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DRUG CLASS:

PI3K inhibitor

Related drugs:
2d
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)
4d
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
5d
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)
5d
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
5d
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
7d
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)
12d
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)
12d
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
13d
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
19d
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)
22d
RAS/MEK/PI3K pathway inhibition augments response to CD40 agonism by targeting CD11b+ Bregs thereby overcoming melanoma PD1-resistance. (PubMed, Nat Commun)
Here, we show that combined treatment with a RAS/PI3K/AKT-pathway inhibitor rigosertib (RGS), and/or a MEK1/2 inhibitor trametinib (T), plus aCD40, overcomes the ICB resistance of BRAFwtNRASwt and BRAFwtNRASmut melanoma tumors growing in C57BL/6 mice. scRNA-Seq analyses confirm CD40-associated CD11b+ Bregs across cancer types in patients. Our data demonstrate that addition of RAS/PI3K/AKT and MEK inhibitors to aCD40 resolves the issue of aCD40 induction of CD11b+PD-L1+ Bregs and provides alternative therapeutic options for ICB-resistant BRAFwtNRASwt or BRAFwtNRASmut metastatic melanoma.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • ITGAM (Integrin, alpha M) • CD40 (CD40 Molecule)
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NRAS wild-type
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Mekinist (trametinib) • Estybon (rigosertib)
25d
Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations (clinicaltrials.gov)
P2, N=7, Terminated, M.D. Anderson Cancer Center | Trial completion date: Feb 2027 --> Dec 2025 | Active, not recruiting --> Terminated; Copanlisib development was discontinued by Bayer following withdrawal of copanlisib in relapsed follicular lymphoma in November 2023.
Trial completion date • Trial termination
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • PI3K (Phosphoinositide 3-kinases)
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PIK3CA mutation • PTEN deletion
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fulvestrant • Aliqopa (copanlisib)