^
    5d
    Rituximab-Chidamide combination chemotherapy enhances autophagy to overcome drug resistance in diffuse large B-cell lymphoma. (PubMed, Int Immunopharmacol)
    These findings suggest that the BTG1/BECN1/ATG5 signaling axis plays a critical role in enhancing autophagy and reversing Rituximab resistance. The combination of Chidamide and Rituximab presents a promising therapeutic strategy, offering new insights into overcoming drug resistance in DLBCL.
    Journal
    |
    PTEN (Phosphatase and tensin homolog) • ATG5 (Autophagy Related 5) • BECN1 (Beclin 1) • MAPK8 (Mitogen-activated protein kinase 8) • HSPA8 (Heat Shock Protein Family A (Hsp70) Member 8)
    |
    Rituxan (rituximab) • Epidaza (chidamide)
    6d
    Desmoplastic small round cell tumor: an update of current management practices. (PubMed, J Egypt Natl Canc Inst)
    This comprehensive review provides a current understanding of DSRCT diagnosis and treatment modalities, highlighting the ongoing challenges and promising avenues for future research. The integration of personalized approaches, novel chemotherapeutic agents, and evolving immunotherapy strategies holds the potential to enhance outcomes for individuals with DSRCT.
    Review • Journal
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • AR (Androgen receptor) • CD276 (CD276 Molecule)
    |
    Focus V (anlotinib) • dordaviprone (ONC201)
    6d
    Effects of AKT Inhibitors for PIK3CA/AKT1/PTEN-Altered Advanced or Metastatic Breast Cancer: A Meta-Analysis of Randomized Clinical Trials. (PubMed, Clin Breast Cancer)
    Our findings suggest that the incorporation of AKT inhibitors holds promise for treating patients with advanced or metastatic PIK3CA/AKT1/PTEN-altered BC.
    Clinical • Retrospective data • Review • Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
    6d
    2β-methoxy-2-deethoxyphantomolin synergistically enhances epirubicin effect against triple-negative breast cancer via targeted inhibition of AKT and HR pathways. (PubMed, Bioorg Chem)
    The results of MDA-MB-231 xenograft tumor model confirmed that EM2 could reduce the dose of Epi and achieve anti-TNBC effect in vivo without toxicity to mice tissues. Overall, our work indicates EM2 in combination with Epi can greatly expand the therapeutic effect of Epi in TNBC, underscoring targeting AKT and RAD51 as a promising approach for TNBC chemotherapy sensitization.
    Journal
    |
    RAD51 (RAD51 Homolog A)
    |
    epirubicin
    9d
    Gene expression profiling and pathway analysis in head and neck squamous cell carcinoma: focus on disulfidptosis. (PubMed, Discov Oncol)
    DRGscore effectively predicted survival (P < 0.001), immunotherapy response (anti-PD1/PD-L1 cohorts: P = 0.0099-0.018), and drug sensitivity (A443654 IC50 = 0.12 μM vs. AICAR = 8.3 μM). Mutational profiling identified TP53 and MUC16 as high-risk biomarkers. These findings establish DRGscore as a robust prognostic tool integrating disulfidptosis biology and immune contexture, enabling risk-stratified therapeutic strategies for HNSCC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    TP53 (Tumor protein P53) • MUC16 (Mucin 16, Cell Surface Associated) • RAC1 (Rac Family Small GTPase 1) • SLC7A11 (Solute Carrier Family 7 Member 11)
    |
    TP53 mutation
    |
    A 443654
    9d
    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 | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    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)
    11d
    Mechanism of allosteric activation in human mitochondrial ClpP protease. (PubMed, Proc Natl Acad Sci U S A)
    Conversely, hyperactivating ClpP with small-molecule activators, such as the recently discovered ONC201, disrupts mitochondrial protein degradation and impairs respiration in cancer cells...We elucidate the ClpP activation mechanism, highlighting a hormetic effect where substoichiometric inhibitor binding triggers an allosteric transition that drives ClpP into its active extended state. Our findings link the conformational dynamics of ClpP to its catalytic function and provide high-resolution structures for the rational design of potent and specific ClpP inhibitors, with implications for targeting AML and other disorders with ClpP involvement.
