide)
    21d
    Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia. (PubMed, J Med Chem)
    Mechanistically, (S)-36 could robustly inhibit the PI3K/AKT pathway for significant suppression of cell proliferation and remarkable induction of apoptosis both in vitro and in vivo. Thus, compound (S)-36 represents a promising PI3Kδ inhibitor for the treatment of acute myeloid leukemia with high efficacy.
    Journal
    |
    PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta)
    21d
    Lycium barbarum polysaccharide reverses drug resistance in oxaliplatin-resistant colon cancer cells by inhibiting PI3K/AKT-dependent phosphomannose isomerase. (PubMed, Front Pharmacol)
    It further verified the results of our in vitro and in vivo experiments, showing the involvement of multi-component, multi-target, and multi-pathway synergism in the drug-reversing effect of LBP in CC. Overall, the findings of the present study provide new avenues for the future clinical treatment of CC.
    Journal • IO biomarker
    |
    EGFR (Epidermal growth factor receptor) • BCL2 (B-cell CLL/lymphoma 2) • HRAS (Harvey rat sarcoma viral oncogene homolog) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • IL17A (Interleukin 17A) • MAPK3 (Mitogen-Activated Protein Kinase 3)
    |
    ABCG2 expression
    |
    oxaliplatin
    22d
    IPATunity150: A Study of Ipatasertib Plus Palbociclib and Fulvestrant Versus Placebo Plus Palbociclib and Fulvestrant in Hormone Receptor Positive and HER2 Negative Locally Advanced Unresectable or Metastatic Breast Cancer (clinicaltrials.gov)
    P3, N=20, Terminated, Hoffmann-La Roche | Completed --> Terminated; The decision to not open the Phase III portion was based on a strategic sponsor decision and not driven by any safety concerns.
    Trial termination • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • fulvestrant • ipatasertib (RG7440)
    22d
    Matrine Enhances the Antitumor Efficacy of Chidamide in CTCL by Promoting Apoptosis. (PubMed, Recent Pat Anticancer Drug Discov)
    Our data have demonstrated chidamide combined with matrine to exhibit elevated antitumor activity in both CTCL cells and xenograft models of NOD/SCID mice, which may be a potential treatment option for CTCL.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • CDH1 (Cadherin 1)
    |
    CDH1 expression
    |
    Epidaza (chidamide)
    22d
    PQR309, a dual PI3K/mTOR inhibitor, synergizes with gemcitabine by impairing the GSK-3β and STAT3/HSP60 signaling pathways to treat nasopharyngeal carcinoma. (PubMed, Cell Death Dis)
    Mechanistically, PQR309 sensitized NPC to gemcitabine by increasing caspase pathway-dependent apoptosis, blocking GSK-3β and STAT3/HSP60 signaling, and ablating epithelial-mesenchyme transition. Thus, targeting PI3K/mTOR using PQR309 might represent a treatment option to promote the response to gemcitabine in NPC, and provides a theoretical foundation for the study of targeted drugs combined with chemotherapy for NPC.
    Journal
    |
    HSPD1 (Heat Shock Protein Family D (Hsp60) Member 1)
    |
    gemcitabine • bimiralisib (PQR309)
    24d
    Lactobacillus rhamnosus HN001 facilitates the efficacy of dual PI3K/mTOR inhibition prolonging cardiac transplant survival and enhancing antitumor effect. (PubMed, Microbiol Spectr)
    We administered a combination therapy of phosphoinositide 3-kinase/mammalian target of rapamycin (PI3K/mTOR) dual inhibitor BEZ235 and Lactobacillus rhamnosus HN001 to primary liver cancer model mice with cardiac allografts...We also found that this phenomenon was accompanied by the regulation of inflammatory IL-6 expression. Our study presents a novel and effective therapeutic approach to address antitumor immunity and prevent allograft rejection.
