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DRUG CLASS:

cSRC inhibitor

Related drugs:
Associations
Trials
8ms
UHRF1-mediated epigenetic reprogramming regulates glycolysis to promote progression of B-cell acute lymphoblastic leukemia. (PubMed, Cell Death Dis)
Furthermore, we identified UM164 as a targeted inhibitor of UHRF1 that substantially inhibits P38 protein phosphorylation, downregulates HK2 expression, and reduces lactate production...In summary, our investigation revealed the molecular mechanisms of epigenetic and metabolic reprogramming in relapsed and refractory B-cell acute lymphoblastic leukemia and provides potential targeted therapeutic strategies to improve its inadequate prognosis. The schematic model showed the regulator network of UHRF1-SFRP5-WNT5A-P38 MAPK-HK2 in B-ALL.
Journal
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UHRF1 (Ubiquitin Like With PHD And Ring Finger Domains 1)
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UM-164
almost2years
Proto-oncogene cSrc-mediated RBM10 phosphorylation arbitrates anti-hypertrophy gene program in the heart and controls cardiac hypertrophy. (PubMed, Life Sci)
Our study establishes that cSrc-mediated RBM10 phosphorylation arbitrates anti-hypertrophy gene program. We also report a new functional regulation of RBM10 by phosphorylation that is poised to control heart failure.
Journal
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RBM10 (RNA Binding Motif Protein 10) • CSK (C-Terminal Src Kinase)
over2years
Progesterone and its metabolite allopregnanolone promote invasion of human glioblastoma cells through metalloproteinase‑9 and cSrc kinase. (PubMed, Oncol Lett)
These results suggest that P4 and its metabolite 3α-THP induce the invasion of glioblastoma cells by increasing MMP-9 expression through the cSrc kinase family. The results of this study provide information of interest in the context of targeted therapies against molecular pathways involved in glioblastoma invasion.
Journal
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PGR (Progesterone receptor) • MMP2 (Matrix metallopeptidase 2) • MMP9 (Matrix metallopeptidase 9) • CSK (C-Terminal Src Kinase)
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PGR expression
over2years
Comparison of the efficacy and safety of third-line treatments for advanced gastric cancer: A systematic review and network meta-analysis. (PubMed, Front Oncol)
Therapies including immunotherapy (nivolumab), chemotherapy (irinotecan, FTD/TPI), targeted therapy (apatinib), and antibody drug conjugates (ADC) have shown to increase the survival rates in patients, but few studies have compared the relative efficacy of these treatments...Apatinib (RR: 3.04; 95% CI: 1.65-5.95) and DS-8201 (RR: 2.67; 95% CI: 1.51-4.83) were more effective than nivolumab in improving DCR...Nivolumab may be the first treatment option for GEJC patients. https://www.crd.york.ac.uk/prospero, identifier CRD42022364714.
Retrospective data • Review • PD(L)-1 Biomarker • IO biomarker • Metastases
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HER-2 overexpression
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Opdivo (nivolumab) • Enhertu (fam-trastuzumab deruxtecan-nxki) • AiTan (rivoceranib) • irinotecan • Lonsurf (trifluridine/tipiracil)
almost3years
Identification of a Novel Heterogeneous Nuclear Ribonucleoprotein A2B1 (hnRNPA2B1) Ligand that Disrupts HnRNPA2B1/Nucleic Acid Interactions to Inhibit the MDMX-p53 Axis in Gastric Cancer. (PubMed, Pharmacol Res)
This work presented a novel strategy to restore p53 activity for the treatment of gastric cancers via chemically targeting hnRNPA2B1. DATA AVAILABILITY STATEMENT: The data that support the findings of this study are available from the authors upon reasonable request.
Journal
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HNRNPAB (Heterogeneous Nuclear Ribonucleoprotein A/B) • HNRNPA2B1 (Heterogeneous Nuclear Ribonucleoprotein A2/B1)
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AiTan (rivoceranib)
almost3years
Apatinib combined with camrelizumab in advanced acral melanoma patients: An open-label, single-arm phase 2 trial. (PubMed, Eur J Cancer)
Apatinib combined with camrelizumab showed manageable safety profile and reasonable anti-tumour activity in advanced acral melanoma patients as first-line therapy.
P2 data • Clinical Trial,Phase II • Journal • PD(L)-1 Biomarker • Metastases
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MUC16 (Mucin 16, Cell Surface Associated) • ALPK2 (Alpha Kinase 2) • SCUBE1 (Signal Peptide, CUB Domain And EGF Like Domain Containing 1) • VPS13D (Vacuolar Protein Sorting 13 Homolog D)
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MUC16 mutation • TTN mutation
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AiRuiKa (camrelizumab) • AiTan (rivoceranib)
almost3years
Apatinib Mesylate Versus Standard Second-line TKI in the Treatment of Advanced GIST (clinicaltrials.gov)
P=N/A, N=258, Recruiting, Xiangya Hospital of Central South University
New trial • Stroma • Metastases
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PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
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dasatinib • imatinib • sunitinib • AiTan (rivoceranib)
almost3years
Preclinical • Journal • PARP Biomarker • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2)
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BCL2 expression • KDR expression
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AiTan (rivoceranib)
almost3years
Artemis: A Prospective, Phase II Trial Using ctDNA to Initiate Post-operation Boost Therapy After Adjuvant Chemotherapy in TNBC (clinicaltrials.gov)
P2/3, N=260, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Not yet recruiting --> Recruiting
Enrollment open • Circulating tumor DNA
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HER-2 (Human epidermal growth factor receptor 2)
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AiRuiKa (camrelizumab) • AiTan (rivoceranib) • capecitabine
almost3years
In vitro and in vivo analyses on anti-NSCLC activity of apatinib: rediscovery of a new drug target V600E mutation. (PubMed, Cancer Cell Int)
BRAF V600E protein kinase is a target of apatinib by kinase screening. We have demonstrated that apatinib can effectively inhibit tumor cells with BRAF V600E mutation by in vitro and in vivo experiments. Our results have demonstrated that targeting BRAF V600E mutation, apatinib appears to be effective and safe for treating NSCLC and possibly other cancers with the same mutation.
Preclinical • Journal
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BRAF (B-raf proto-oncogene)
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BRAF V600E • BRAF V600
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AiTan (rivoceranib)
almost3years
A Study of SHR-1210 in Combination With Apatinib in Advanced Non-Small Cell Lung Cancer(NSCLC) (clinicaltrials.gov)
P2, N=210, Completed, Jiangsu HengRui Medicine Co., Ltd. | Unknown status --> Completed | N=118 --> 210 | Trial completion date: Jun 2019 --> May 2022 | Trial primary completion date: Dec 2018 --> Apr 2022
Trial completion • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
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PD-L1 (Programmed death ligand 1)
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AiRuiKa (camrelizumab) • AiTan (rivoceranib)