    Journal
    |
    CLPP (Caseinolytic Mitochondrial Matrix Peptidase Proteolytic Subunit)
    |
    dordaviprone (ONC201)
    12d
    KiBS: A Study of Zidovudine/Lamivudine and Either Nevirapine or Nelfinavir for Reduction of Mother-to-child HIV Transmission During Breastfeeding (clinicaltrials.gov)
    P2, N=520, Completed, Centers for Disease Control and Prevention | Unknown status --> Completed
    Trial completion
    |
    CD4 (CD4 Molecule)
    |
    Viracept (nelfinavir)
    12d
    CAPIVASERTIB REGULATORY POSTMARKETING SURVEILLANCE IN KOREA (clinicaltrials.gov)
    P=N/A, N=130, Not yet recruiting, AstraZeneca
    New trial
    |
    Truqap (capivasertib)
    12d
    F-box/WD Repeat-Containing Protein 5 Promotes Breast Cancer Progression by Regulating Ferroptosis via Enhancing Krüppel-like Factor 13 Ubiquitination Through Phosphoinositide 3-Kinase/Serine/Threonine Protein Kinase Pathway. (PubMed, Rejuvenation Res)
    KLF13 silencing counteracted the inhibitory effects of FBXW5 depletion on cell proliferation, migration, and invasion, as well as its promotion of ferroptosis, effects that were reversed by LY294002. In conclusion, targeting FBXW5 may serve as a potential therapeutic strategy for BC by modulating the KLF13/PI3K/AKT axis.
    Journal • BRCA Biomarker
    |
    BRCA (Breast cancer early onset) • WDR5 (WD Repeat Domain 5)
    |
    LY294002
    12d
    Investigation of mitochondrial DNA methylation-related prognostic biomarkers in hepatocellular carcinoma using The Cancer Genome Atlas (TCGA) database. (PubMed, Transl Cancer Res)
    The chemotherapeutic drug sensitivity analysis revealed significant differences in sensitivity to BI.2536 [a Polo-like kinase 1 (Plk1) inhibitor], A.443654 [a protein kinase B (Akt) 1/2 inhibitor], and ABT.888 [Veliparib, a poly(ADP-ribose) polymerase 1/2 (PARP1/2) inhibitor] between the high- and low-risk groups. It also elucidated the pathogenesis of MTDM-associated HCC. Our findings provide novel insights that could lead to the development of future therapeutic strategies.
    Journal • PARP Biomarker
    |
    CD8 (cluster of differentiation 8) • PLK1 (Polo Like Kinase 1) • ADH4 (Alcohol Dehydrogenase 4 (Class II), Pi Polypeptide) • DNASE1L3 (Deoxyribonuclease 1 Like 3)
    |
    veliparib (ABT-888) • BI2536 • A 443654
    14d
    Loss of LATS1 and LATS2 promotes ovarian tumor formation by enhancing AKT activity and PD-L1 expression. (PubMed, Oncogene)
    The stimulatory effect of Lats1/2 knockout on cell proliferation can be partially reversed by treatment with the AKT inhibitor MK2206. Treatment with verteporfin, a potent inhibitor of YAP/TAZ, decreases ovarian tumor progression and reduces the activated AKT in the tumors. In summary, this study uncovers several biological mechanisms for the initiation of HGSOC and identifies LATS1/2 as potential prognostic indicators and therapeutic targets.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • LATS1 (Large Tumor Suppressor Kinase 1) • LATS2 (Large Tumor Suppressor Kinase 2)
    |
    PD-L1 expression
    |
    MK-2206 • Visudyne (verteporfin)
    15d
    Chelidonine inhibits melanoma cell malignancy by inactivating TLR4/NF-κB and PI3K/AKT signaling pathways. (PubMed, Korean J Physiol Pharmacol)
    Furthermore, TAK-242 or LY294002 further enhanced the inhibitory effects chelidonine of on malignant cell behavior. In conclusion, our findings demonstrate that chelidonine effectively suppresses the malignancy of melanoma cells through the inhibition of TLR4/NF-κB and PI3K/AKT signaling pathways, suggesting its potential as a promising therapeutic agent for melanoma treatment.
