foretinib (GSK1363089) / Exelixis - LARVOL DELTA

Potential c-Met-targeted pyrazole-pyridine-oxadiazole hybrids: synthesis, anticancer activity, and computational rationale. (PubMed, Org Biomol Chem) - "Derivatives were screened for anticancer activity against A549 (lung) and MCF-7 (breast) cell lines using Foretinib as reference...DFT calculations (B3LYP/6-311++G(d,p)) for 10c, 10d, and 10h confirmed that 10d has the smallest HOMO-LUMO gap (3.74 eV) and highest chemical softness, consistent with its superior activity. Collectively, these findings identify 10d as a promising scaffold for further optimization and biological evaluation."

Journal • Oncology • MET

Foretinib triggers immunogenic cell death and enhances efficacy of anti-CD47 immunotherapy in colorectal cancer. (PubMed, Neoplasia) - "Moreover, combined treatment with foretinib and anti-CD47 antibody exerts synergistic antitumor effects. Together, these findings uncover a previously unreported immunomodulatory function of c-Met/VEGFR2 inhibition, demonstrating that foretinib elicits potent anti-CRC efficacy via direct cytotoxicity and immunogenic regulation, and highlighting its considerable clinical therapeutic potential."

Journal • Colorectal Cancer • Oncology • Solid Tumor • CALR • HMGB1 • MET • TNFRSF10B

Zongertinib-tolerant cells enhanced sensitivity to Topo1 inhibition in Her2-positive NCSLC (AACR 2026) - "For the treatment of Her2 mutated/amplified NSCLC, the antibody-drug conjugate Trastuzumab deruxtecan, several Her2-selective inhibitors, such as zongertinib and sevabertinib, have shown beneficial efficacy in clinical settings...Drug screening revealed that zongerR cells exhibited sensitivity to the multi-tyrosine kinase inhibitor ponatinib and foretinib. Additionally, PI3K/AKT pathway inhibitors (PI3Ki) such as GDC0941 and mTOR inhibitor PP242 also markedly suppressed the survival of zongerR cells in combination with zongertinib...Currently, zongertinib and T-Dxd have been approved for Her2-positive NSCLC, whereas treatment strategies to prolong the durable response have not been well-established. Further investigations were needed, but our findings suggested that T-DXd treatment after zongertinib may be a potential therapeutic strategy in a subset of Her2-positive NSCLC."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Tumor endothelial cell lines and their use for the identification of new tumor vascular targets during dysbiosis (AACR 2025) - "Moreover, c-Met inhibitors Foretinib, Crizotinib, and Cabozantinib were significantly more effective against TEC-Dys than TEC-Ortho...Thus, we surmise that tumor response in dysbiotic patients may be greatly improved by targeting dysbiosis-induced pathways, such as c-Met, as compared to the targets suppressed due to dysbiosis. These matched tumor endothelial cell lines generated under orthobiotic and dysbiotic conditions can now be used in in vitro and in vivo cell-based models, and provide an improved and specialized platform for current and next-generation anti-cancer drug discovery and development."

Dysbiosis • Preclinical • Oncology

Repurposing non-oncology drugs with MET inhibitory effect to overcome osimertinib resistance in lung cancer (AACR 2024) - "This study investigated the repurposing of non-oncology MET inhibiting drug to overcome osimertinib resistance. A few clinically-approved drugs with putative MET inhibitory effects were identified by a computational drug repurposing tool called "DRAR-CPI" via analysis of the chemical-protein interactome of known MET inhibitors (crizotinib, cabozantinib, foretinib, and tivantinib)... These findings advocate the clinical evaluation of repurposing FEX to overcome osimertinib resistance."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Lactylation-related genes signature panel in hepatocellular carcinoma reveals the prognostic and therapeutic optimization. (PubMed, Mol Cell Oncol) - "Conversely, the high-LRGS group demonstrated heightened sensitivity to several antitumor agents, including AZD5153, cediranib, foretinib, and vorinostat, relative to the low-LRGS group. Our findings establish a robust LRGS model, offering a clinically actionable tool for prognostic assessment and precision therapy in HCC."

