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DRUG CLASS:

PI3K inhibitor

Related drugs:
24h
Identification of molecularly targeted therapy-induced immunopeptidome in diffuse midline glioma (DMG). (PubMed, Neoplasia)
MTX-241F changes the glioma immunopeptidome, unveiling H2B1K, brain-enriched, and treatment-induced immunopeptides as immunologically visible targets. These findings provide a rationale for integrating molecularly targeted therapy with immunotherapeutic approaches to enhance tumor recognition and treatment efficacy in DMG and GBM.
Journal • IO biomarker
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HLA-A (Major Histocompatibility Complex, Class I, A)
1d
Discovery and Optimization of 4-Aminopteridin-7(8H)-one Derivatives as Potent and Selective mTOR Inhibitors with Favorable Pharmacodynamic and Safety Characteristics. (PubMed, J Med Chem)
The mechanistic target of rapamycin (mTOR) is a central regulator of cell growth and a promising cancer therapeutic target...In the HGC-27 xenograft mouse model, oral administration of T133 exhibited dose-dependent efficacy comparable to clinical-stage inhibitor PF-04691502, while exhibiting significantly reduced hepatotoxicity, nephrotoxicity, and pulmonary toxicity. Moreover, assessments of T133 on cytochrome P450, hERG, and AMES indicate a favorable safety profile. These findings suggest T133 is a promising mTOR inhibitor, warranting further investigation for cancer therapy.
PK/PD data • Journal
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EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
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sirolimus • PF-04691502
5d
A Study to Evaluate the Efficacy and Safety of CYH33 in Patients With Recurrent/Persistent Ovary Clear Cell Carcinoma (clinicaltrials.gov)
P2, N=93, Active, not recruiting, Haihe Biopharma Co., Ltd. | Completed --> Active, not recruiting | Trial completion date: Jul 2024 --> Feb 2026
Enrollment closed • Trial completion date
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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risovalisib (CYH33)
7d
MICALL2 promotes angiogenesis of colorectal cancer by regulating the EGFR/PI3K/AKT/KLF5/VEGFA axis. (PubMed, Biochem Pharmacol)
Pharmacological inhibition of PI3K via LY294002 reversed MICALL2-induced angiogenesis. Therefore, MICALL2 facilitates CRC angiogenesis through the EGFR/PI3K/AKT/KLF5/VEGFA axis and may serve as a promising target for anti-angiogenic therapy.
Journal
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EGFR (Epidermal growth factor receptor)
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LY294002
8d
topMIND: A Study Evaluating Safety, PK, and Efficacy of Tafasitamab and Parsaclisib in Participants With Relapsed/Refractory Non Hodgkin Lymphoma (R/R NHL) or Chronic Lymphocytic Leukemia (CLL) (clinicaltrials.gov)
P1/2, N=54, Terminated, Incyte Corporation | Completed --> Terminated; A business decision was made to discontinue further enrollment. There were no safety concerns that contributed to this decision.
Trial termination • Pan tumor
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BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • BCL6 (B-cell CLL/lymphoma 6)
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Chr t(11;14)
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parsaclisib (INCB50465) • Monjuvi (tafasitamab-cxix)
8d
Phase 1/2 Study of HYP-2090PTSA in Patients With Advanced Solid Tumors Harboring KRAS Mutation (clinicaltrials.gov)
P1/2, N=257, Recruiting, Sichuan Huiyu Pharmaceutical Co., Ltd | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Dec 2026
Trial completion date • Trial primary completion date
8d
Overexpression of IL7R Attenuates Cerebral Ischemia-Reperfusion Injury by Inhibiting Apoptosis. (PubMed, J Integr Neurosci)
Overexpression of IL7R was shown to alleviate CIRI by suppressing apoptosis. These findings indicate IL7R as a novel target for IS treatment.
Journal • IO biomarker
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IL7R (Interleukin 7 Receptor) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • IL7 (Interleukin 7)
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LY294002
10d
Epitranscriptomic regulation of NVP-BEZ235 resistance in ccRCC via the YTHDF3-SYNM regulatory pathway. (PubMed, Genes Genomics)
Reversible resistance to NVP-BEZ235 in ccRCC is driven, at least in part, by an m6A-dependent YTHDF3-SYNM axis. Targeting YTHDF3 or SYNM may provide a rational strategy to overcome PI3K/mTOR inhibitor resistance in ccRCC.
Journal
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PTEN (Phosphatase and tensin homolog) • YTHDF3 (YTH N6-Methyladenosine RNA Binding Protein F3)
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dactolisib (RTB101)
15d
GDC-0084 in Combination With Trastuzumab for Patients With HER2-Positive Breast Cancer Brain Metastases (clinicaltrials.gov)
P2, N=17, Terminated, Dana-Farber Cancer Institute | N=47 --> 17 | Active, not recruiting --> Terminated; participants are no longer being examined or receiving intervention
Enrollment change • Trial termination
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HER-2 (Human epidermal growth factor receptor 2) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
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HER-2 positive • HER-2 overexpression • HER-2 amplification • HER-2 positive + HER-2 overexpression
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Herceptin (trastuzumab) • paxalisib (GDC-0084)
16d
Mechanisms of electroacupuncture at Foot Shaoyang meridian acupoints on inflammatory response in postmenopausal osteoporosis rats based on the PI3K/AKT signaling pathway (PubMed, Zhen Ci Yan Jiu)
EA at Foot Shaoyang meridian acupoints can alleviate inflammatory responses and bone loss in postmenopausal osteoporosis rats, and its mechanism may be related to the activation of the PI3K/AKT pathway.
Preclinical • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta) • RUNX2 (RUNX Family Transcription Factor 2)
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LY294002
17d
Downregulation of OPCML is associated with activation of AKT signaling and aggressive phenotypes in glioblastoma cells. (PubMed, Front Oncol)
Functional validation used a single OPCML small interfering RNA (siRNA) with a non-targeting siRNA control (siNC) in U87 and U251 cells with Transwell invasion, wound healing, colony formation, CCK-8 proliferation, and Western blotting for p-AKT and p-mTOR, with LY294002 rescue...Loss of OPCML aligns with proliferative programs and a GBM-specific immune pattern. These data nominate OPCML as a prognostic marker and a surface-level modulator that could be leveraged alongside RTK/PI3K axis inhibitors in GBM.
Journal
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OPCML (Opioid Binding Protein/Cell Adhesion Molecule Like)
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IDH wild-type
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LY294002
22d
GDC-0084 in Combination With Trastuzumab for Patients With HER2-Positive Breast Cancer Brain Metastases (clinicaltrials.gov)
P2, N=47, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Nov 2025 --> May 2026
Trial completion date
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HER-2 (Human epidermal growth factor receptor 2) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
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HER-2 positive • HER-2 overexpression • HER-2 amplification • HER-2 positive + HER-2 overexpression
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Herceptin (trastuzumab) • paxalisib (GDC-0084)