    Journal
    |
    TLR4 (Toll Like Receptor 4)
    |
    LY294002
    15d
    NCI-2021-13902: Testing the Addition of an Anti-cancer Drug, Ipatasertib, to the Usual Immunotherapy Treatment (Pembrolizumab) in Patients With Recurrent or Metastatic Squamous Cell Cancer of the Head and Neck (clinicaltrials.gov)
    P2, N=52, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • ipatasertib (RG7440)
    16d
    ONC201 exerts oncogenic effects beyond its mitochondria-disturbing role in neuroblastoma subsets. (PubMed, J Mol Med (Berl))
    Rho zero (ρ0)-SK-N-AS cells treated with ONC201 showed comparable observed trends in parental SK-N-AS cells, including LGR5 upregulation and ATRX downregulation, suggesting that ONC201's multifaceted actions extend beyond mitochondrial targets. Our elucidation highlights the need to discern molecular signatures when deploying ONC201 monotherapy against NB, which lacks MYCN-amplification.
    Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • ATRX (ATRX Chromatin Remodeler) • LGR5 (Leucine Rich Repeat Containing G Protein-Coupled Receptor 5)
    |
    dordaviprone (ONC201)
    16d
    Identification of Active Phytochemicals to Inhibit Signal Transducer and Activator of Transcription 5A (STAT5A) Dimerization for Prostate Cancer Therapy: An In Silico Approach. (PubMed, Anticancer Agents Med Chem)
    Pedunculagin demonstrated the strongest binding energy and stability, making it a promising candidate for further development as a novel lead compound to disrupt STAT5a/b dimerization in PCa therapy.
    Journal
    |
    STAT5A (Signal Transducer And Activator Of Transcription 5A)
    |
    oleandrin (PBI-05204)
    19d
    EAY131-Y: Testing AZD5363 as a Potential Targeted Treatment in Cancers With AKT Genetic Changes (MATCH-Subprotocol Y) (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Mar 2025 --> Mar 2026
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor)
    |
    HR positive • HER-2 negative
    |
    Truqap (capivasertib)
    24d
    Chidamide-REAC in autologous stem cell transplantation of high-risk or relapsed/refractory B-cell lymphoma (ChiCTR2500098425)
    P=N/A, N=30, Recruiting, Dongguan Kanghua Hospital; Dongguan Kanghua Hospital
    New trial
    |
    Rituxan (rituximab) • cytarabine • cyclophosphamide • etoposide IV • Epidaza (chidamide)
    24d
    A single arm multicenter clinical study of Zanubrutinib combined with Chidamide and Rituximab for first-line treatment of elderly patients with double expression diffuse large B-cell lymphoma (ChiCTR2500098804)
    P2, N=50, Recruiting, Fujian Medical University Union Hospital; Fujian Medical University Union Hospital
    New P2 trial
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2) • CD20 (Membrane Spanning 4-Domains A1) • BCL6 (B-cell CLL/lymphoma 6)
    |
    CD20 positive • MYC rearrangement + BCL6 rearrangement
    |
    Rituxan (rituximab) • Brukinsa (zanubrutinib) • Epidaza (chidamide)
    24d
    Cadonilimab in Combination with Chemotherapy and Chidamide as First-Line Treatment of Advanced Gastric Cancer (ChiCTR2500096832)
    P2, N=42, Not yet recruiting, The First Affiliated Hospital of Soochow University; The First Affiliated Hospital of Soochow University
    New P2 trial
    |
    capecitabine • albumin-bound paclitaxel • oxaliplatin • Epidaza (chidamide) • Kaitanni (cadonilimab)
    24d
    Phase II Clinical Study of the Efficacy and Safety of Chidamide and Anlotinib in Combination with AG Regimen in Patients with Advanced or Recurrent Pancreatic Cancer (ChiCTR2500095869)
    P2, N=223, Not yet recruiting, The Affiliated Hospital of Qingdao University; the Affiliated Hospital of Qingdao University
    New P2 trial
    |
    Focus V (anlotinib) • Epidaza (chidamide)
    24d
    Capivasertib Plus Fulvestrant vs. Fulvestrant in Primary High-risk Lobular Breast Cancer (clinicaltrials.gov)
    P2, N=120, Recruiting, GBG Forschungs GmbH | Not yet recruiting --> Recruiting
    Enrollment open
    |
    fulvestrant • Truqap (capivasertib)
    25d
    Silencing CACYBP suppresses lung adenocarcinoma growth via CDK1 inhibition. (PubMed, Biomol Biomed)
    Additionally, the phosphoinositide 3-kinase (PI3K) inhibitor LY294002 was used to investigate the involvement of CDK1 in the PI3K/AKT pathway...In conclusion, CACYBP appears to function as a tumor promoter in LUAD, at least in part through CDK1-mediated activation of the PI3K/AKT pathway. These findings suggest that CACYBP could serve as a promising therapeutic target and a novel biomarker for LUAD prognosis.
