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DRUG:

PI-103

i
Other names: PI-103
Company:
Roche
Drug class:
mTOR inhibitor, PI3K inhibitor
Related drugs:
2ms
DSCC1 as a Novel Biomarker in Hepatocellular Carcinoma: Diagnostic Potential, Prognostic Impact, Correlation With Key Pathways, and Association With the Immune Landscape. (PubMed, J Gene Med)
Overall, this study suggests that DSCC1 may function as a valuable prognostic biomarker, an early diagnostic indicator, and a potential therapeutic target in LIHC, given its diverse involvement in tumor progression, drug responsiveness, immune regulation, and genomic instability.
Journal
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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Mekinist (trametinib) • Zolinza (vorinostat) • PI-103
6ms
Repurposing of PI3K inhibitors for high-grade serous ovarian cancer: A novel competing endogenous network analysis-based approach. (PubMed, Comput Biol Med)
Investigation of fine-tune regulation of RNA by non-coding RNAs and TFs uncovered a significant role of ceRNA network in cancer development, highlighting its integration with master regulatory pathways that drive tumor progression and sustainability. The drug repurposing workflow based on ceRNA-limited differentially expressed mRNAs allowed for effective prioritization of compounds with potential to be applied as treatment.
Journal
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SNAI2 (Snail Family Transcriptional Repressor 2) • E2F1 (E2F transcription factor 1)
|
PI-103 • OP-11
6ms
Identification of AKTIP as a biomarker for fibrolamellar carcinoma using WGCNA and machine learning. (PubMed, 3 Biotech)
Four compounds (PI-103, BVT-948, Digitoxigenin, and SB-218078) were identified as potential therapeutic agents targeting AKTIP...This study uncovers new perspectives on diagnosing and managing of this rare type of liver carcinoma, offering promising avenues for future research and clinical applications. The online version contains supplementary material available at 10.1007/s13205-025-04323-4.
Journal
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AKTIP (AKT Interacting Protein)
|
PI-103
9ms
STAG2 expression imparts distinct therapeutic vulnerabilities in muscle-invasive bladder cancer cells. (PubMed, Oncogenesis)
We identified 100 total drug hits and found that STAG2 KO sensitized cells to treatment with PLK1 inhibitor rigosertib, whereas STAG2 KO protected cells from treatment with MEK inhibitor TAK-733 and PI3K inhibitor PI-103. Finally, synergy experiments revealed that berzosertib exhibits significant synergistic cytotoxicity in combination with cisplatin against MIBC cells. Altogether, our study presents evidence that berzosertib, PI-103, and the combination of berzosertib with cisplatin may be novel opportunities to investigate as precision medicine approaches for MIBC patients based on STAG2 tumor expression.
Journal
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STAG2 (Stromal Antigen 2)
|
cisplatin • berzosertib (M6620) • Estybon (rigosertib) • REC-4881 • PI-103
9ms
LncRNA HITT inhibits autophagy by attenuating ATG12-ATG5-ATG16L1 complex formation. (PubMed, Cancer Lett)
This results in HITT sensitizing PI-103-mediated cell death both in vitro and in vivo in nude mice by attenuating protective autophagy. The data presented herein demonstrate that HITT is a newly identified RNA regulator of autophagy and that it can be used to sensitize the colon cancer response to cell death by blocking the protective autophagy.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • ATG5 (Autophagy Related 5) • ATG12 (Autophagy Related 12) • ATG16L1 (Autophagy Related 16 Like 1) • MIR205 (MicroRNA 205)
|
PI-103
9ms
The comprehensive potential of AQP1 as a tumor biomarker: evidence from kidney neoplasm cohorts, cell experiments and pan-cancer analysis. (PubMed, Hum Genomics)
Our study uncovered AQP1 as a biomarker for favorable survival outcomes in renal cancers. Furthermore, the bioinformatic analysis promoted its implication in pan-cancer scope.
Journal • Pan tumor
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AQP1 (Aquaporin 1)
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PI-103
1year
Identification of Cuproptosis-Related Genes for Molecular Subtyping: Predicting Prognostic and Therapeutic Response in Glioma. (PubMed, Onco Targets Ther)
We screened PI-103 as the most promising candidate for patients with higher CupScore and confirmed its experimental evidence and clinical trial status...Cuproptosis has the ability to reprogram the tumor microenvironment (TME) in HGG, leading to the stratification of patients into two distinct molecular subgroups. The CupScore model emerged as a robust metric for predicting the prognostic and therapeutic benefits, as well as may therefore facilitate personalized treatment strategies for patients with HGG.
