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DRUG:

foretinib (GSK1363089)

i
Other names: GSK1363089, XL880, EXEL-2880, GSK089
Company:
Exelixis
Drug class:
c-MET inhibitor, VEGFR-2 inhibitor
Related drugs:
10d
Unveiling disulfidptosis-linked lncRNA signatures: insights into the immune microenvironment and drug responsiveness in oral squamous cell carcinoma. (PubMed, Front Genet)
12 drugs were identified for OSCC treatment, such as BMS-754807_2171 and Foretinib_2040. Our study identified 9 DE-DRLs correlated with OSCC, which will be a personalized prediction tool for prognosis and immune responses in OSCC patients.
Journal • Tumor mutational burden
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TMB (Tumor Mutational Burden) • CD4 (CD4 Molecule)
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TMB-H
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BMS-754807 • foretinib (GSK1363089)
6ms
Exploring the role of circRNA-miRNA-mRNA interactions in cervical cancer progression: insights into HPV status and potential therapeutic approaches. (PubMed, J Appl Genet)
The study utilized CMAP2 and CTDBASE, identifying foretinib, TPCA-1, and dequalinium as promising drugs targeting key hub genes. Although limitations include a small sample size and ethnic heterogeneity in in vitro validation, this study advances our understanding of circRNA mechanisms in cervical cancer and identifies novel biomarkers and therapeutic targets.
Journal
|
KIF4A (Kinesin Family Member 4A)
|
foretinib (GSK1363089)
6ms
Responsiveness of different MET tumour alterations to type I and type II MET inhibitors. (PubMed, Clin Transl Med)
Kinase mutations in RTKs are primary or secondary drivers in multiple cancer types Some of these mutations confer resistance to type I but not to type II inhibitors in preclinical samples and in patients The biochemical characterization of mutations in oncogenic kinases based on their sensitivity to type I and type II inhibitors is crucial to inform clinical intervention.
Journal
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET mutation
|
Cabometyx (cabozantinib tablet) • foretinib (GSK1363089)
12ms
Establishment and characterization of NCC-GCTB10-C1: a novel cell line derived from a patient with recurrent giant cell tumor of bone. (PubMed, Hum Cell)
However, doxorubicin, foretinib, and ceritinib were identified as promising therapeutic candidates due to their low IC50 values in NCC-GCTB10-C1. The establishment of NCC-GCTB10-C1 offers a critical resource for further research into GCTB, especially in the context of recurrent disease, and holds potential for the development of more effective treatment strategies.
Preclinical • Journal
|
H3-3A (H3.3 Histone A)
|
doxorubicin hydrochloride • Zykadia (ceritinib) • foretinib (GSK1363089)
1year
CDH2 and CDH13 as potential prognostic and therapeutic targets for adrenocortical carcinoma. (PubMed, Cancer Biol Ther)
Foretinib and elesclomol were predicted to exert strong inhibitory effects on SW13 cells by inhibiting the expression of CDH2 and CDH13. These data indicate that CDH2 and CDH13 are promising targets for precise treatment of ACC and may serve as new biomarkers for ACC prognosis.
Journal • PD(L)-1 Biomarker • IO biomarker
|
CDH2 (Cadherin 2)
|
CDH1 expression
|
elesclomol (STA-4783) • foretinib (GSK1363089)
1year
TNFSF12 is associated with breast cancer prognosis and immune cell infiltration. (PubMed, Am J Transl Res)
This study presents a comprehensive analysis of the close correlation between TNFSF12 and prognosis, immune response, as well as the effectiveness of chemotherapeutic agents in BRCA patients.