IO biomarker • Journal • Hepatocellular Cancer • Oncology • Solid Tumor

Foretinib Alleviates Osteoblast Senescence and Protects Against Bone Loss in Ovariectomized Mice by Promoting Osteoblast Differentiation. (PubMed, Cells) - "Foretinib inhibited doxorubicin-induced senescence in osteoblast progenitors via the p53/p21 and p16 pathways and reduced the expression of osteogenesis-inhibiting SASP factors, including CCL2, interleukin (IL)-1α, IL-1β, and IL-6. In ovariectomized, estrogen-deficient mice, foretinib significantly reduced trabecular and cortical bone loss by enhancing in vivo osteoblast differentiation, as shown by histological analysis and micro-computed tomography of femoral bone. These results suggest that foretinib alleviates osteoblast senescence and enhances osteogenic differentiation, supporting its promise as a therapeutic candidate for postmenopausal osteoporosis."

Journal • Preclinical • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology • CCL2 • CDKN1A • IL1B • IL6

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 • Oncology • Oral Cancer • Squamous Cell Carcinoma • CD4 • TMB

Kaempferols from Echinacea purpurea demonstrate anti-cancer potential by targeting anexelekto in breast cancer therapy using chemoinformatics approach. (PubMed, Discov Oncol) - "In silico studies show that E. purpurea-derived compounds, especially Kaempferol 3-o-beta-d-glucopyranosyl-7-o-alpha-L-rhamnopyranoside, have better inhibitory potential against AXL and better pharmacokinetic profiles when compared with Foretinib. These compounds are thus proposed as novel AXL inhibitors for the treatment of breast cancer. Further, in vivo studies are needed to confirm the potency of the studied compounds."

Journal • Breast Cancer • Oncology • Solid Tumor

Dual inhibitors of P-glycoprotein and breast cancer resistance protein for overcoming the blood-brain barrier: in silico discovery and preclinical evaluation. (PubMed, Arch Pharm Res) - "This study sought potential dual P-gp/BCRP inhibitors to determine their ability to enhance brain penetration of the anticancer drug mitoxantrone (MX) and thereby improve its therapeutic efficacy against brain cancer...The 5 compounds selected as final candidates were CDK 4/6 inhibitor IV, BX795, foretinib, BI-D1870, and CGP60474...In conclusion, potential dual P-gp/BCRP inhibitors were discovered through in silico screening and verified through in vitro and in vivo studies. CDK 4/6 inhibitor IV was the most effective dual P-gp/BCRP inhibitor candidate for enhancing the brain penetration of an anticancer drug for the treatment of brain tumors."

Journal • Preclinical • Brain Cancer • Breast Cancer • Oncology • Solid Tumor

Foretinib Inhibits Osteoblast Senescence and Bone Loss in an Ovariectomized Estrogen-deficient Mice by Promoting Osteogenic Differentiation (ASBMR 2025) - No abstract available

Preclinical • Osteoporosis

Cell-in-cell associated lncRNA signature predicts prognosis and immunotherapy response in gastric cancer. (PubMed, Front Oncol) - "Drug sensitivity analysis revealed low-risk patients responded better to gefitinib/entinostat, while high-risk patients benefited from dasatinib/foretinib. Experimental validation confirmed AP000695.2 promoted proliferation and invasion in GC cells (P <0.01). This study establishes CICRlncRNAs as prognostic biomarkers and provides insights for precision therapy, though clinical applicability requires prospective validation."

IO biomarker • Journal • Gastric Cancer • Oncology • Solid Tumor

IDENTIFICATION OF NOVEL THERAPEUTIC COMPOUNDS FOR THE TREATMENT OF INFANT PATIENTS WITH KMT2A-REARRANGED ACUTE LYMPHOBLASTIC LEUKEMIA BY DRUG REPURPOSING (EHA 2025) - "Additionally, synergistic effects with standard chemotherapy (Vincristine, Dexamethasone, L-Asparaginase; VXL) were assessed.The drug screening identified 119 compounds with selective activity against KMT2Ar iALL while sparing normal cells. This study successfully identified two RTKi as novel therapeutic candidates for KMT2Ar iALL through a drug repurposing approach. Dovitinib and Foretinib have a potent anti-leukemic activity, while sparing healthy cells. Their ability to synergize with standard chemotherapy highlights their potential for clinical application."