    Journal
    |
    CDK1 (Cyclin-dependent kinase 1) • S100A6 (S100 calcium binding protein A6)
    |
    LY294002
    29d
    FINER: Fulvestrant and Ipatasertib for Advanced HER-2 Negative and Estrogen Receptor Positive (ER+) Breast Cancer Following Progression on First Line CDK 4/6 Inhibitor and Aromatase Inhibitor (clinicaltrials.gov)
    P3, N=250, Active, not recruiting, Canadian Cancer Trials Group | Trial primary completion date: Dec 2024 --> Jun 2025
    Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • HER-2 negative + ER positive
    |
    fulvestrant • ipatasertib (RG7440)
    29d
    Comprehensive Molecular and Genomic Analysis of NCI-MATCH Subprotocol Y: Capivasertib in Patients With an AKT1 E17K-Mutated Tumor. (PubMed, JCO Precis Oncol)
    In patients with AKT1 E17K-mutated tumors, capivasertib achieved a clinically significant ORR. TP53 mutations appear to be associated with response, whereas certain additional PI3K/AKT/mTOR pathway mutations and EGFR overexpression appear to be associated with nonresponse to capivasertib. Further investigation of predictive biomarkers is warranted.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • TP53 (Tumor protein P53) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
    |
    TP53 mutation • EGFR mutation • EGFR expression
    |
    Truqap (capivasertib)
    29d
    Somatic uniparental disomy of PTEN in endothelial cells causes vascular malformations in patients with PTEN Hamartoma Tumor Syndrome. (PubMed, Cancer Discov)
    We established a mouse model of PHTS-related vascular malformations and identified that the mTOR inhibitor rapamycin and AKT inhibitor capivasertib block vascular lesion growth. As proof-of-concept for clinical activity, off-label treatment with rapamycin of two patients with PHTS reduced vascular overgrowth and abrogated lesion-associated pain. Overall, our results uncover the genetic cause of vascular malformations in patients with PHTS and open new avenues for therapeutic intervention.
    Journal
    |
    PTEN (Phosphatase and tensin homolog)
    |
    PTEN mutation
    |
    Truqap (capivasertib) • sirolimus
    1m
    PI3Kδ Inhibitor Parsaclisib Combined with Chidamide for the Treatment of Relapsed/Refractory Peripheral T-cell Lymphoma (clinicaltrials.gov)
    P1/2, N=12, Terminated, Henan Cancer Hospital | N=28 --> 12 | Trial completion date: Jan 2027 --> Feb 2025 | Recruiting --> Terminated; The clinical development of parsaclisib was stopped by it's manufacturer.
    Enrollment change • Trial completion date • Trial termination
    |
    ALK (Anaplastic lymphoma kinase)
    |
    ALK positive • ALK negative
    |
    Epidaza (chidamide) • parsaclisib (INCB50465)
    1m
    Targeting the AKT/mTOR pathway attenuates the metastatic potential of colorectal carcinoma circulating tumor cells in a murine xenotransplantation model. (PubMed, Mol Oncol)
    The efficacy of the AKT inhibitor MK2206, the mTOR inhibitor RAD001, and the combination was examined in CTC-MCC-41 cells in a murine intracardiac xenotransplantation model. AKT KDs share commonly regulated proteins and phospho-proteins, but also regulate a large number uniquely. AKT1/AKT2 double-KD cells show a strongly dysregulated replication machinery, as well as a decrease in cell cycle activity and stem-cell-associated processes, underlining the non-redundant role of AKT isoforms.
    Preclinical • Journal • Circulating tumor cells
    |
    AKT2 (V-akt murine thymoma viral oncogene homolog 2)
    |
    everolimus • MK-2206
    1m
    Zanubrutinib, Chidamide, and Rituximab Induction with or Without CHOP Versus R-CHOP in Newly Diagnosed Double-Expressor DLBCL (clinicaltrials.gov)
    P2, N=128, Not yet recruiting, Li Zhiming
    New P2 trial
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • Brukinsa (zanubrutinib) • Epidaza (chidamide)
    1m
    Chidamide Plus R-CHOP in Newly Diagnosed Double-Expressor Diffuse Large B-Cell Lymphoma With Other Molecular Subtypes (clinicaltrials.gov)
    P2, N=148, Recruiting, The First Affiliated Hospital with Nanjing Medical University
    New P2 trial
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • Epidaza (chidamide)
    1m
    Targeting PKC as a Therapeutic Strategy to Overcome Chemoresistance in TNBC by Restoring Aurora Kinase B Expression. (PubMed, J Cell Mol Med)
    By taking advantage of a library screening with various kinase inhibitors, we found that the small-molecule inhibitor enzastaurin targeting protein kinase C (PKC) could overcome resistance in TNBC cells. Moreover, the efficiency of dual treatment was largely determined by AURKB, implying that AURKB could be a potential predictive marker for stratifying patients who may benefit from the combinatorial treatment. Collectively, our study not only unravels a novel underlying mechanism for paclitaxel resistance in TNBC but also provides a new potential combinatorial therapeutic strategy in the clinic.
    Journal
    |
    AURKB (Aurora Kinase B)
    |
    paclitaxel • Kinenza (enzastaurin)
    1m
    MYBL2 promotes cell proliferation and inhibits cell apoptosis via PI3K/AKT and BCL2/BAX/Cleaved-caspase-3 signaling pathway in gastric cancer cells. (PubMed, Sci Rep)
    Additionally, the AKT inhibitor MK2206 significantly reversed the proliferation capacity of GC cells induced by MYBL2 overexpression. Therefore, these results suggest that upregulated expression of MYBL2 contributes to GC cell growth and inhibits cell apoptosis by regulating the PI3K/AKT and BCL2/BAX/Cleaved-caspase-3 signaling pathways in GC cells indicating that MYBL2 may be a new therapeutic target and prognostic marker for GC.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • CASP3 (Caspase 3) • MYBL2 (MYB Proto-Oncogene Like 2)
    |
    MK-2206
    1m
    Mogroside V enhances bone marrow mesenchymal stem cells osteogenesis under hyperglycemic conditions through upregulating miR-10b-5p and PI3K/Akt signaling. (PubMed, J Orthop Surg Res)
    MV favors BMSCs osteogenic differentiation under high-glucose conditions through the upregulation of miR-10b-5p and the activation of PI3K/Akt signaling.
    Journal
    |
    MIR10B (MicroRNA 10b)
    |
    LY294002
    1m
    Necroptotic Suppression of Lung Cancer Cell Proliferation and Migration: A Comprehensive In Vitro and In Silico Study to Determine New Molecular Targets for Pexidartinib. (PubMed, Cell Biochem Funct)
    It selectively inhibits cancer cell viability, induces necroptosis, and reduces cell migration. Its stronger binding to RIPK1 and VEGFR2 more than CSF1R.
    Preclinical • Journal
    |
    KDR (Kinase insert domain receptor) • CASP3 (Caspase 3) • RIPK1 (Receptor Interacting Serine/Threonine Kinase 1) • ANXA5 (Annexin A5)
    |
    Turalio (pexidartinib)
    1m
    Glofitamab Combination With Chidamide in Patients With Recurrent/Refractory DLBCL (clinicaltrials.gov)
    P2, N=22, Recruiting, Tianjin Medical University Cancer Institute and Hospital | Not yet recruiting --> Recruiting | Initiation date: Sep 2024 --> May 2025
    Enrollment open • Trial initiation date
    |
    Epidaza (chidamide) • Columvi (glofitamab-gxbm)
    1m
    A Study of TAS0612 in Participants With Advanced or Metastatic Solid Tumor Cancer (clinicaltrials.gov)
    P1, N=47, Terminated, Taiho Oncology, Inc. | N=100 --> 47 | Trial completion date: Jul 2027 --> Nov 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Apr 2025 --> Nov 2024; Taiho Oncology as the sponsor of study TAS0612-101, has made a strategic decision to terminate the TAS0612-101 study, taking into consideration the safety profile of TAS0612 and the absence of encouraging anti-tumor activity.