    Journal
    |
    IL6 (Interleukin 6)
    |
    IL6 expression
    |
    dactolisib (RTB101)
    24d
    Gedatolisib in combination with palbociclib and endocrine therapy in women with hormone receptor-positive, HER2-negative advanced breast cancer: results from the dose expansion groups of an open-label, phase 1b study. (PubMed, Lancet Oncol)
    Gedatolisib plus palbociclib and endocrine therapy showed a promising objective response rate compared with the published results for standard-of-care therapies and had an acceptable safety profile.
    P1 data • Journal • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HR positive • HER-2 negative • PIK3CA mutation • HR positive + HER-2 negative • PTEN mutation + HR positive
    |
    Ibrance (palbociclib) • fulvestrant • letrozole • gedatolisib (PF-05212384)
    27d
    Osteopontin promotes tumor growth and metastasis and GPX4-mediated anti-lipid peroxidation in triple-negative breast cancer by activating the PI3k/Akt/mTOR pathway. (PubMed, J Cancer Res Clin Oncol)
    OPN promoted tumor sphere formation and angiogenesis in TNBC by activating the PI3K/AKT/mTOR pathway to regulate GPX4-mediated anti-lipid peroxidation levels.
    Journal
    |
    SPP1 (Secreted Phosphoprotein 1) • GPX4 (Glutathione Peroxidase 4)
    |
    SPP1 elevation
    |
    LY294002
    29d
    GDC-0084 With Radiation Therapy for People With PIK3CA-Mutated Solid Tumor Brain Metastases or Leptomeningeal Metastases (clinicaltrials.gov)
    P1, N=21, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=36 --> 21
    Enrollment closed • Enrollment change
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta) • INPP4B (Inositol polyphosphate-4-phosphatase type II B) • AKT2 (V-akt murine thymoma viral oncogene homolog 2) • INPP5D (Inositol Polyphosphate-5-Phosphatase D) • PIK3C3 (Phosphatidylinositol 3-Kinase Catalytic Subunit Type 3) • PIK3R2 (Phosphoinositide-3-Kinase Regulatory Subunit 2 ) • PIK3R3 (Phosphoinositide-3-Kinase Regulatory Subunit 3)
    |
    paxalisib (GDC-0084)
    1m
    HBI-8000 improves heart failure with preserved ejection fraction via the TGF-β1/MAPK signalling pathway. (PubMed, J Cell Mol Med)
    In conclusion, our data suggest that HBI-8000 inhibits fibrosis by modulating the TGF-β1/MAPK pathway thereby improving HFpEF. Therefore, HBI-8000 may become a new hope for the treatment of HFpEF patients.
    Journal
    |
    TGFB1 (Transforming Growth Factor Beta 1)
    |
    Epidaza (chidamide)
    1m
    The roles of autophagy, ferroptosis and pyroptosis in the anti-ovarian cancer mechanism of harmine and their crosstalk. (PubMed, Sci Rep)
    LY294002 and siFOXO3 rescued the inhibition of the PI3K/AKT/mTOR/FOXO3 signalling pathway and the promotion of autophagy by Har...Interestingly, pretreatment with chloroquine (CQ), erastin, rapamycin (Rap), or ferrostatin-1 (Fer-1) increased or reversed the ferroptosis and pyroptosis promoted by Har, respectively...In conclusion, Har exerts its anti-ovarian cancer effect not only by promoting autophagy by regulating the PI3K/AKT/mTOR/FOXO3 signalling pathway but also by promoting ferroptosis and pyroptosis. Additionally, there is complex crosstalk between autophagy, ferroptosis, and pyroptosis in ovarian cancer.