Clinical • Acute Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Oncology • CD34 • CDC37 • KMT2A

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 • Cervical Cancer • Cervical Squamous Cell Carcinoma • Oncology • Solid Tumor • Squamous Cell Carcinoma • KIF4A • PQBP1 • UBE2D2

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 • Genito-urinary Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • MET

Small molecule kinase inhibitor altiratinib inhibits brain cyst forming bradyzoites of Toxoplasma gondii. (PubMed, J Microbiol) - "Bradyzoites were obtained from mouse brain cysts, cultured in ARPE-19 cells, and treated with afatinib and neratinib (HER2/HER4 inhibitors), ACTB-1003 and regorafenib (VEGFR-2 inhibitors), or altiratinib and foretinib (c-MET inhibitors). Altiratinib demonstrated an effect against bradyzoites at the lowest concentration with minimal impact on the host cells. It may be effective in blocking the reactivation of brain cysts in immunodeficiency patients caused by bradyzoites."

Journal • Infectious Disease • ERBB4 • HER-2

Emerging AXL Inhibitors in Oncology: Chemical and Biological Advances in Targeted Cancer Therapy. (PubMed, Anticancer Agents Med Chem) - "In conclusion, developing AXL inhibitors represents a promising avenue for improving cancer treatment outcomes. Continued research efforts are essential to overcome the existing challenges and translate these compounds into effective clinical therapies."

Journal • Gene Therapies • Oncology

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."

Journal • Preclinical • Giant Cell Tumor of Bone • Oncology • Osteosarcoma • Solid Tumor • H3-3A

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."

IO biomarker • Journal • Adrenal Cortex Carcinoma • Endocrine Cancer • Genito-urinary Cancer • Metabolic Disorders • Oncology • Solid Tumor • CDH13 • CDH2

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."

Immune cell • IO biomarker • Journal • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • BRCA • CD8 • HER-2 • KRAS • TNFA • TNFSF12

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 • Oncology • EGFR

DRN-CDR: A cancer drug response prediction model using multi-omics and drug features. (PubMed, Comput Biol Chem) - "The drugs such as Tivozanib, SNX-2112, CGP-60474, PHA-665752, Foretinib etc., exhibited low median IC50 values and were found to be effective anti-cancer drugs. The case studies with different TCGA cancer types also revealed the effectiveness of SNX-2112, CGP-60474, Foretinib, Cisplatin, Vinblastine etc. This consistent pattern strongly suggests the effectiveness of the model in predicting CDR."

Journal • Oncology

Machine learning-based integration develops a multiple programmed cell death signature for predicting the clinical outcome and drug sensitivity in colorectal cancer. (PubMed, Anticancer Drugs) - "In addition, the high-MPCDI group was more sensitive to AZD1332, Foretinib, and IGF1R_3801, and insensitive to AZD3759, AZD5438, AZD6482, Erlotinib, GSK591, IAP_5620, and Picolinici-acid, which suggests that the MPCDI can guide drug selection for CRC patients. As a new clinical classifier, the MPCDI can more accurately distinguish CRC patients who benefit from immunotherapy and develop personalized treatment strategies for CRC patients."

Clinical data • Journal • Machine learning • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

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 • Esophageal Cancer • Gastrointestinal Cancer • Oncology • SLC2A1 • STMN1

The combination therapy using tyrosine kinase receptors inhibitors and repurposed drugs to target patient-derived glioblastoma stem cells. (PubMed, Biomed Pharmacother) - "The most cytotoxic compounds for U3042 cells were Disulfiram combined with Copper gluconate (DSF/Cu), Dacomitinib, and Foretinib with IC50 values of 52.37 nM, 4.38 µM, and 4.54 µM after 24 h incubation, respectively. Our findings indicate that the most promising drug combinations are Dacomitinib and Foretinib, Dacomitinib and DSF/Cu, and Foretinib and AZD3759. Since most tested combinations have not been previously examined against glioblastoma stem-like cells, these results can shed new light on designing the therapeutic approach to target the GSC population."

Combination therapy • Journal • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor