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DRUG CLASS:

PI3Kβ inhibitor

1d
Multi-omics profiling of ACOX3 unveils pan-cancer clinical biomarker potential. (PubMed, Comput Biol Chem)
ACOX3 represents a dual diagnostic and prognostic biomarker with broad pan-cancer relevance, exhibiting distinct immune correlates and therapeutic potential.
Journal • Pan tumor
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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AZD6482 • TGX-221
4d
Study of the Selective PI3K-Beta Inhibitor GSK2636771 in Combination With Pembrolizumab in Patients With Metastatic Melanoma and PTEN Loss (clinicaltrials.gov)
P1/2, N=27, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2027
Trial completion date • Trial primary completion date
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PTEN (Phosphatase and tensin homolog)
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Keytruda (pembrolizumab) • GSK2636771
18d
Integrative bioinformatics and machine learning approach unveils potential biomarkers linking coronary atherosclerosis and glutamine metabolism-associated gene. (PubMed, J Cardiothorac Surg)
This study successfully discovered nine GlnMgs that are associated with AS. These findings provide valuable insights into potential novel biomarkers for AS and offer prospects for monitoring disease progression.
Journal
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MIR21 (MicroRNA 21) • NOS3 (Nitric oxide synthase 3) • SIRT4 (Sirtuin 4)
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acalisib (GS-9820)
18d
STARS: Safety and Tolerability of Adjunctive TBO-309 in Reperfusion for Stroke (clinicaltrials.gov)
P2, N=80, Recruiting, The Florey Institute of Neuroscience and Mental Health | Suspended --> Recruiting
Enrollment open
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AZD6482
24d
Enrollment open
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AZD6482
1m
PDCD1 as a targetable immune checkpoint hub: therapeutic insights for ibrutinib-resistant CLL management. (PubMed, Clin Exp Med)
Using two independent datasets (GSE249956 and GSE98206), differentially expressed genes (DEGs) were identified between ibrutinib-resistant and sensitive CLL samples. In the broader context, PD-1 expression in CLL cells is linked to active proliferation and immune escape. Overall, our findings emphasize PDCD1's central role in ibrutinib resistance through immune checkpoint pathways and support the rationale for combining BTK inhibitors with immune checkpoint blockade therapies in resistant CLL cases.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-1 (Programmed cell death 1) • ITGB2 (Integrin Subunit Beta 2) • CD1C (CD1c Molecule)
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PD-L1 expression
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Imbruvica (ibrutinib) • acalisib (GS-9820)
1m
PI3K inhibitors: Efficacy in diverse cancer forms. (PubMed, Cancer Treat Res Commun)
The PI3K inhibitors GDC-0032 and INK1117 for PI3K-α and AZD8186 for PI3K-β are now being studied in clinical trials. Research on the clinical development, therapeutic utility, and structural insights of new PI3K inhibitors is the main emphasis of this review. The inhibitors have been shown promising anticancer activity relationships.
Review • Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • 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)
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taselisib (GDC-0032) • AZD8186 • serabelisib (MLN1117)
2ms
EAY131-N: Testing GSK2636771 as a Potential Targeted Treatment in Cancers With PTEN Genetic Changes (MATCH-Subprotocol N) (clinicaltrials.gov)
P2, N=24, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Nov 2025 --> Dec 2026
Trial completion date
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PTEN (Phosphatase and tensin homolog)
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GSK2636771
2ms
Trial completion date
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PTEN (Phosphatase and tensin homolog) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
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ER positive • HR positive • HER-2 negative • ER positive + HER-2 negative • HER-2 negative + ER positive
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docetaxel • AZD8186
2ms
EAY131-P: Testing GSK2636771 as a Potential Targeted Treatment in Cancers With PTEN Loss of Expression (MATCH-Subprotocol P) (clinicaltrials.gov)
P2, N=35, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Nov 2025 --> Dec 2026
Trial completion date
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PTEN (Phosphatase and tensin homolog)
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GSK2636771
2ms
Mendelian randomization combined with single-cell sequencing analysis revealed prognostic genes related to myeloid cell differentiation in prostate cancer and experimental verification. (PubMed, Front Immunol)
The HRG and LRG suggested notable differences in sensitivity to 86 drugs such as AZD8186...The in vitro results were consistent with the results of bioinformatics analysis, indicating that the analysis results were reliable. This study identified 5 prognostic genes and a risk model, suggesting a fresh thought on the subsequent development of PCa related drugs.
Journal
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FASN (Fatty acid synthase) • TLR3 (Toll Like Receptor 3) • RACGAP1 (Rac GTPase activating protein 1) • BMP2 (Bone Morphogenetic Protein 2)
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AZD8186
3ms
NK cell-related genes-driven novel molecular subtyping and prognostic signatures for Wilms tumor: uncovering the therapeutic potential of TGX-221 and biomarker role of HS2ST1. (PubMed, Front Oncol)
Moreover, TGX-221 represents a promising novel therapeutic candidate, while HS2ST1 serves as a potential prognostic biomarker. These findings collectively provide tools for risk stratification and targeted therapy, advancing precision oncology for WT.
Journal
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PPP3CA (Protein Phosphatase 3 Catalytic Subunit Alpha)
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TGX-221