    Journal
    |
    GPX4 (Glutathione Peroxidase 4) • ATG5 (Autophagy Related 5)
    |
    sirolimus • LY294002 • erastin • chloroquine phosphate
    1m
    Study of CYH33 in Combination With Olaparib an Oral PARP Inhibitor in Patients With Advanced Solid Tumors. (clinicaltrials.gov)
    P1, N=24, Terminated, Haihe Biopharma Co., Ltd. | N=350 --> 24 | Recruiting --> Terminated; Business decision
    Enrollment change • Trial termination • Combination therapy • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MUC16 (Mucin 16, Cell Surface Associated)
    |
    PIK3CA mutation
    |
    Lynparza (olaparib) • CYH33
    1m
    Design, synthesis and activity evaluation of arctigenin derivatives with HDAC inhibition activity. (PubMed, RSC Adv)
    Among them, compound B7 exhibited significantly higher antiproliferative activity in the MV411 cell line compared to the positive control, tucidinostat...Further mechanistic studies indicated that compound B7 induced apoptosis through the Caspase-3 pathway in MV411 cells and enhanced histone acetylation levels in the MV411 cell line. These findings highlight the broad potential application of these arctigenin derivatives in cancer therapy.
    Journal
    |
    CASP3 (Caspase 3)
    |
    Epidaza (chidamide)
    1m
    Identification of Novel PI3Kα Inhibitor Against Gastric Cancer: QSAR-, Molecular Docking-, and Molecular Dynamics Simulation-Based Analysis. (PubMed, Appl Biochem Biotechnol)
    Furthermore, compound 1-(3-(2,4-dimethylthiazol-5-YL)-4-oxo-2,4-dihydroindeno[1,2-C]pyrazol-5-YL)-3-(4-methylpiperazin-1-YL) urea was selected as a potential hit in the final screening by analyzing a number of parameters, including the Rg, RMSD, RMSF, H bonding, and SASA profile. Therefore, we conclude that compound 1-(3-(2, 4-dimethylthiazol-5-YL)-4-oxo-2,4-dihydroindeno[1,2-C]pyrazol-5-YL)-3-(4-methylpiperazin-1-YL) urea has efficient inhibitory potential against PI3Kalpha protein and could be utilized for the development of effective drugs against GC.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    1m
    Combining VPS34 inhibitors with STING agonists enhances type I interferon signaling and anti-tumor efficacy. (PubMed, Mol Oncol)
    These results show that VPS34 inhibition augments the cGAS/STING pathway, leading to greater tumor control through immune-mediated mechanisms. We propose that pharmacological VPS34 inhibition may synergize with emerging therapies targeting the cGAS/STING pathway.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CXCL10 (Chemokine (C-X-C motif) ligand 10) • STING (stimulator of interferon response cGAMP interactor 1) • CGAS (Cyclic GMP-AMP Synthase)
    |
    SB02024
    1m
    A novel pan-PI3K inhibitor KTC1101 synergizes with anti-PD-1 therapy by targeting tumor suppression and immune activation. (PubMed, Mol Cancer)
    KTC1101's dual mechanism of action-directly inhibiting tumor cell growth and dynamically enhancing the immune response- represents a significant advancement in cancer treatment strategies. These findings support incorporating KTC1101 into future oncologic regimens to improve the efficacy of immunotherapy combinations.
    Journal
    |
    CD8 (cluster of differentiation 8)
    1m
    STX-478-101: First-in-Human Study of STX-478 as Monotherapy and in Combination With Other Antineoplastic Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=400, Recruiting, Scorpion Therapeutics, Inc. | N=220 --> 400 | Trial completion date: Jun 2026 --> Apr 2028
    Enrollment change • Trial completion date • Combination therapy • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    fulvestrant • STX-478
    1m
    Chidamide enhances T-cell-mediated anti-tumor immune function by inhibiting NOTCH1/NFATC1 signaling pathway in ABC-type diffuse large B-cell lymphoma. (PubMed, Leuk Lymphoma)
    It can also improve the abnormal DLBCL microenvironment in which immune escape occurs, and inhibit immune escape. This study provides a new therapeutic idea for the exploration of individualized precision therapy for patients with malignant lymphoma.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    NOTCH1 (Notch 1) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • CD4 (CD4 Molecule) • IL2 (Interleukin 2) • IL10 (Interleukin 10) • NFATC1 (Nuclear Factor Of Activated T Cells 1)
    |
    PD-1 expression • HAVCR2 expression • NOTCH1 expression
    |
    Epidaza (chidamide)
    1m
    Inhibition of PI3K/AKT signaling using BKM120 reduced the proliferation and migration potentials of colorectal cancer cells and enhanced cisplatin-induced cytotoxicity. (PubMed, Mol Biol Rep)
    Based on our results, inhibition of PI3K/AKT signaling can be a promising approach, either as a single modality or in combination with Cisplatin. However, further clinical studies should be performed to improve our understanding.
    Journal
    |
    ANXA5 (Annexin A5)
    |
    cisplatin • buparlisib (AN2025)
    1m
    The antitumor effects of herbal medicine Triphala on oral cancer by inactivating PI3K/Akt signaling pathway: based on the network pharmacology, molecular docking, in vitro and in vivo experimental validation. (PubMed, Phytomedicine)
    Triphala exerted significant inhibitory effects on cell metabolic activity, migration, invasion, and proliferation in OSCC cell lines, accompanied by the induction of apoptosis, which was mediated through the inactivation of the PI3K/Akt pathway.
    Preclinical • Journal
    |
    EGFR (Epidermal growth factor receptor) • ER (Estrogen receptor) • JUN (Jun proto-oncogene) • RELA (RELA Proto-Oncogene)
    |
    LY294002
    1m
    Safety, Pharmacokinetics and Efficacy of Paxalisib (GDC-0084) in Newly-diagnosed Glioblastoma (clinicaltrials.gov)
    P2, N=30, Completed, Kazia Therapeutics Limited | Active, not recruiting --> Completed
    Trial completion
    |
    temozolomide • paxalisib (GDC-0084)
    1m
    LncRNA SNHG11 promotes malignant progression of colorectal cancer cells through the PI3K/Akt/mTOR signaling pathway (PubMed, Zhonghua Yi Xue Za Zhi)
    Phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR) signalling pathway inhibitor LY294002 was used for rescue experiments... LncRNA SNHG11 is highly expressed in colorectal cancer. lncRNA SNHG11 can promote the malignant progression of colorectal cancer cells by regulating the PI3K/Akt/mTOR signaling pathway, and this finding provides a new theoretical basis for targeted therapy of colorectal cancer.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1) • CDH1 (Cadherin 1) • BAX (BCL2-associated X protein) • VIM (Vimentin) • CDH2 (Cadherin 2) • MMP9 (Matrix metallopeptidase 9) • SNHG11 (Small Nucleolar RNA Host Gene 11)
    |
    BCL2 expression • CDH1 expression • BAX expression • VIM expression
    |
    LY294002
    1m
    Mass Balance Recovery, Metabolite Profile, and Metabolite Identification of [14C]-Paxalisib in Healthy Male Subjects (clinicaltrials.gov)
    P1, N=6, Completed, Kazia Therapeutics Limited | Active, not recruiting --> Completed | Trial completion date: Mar 2023 --> Jan 2024
    Trial completion • Trial completion date
    |
    paxalisib (GDC-0084)
    1m
    Gypenoside induces apoptosis by inhibiting the PI3K/AKT/mTOR pathway and enhances T-cell antitumor immunity by inhibiting PD-L1 in gastric cancer. (PubMed, Front Pharmacol)
    Gypenoside induced the apoptosis of gastric cancer cells by inhibiting the PI3K/AKT/mTOR pathway and simultaneously inhibited the expression of PD-L1 in gastric cancer cells, thus enhancing the antitumor immunity of T cells. This study provides a theoretical basis for applying gypenoside as a new therapeutic agent to enhance the efficacy of immunotherapy in gastric cancer.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • STAT3 (Signal Transducer And Activator Of Transcription 3)
    |
    PD-L1 expression