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • PTEN (Phosphatase and tensin homolog) • NF1 (Neurofibromin 1)
    |
    KRAS mutation • HR positive • KRAS G12C • HER-2 negative • KRAS G12D • KRAS G12 • HR positive + HER-2 negative
    |
    TAS0612
    1m
    Akt inhibition is effective against PTEN-deleted, chemoirradiation-resistant glioblastoma stem cells. (PubMed, Growth Factors)
    Akt X (20 µM) proved more effective at inducing in vitro GSC cytotoxicity (range: 22-73%) over 48 hours than triciribine (20 µM) (0-27%), although both agents inhibited Akt phosphorylation as detected by western blot analysis. A statistically significant correlation between PTEN loss (western blot) and the extent of Akt X-induced cytotoxicity was found (p = 0.03). Akt inhibition reduces in vitro proliferation of treatment-resistant GSC lines, especially in PTEN-deficient lines, warranting further translational investigation in glioblastoma.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • PTEN (Phosphatase and tensin homolog)
    |
    PTEN deletion • EGFR expression
    |
    triciribine phosphate (PTX-200)
    2ms
    Introducing carbon quantum dot-Capivasertib drug carrier complex for enhanced treatment of breast cancer. (PubMed, PLoS One)
    After obtaining immunocytochemistry results, flow cytometry and cell invasion tests were employed to demonstrate the high potential of the introduced drug carrier complex in reducing AKT protein expression, induction of apoptosis and prevention of cell metastasis and invasion. According to these results, the binding of N/S-doped CQD to AZD5363 increases the effectiveness of this drug, with reducing the IC50 concentration, and more specificity to cancerous cells, introducing it as a suitable candidate for the treatment of breast cancer.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    Truqap (capivasertib)
    2ms
    Regulatory dynamics of Nanog in chondrocyte dedifferentiation: role of KLF4/p53 and p38/AKT signaling. (PubMed, Funct Integr Genomics)
    Moreover, the p53 activator Nutlin-3 A accelerated Nanog degradation, while the p53 inhibitor Pifithrin-α stabilized Nanog...Inhibition of p38 and AKT with SB203580 and LY294002 reduced Nanog expression and partially restored Type II collagen levels...The injected zebrafish exhibited structural defects in craniofacial cartilage, confirming Nanog's involvement in chondrocyte differentiation. These findings suggest that Nanog induces chondrocyte dedifferentiation, and this process can be modulated via the p53/KLF4 and p38/AKT pathways.
    Journal
    |
    KLF4 (Kruppel-like factor 4) • SOX9 (SRY-Box Transcription Factor 9) • NANOG (Nanog Homeobox)
    |
    LY294002 • Nutlin-3
    2ms
    Effects of tucidinostat in adult T-cell leukemia/lymphoma in clinical practice. (PubMed, Int J Hematol)
    Between October 2021 and July 2023, 24 patients aged 41 to 88 years (median, 73.4 years) who had undergone prior therapies, including intensive chemotherapy (79.2%) and mogamulizumab immunotherapy (79.2%), received tucidinostat. Treatment-related adverse events were mainly hematologic but were managed over the course of treatment. Our findings indicate that tucidinostat provides survival benefits in patients with relapsed/refractory ATL in clinical practice and highlight key clinical factors for better outcomes.
    Journal
    |
    IL2 (Interleukin 2)
    |
    Epidaza (chidamide) • Poteligeo (mogamulizumab-kpkc)
    2ms
    Chidamide + Regorafenib in Hepatocellular Carcinoma (HCC) (clinicaltrials.gov)
    P1/2, N=7, Terminated, Great Novel Therapeutics Biotech & Medicals Corporation | N=46 --> 7 | Trial completion date: Jan 2026 --> Jan 2025 | Recruiting --> Terminated; The overall profile does not support development for Hepatocellular Carcinoma
    Enrollment change • Trial completion date • Trial termination
    |
    Stivarga (regorafenib) • Epidaza (chidamide)
    2ms
    PAKT: AZD5363 in Combination With Paclitaxel in Triple-Negative Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=71, Completed, Queen Mary University of London | Active, not recruiting --> Completed | N=140 --> 71
    Trial completion • Enrollment change
    |
    paclitaxel • Truqap (capivasertib)