Journal • PD(L)-1 Biomarker • IO biomarker
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CDKN2A (Cyclin Dependent Kinase Inhibitor 2A)
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PI-103
almost2years
Molecular Expression and Prognostic Implications of Krüppel-Like Factor 3 (KLF3) in Clear Cell Renal Cell Carcinoma. (PubMed, Crit Rev Eukaryot Gene Expr)
Based on GDSC database, KLF3 upregulation was identified to be associated with higher sensitivities towards PI3K-Akt-mTOR pathway inhibitors such as PI-103, PIK-93, and OSI-027. In addition, patients with down-regulated KLF3 expressions were found more sensitive towards Trametinib, Cetuximab, and Erlotinib. Collectively, our findings suggest that KLF3 may act as a suitable biomarker for prognosis prediction, tumor microenvironment (TME) phenotype identification, thereby helping ccRCC patients to make better therapeutic decisions.
Journal
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TGFB1 (Transforming Growth Factor Beta 1)
|
Erbitux (cetuximab) • Mekinist (trametinib) • erlotinib • AVTX-006 • PI-103
over2years
Suppression of Autophagy Can Augment PIK3 Inhibitor Induced Apoptosis in T Lymphoblastic Leukemia Cell Lines. (PubMed, Ann Clin Lab Sci)
The results demonstrated that 3-MA could suppress PI3K inhibitor-mediated activation of autophagy to promote the apoptosis of tumor cells. This discovery provided experimental support for constituting a promising strategy for T-cell acute lymphoblastic leukemia (T-ALL) therapy.
Preclinical • Journal
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ATG5 (Autophagy Related 5) • ATG12 (Autophagy Related 12) • BECN1 (Beclin 1)
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ATG5 expression
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PI-103 • sonolisib (PX 866)
over2years
Overcoming roadblocks of immunotherapy in non-small cell lung cancer (AACR 2023)
Here, we introduce antibody conjugated drug loaded nanotherapeutics (ADNs) consisting of a targeted therapy drug, phosphatidylinositol 3-kinase (PI3K) inhibitor PI103, and decorated with two ICIs for CD47 and PDL1...Reduced tumor growth and higher survival probability have been observed in the syngeneic LLC tumor model for anti-CD47-PDL1-ADN than monotherapy and traditional immunotherapy.In summary, we have introduced a lung cancer treatment strategy that can be an effective therapy for NSCLC patients, irrespective of the PDL1 expression level. The strategy combining bispecific immunotherapy and targeted therapy for activating the innate and adaptive immune systems and delivering targeted therapy drugs can emerge as a significant advance in the treatment of NSCLC patients.
PD(L)-1 Biomarker • IO biomarker
|
CD47 (CD47 Molecule) • SIRPA (Signal Regulatory Protein Alpha)
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PD-L1 overexpression • CD47 overexpression • CD47 expression
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PI-103
almost3years
Enhancement of the antitumor effect of 5-fluorouracil with modulation in drug transporters expression using PI3K inhibitors in colorectal cancer cells. (PubMed, Life Sci)
Our data provide evidence that survival signaling pathways represent distinctive targets for the enhancement of chemotherapeutic sensitivity. The antitumor efficacy of 5-FU is enhanced when combined with a PI3K inhibitor, and this effect was mediated by alterations in the expression of specific drug transporters.
Journal
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ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC5 (ATP Binding Cassette Subfamily C Member 5)
|
ABCG2 expression
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5-fluorouracil • LY294002 • PI-103
3years
An autophagy-related gene prognostic index predicting biochemical recurrence, metastasis, and drug resistance for prostate cancer. (PubMed, Asian J Androl)
Drug analysis showed that PI-103 was the common sensitive drug and cell line analysis indicated that PC3 was the common cell line of PI-103 and the definitive gene. In conclusion, we found that ARGPI could predict BCR, metastasis, and chemoresistance in PCa patients who underwent radical radiotherapy or prostatectomy.
Journal
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SPP1 (Secreted Phosphoprotein 1) • ALDH2 (Aldehyde Dehydrogenase 2 Family Member) • ACSL3 (Acyl-CoA Synthetase Long Chain Family Member 3)
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PI-103