Journal • BRCA Biomarker • IO biomarker • Immune cell
|
HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • CD8 (cluster of differentiation 8) • TNFA (Tumor Necrosis Factor-Alpha) • BRCA (Breast cancer early onset)
|
HER-2 positive • MYC expression
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Prosigna™ Breast Cancer Prognostic Gene Signature Assay
|
erlotinib • paclitaxel • sirolimus • foretinib (GSK1363089)
over1year
Design, synthesis, and antiproliferative activity of new indole/1,2,4-triazole/chalcone hybrids as EGFR and/or c-MET inhibitors. (PubMed, Arch Pharm (Weinheim))
Compound 9b showed the highest c-MET inhibition (IC50 = 4.70 nM) compared to foretinib (IC50 = 2.5 nM). Compound 9d showed equipotent activity compared with erlotinib against EGFR (IC50 = 0.052 µM) and displayed significant c-MET inhibition with an IC50 value of 4.90 nM.
Journal
|
EGFR (Epidermal growth factor receptor)
|
erlotinib • foretinib (GSK1363089)
over1year
Integrated analysis of ferroptosis and stemness based on single-cell and bulk RNA-sequencing data provide insights into the prognosis and treatment of esophageal carcinoma. (PubMed, Gene)
This study constructed a novel ferroptosis-related stemness signature, identified two marker genes for ESCA, and provided valuable insights for developing more effective therapeutic targets targeting ESCA CSCs in the future.
Journal • PARP Biomarker
|
SLC2A1 (Solute Carrier Family 2 Member 1) • STMN1 (Stathmin 1)
|
Talzenna (talazoparib) • Inlyta (axitinib) • navitoclax (ABT 263) • foretinib (GSK1363089)
over1year
The HGF/Met Receptor Mediates Cytotoxic Effect of Bacterial Cyclodipeptides in Human Cervical Cancer Cells. (PubMed, Curr Cancer Drug Targets)
Data provide new insights into the molecular mechanisms involved in CDPs cytotoxicity and antiproliferative effects, suggesting that the signal transduction mechanism may be related to the inhibition of the phosphorylation of the EGF/MET receptor at the level of substrate binding site by an inhibition mechanism similar to that of Gefitinib and foretinib anti-neoplastic drugs.
Journal
|
EGF (Epidermal growth factor)
|
gefitinib • foretinib (GSK1363089)
over1year
Design, synthesis, and biological evaluation of new biaryl derivatives of cycloalkyl diacetamide bearing chalcone moiety as type II c-MET kinase inhibitors. (PubMed, Mol Divers)
Herein, we report the discovery of a novel structure of potent chalcone-based derivatives type II c-Met inhibitors which are comparable to Foretinib (IC50 = 14 nM) as a potent reference drug...However, the weak inhibitory effects on microtubules were confirmed by cell cycle analyses implicated that the observed cytotoxicity against HeLa cells probably was not derived from tubulin inhibition. Compounds 14q and 14k with IC50 values of 24 nM and 45 nM, respectively, demonstrated favorable inhibition of MET kinase activity, and desirable bonding interactions in the ligand-MET enzyme complex stability in molecular docking studies.
Journal
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
foretinib (GSK1363089)
almost2years
Foretinib, a c-MET receptor tyrosine kinase inhibitor, tackles multidrug resistance in cancer cells by inhibiting ABCB1 and ABCG2 transporters. (PubMed, Toxicol Appl Pharmacol)
Overall, our results suggest that foretinib can target MDR-linked ABCB1 and ABCG2 transporters in clinical cancer therapy.
Journal
|
MET (MET proto-oncogene, receptor tyrosine kinase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
|
ABCB1 overexpression • ABCB1 expression • ABCG2 expression
|
doxorubicin hydrochloride • mitoxantrone • foretinib (GSK1363089)
almost2years
Foretinib is effective in acute myeloid leukemia by inhibiting FLT3 and overcoming secondary mutations that drive resistance to quizartinib and gilteritinib. (PubMed, Cancer Res)
Moreover, foretinib showed potent activity against secondary mutations of FLT3-ITD that confer resistance to quizartinib and gilteritinib. These findings support the potential of foretinib for treating AML patients with FLT3-ITD mutations, especially for those carrying secondary mutations after treatment failure with other FLT3 inhibitors.
Journal
|
FLT3 (Fms-related tyrosine kinase 3)
|
FLT3-ITD mutation • FLT3 mutation
|
Xospata (gilteritinib) • Vanflyta (quizartinib) • foretinib (GSK1363089)