TAK-901 / Takeda - LARVOL DELTA

TAK-901, a novel EPHA2 inhibitor as a therapeutic strategy against prostate cancer. (PubMed, Cell Signal) - "Our study is the first to reveal that TAK-901 induces apoptosis in prostate cancer cells and inhibits cell growth by targeting EPHA2. These findings provide valuable insights into the underlying mechanisms of TAK-901 and may develop its therapeutic applications in prostate cancer."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AURKB

Identification of therapeutic targets for Alzheimer's Disease Treatment using bioinformatics and machine learning. (PubMed, Sci Rep) - "Furthermore, Noscapine, PX-316, and TAK-901 were selected as potential therapeutic drugs for AD based on PLCB1. This research provides a comprehensive and reliable method for the discovery of AD therapeutic targets and the construction of diagnostic models, offering important insights and directions for future AD treatment strategies and drug development."

Journal • Alzheimer's Disease • CNS Disorders • KRAS

TAK-901 targeted inhibition of EGFR activates transcription factor FOXO causing cell cycler arrest and apoptosis in bladder cancer (EAU 2025) - No abstract available

Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • EGFR

Precise Drug Combinations for Pediatric AML (EACR-AACR 2024) - "Further, Aurora B inhibitors have been shown to synergize with BCl-xL inhibition in cancer leading us to test the combination treatment of TAK-901(Aurora B kinase inhibitor) with Navitoclax (Bcl-Xl inhibitor). Conclusion The synergistic effect of the lower doses of these two drugs will then be tested in AML cells taken directly from patients and in clinically relevant mouse models of human AML to identify effective treatment of high-risk AML. The identified drug combination may promise more efficacious therapies to improve outcomes for this group of patients who respond poorly to current therapies."

Clinical • Acute Myelogenous Leukemia • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Oncology • Pediatrics • BCL2L1

Unveiling Epigenetic Vulnerabilities in Triple-Negative Breast Cancer through 3D Organoid Drug Screening. (PubMed, Pharmaceuticals (Basel)) - "Four compounds, panobinostat, pacritinib, TAK-901, and JIB-04, targeting histone deacetylase, JAK/STAT, histone demethylases, and aurora kinase pathways, respectively, exhibited potent anti-tumor activity in TNBC organoids, surpassing the effect of paclitaxel. Our study highlights the potential of these novel epigenetic drugs as effective therapeutic agents for TNBC and demonstrates the valuable role of patient-derived organoids in advancing drug discovery."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Inhibitors of One or More Cellular Aurora Kinases Impair the Replication of Herpes Simplex Virus 1 and Other DNA and RNA Viruses with Diverse Genomes and Life Cycles. (PubMed, Microbiol Spectr) - "The compounds TAK 901, JNJ 7706621, and PF 03814735 decreased HSV-1 titers by 4,500-, 13,200-, and 8,400-fold, respectively, when present in a low micromolar range. Together, our results illustrate a novel role for aurora kinases in the HSV-1 lytic cycle and demonstrate that aurora kinase inhibitors can restrict HSV-1 replication. Furthermore, these aurora kinase inhibitors also reduced the replication of murine coronavirus and vaccinia virus, suggesting that multiple viral families utilize the aurora kinases for their own replication."

Journal • Hepatology • Herpes Simplex • Infectious Disease • Inflammation • Novel Coronavirus Disease

The Aurora Kinase Inhibitor TAK901 Inhibits Glioblastoma Growth by Blocking SREBP1-Mediated Lipid Metabolism. (PubMed, Cancers (Basel)) - "The standard treatment for GBM including surgical resection followed by radiation therapy and adjuvant chemotherapy with temozolomide remains unsatisfactory. Moreover, SREBP1 overexpression alleviated the TAK901-mediated suppression of cell viability and apoptosis in GBM cells. Our results provide evidence that TAK901 inhibits GBM growth by suppressing SREBP1-mediated lipid metabolism."

Journal • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Metabolic Disorders • Oncology • Solid Tumor

Epigenome-wide DNA methylation analysis of small cell lung cancer cell lines suggests potential chemotherapy targets. (PubMed, Clin Epigenetics) - "Multiple associations indicate potential epigenetic mechanisms affecting SCLC response to chemotherapy and suggest targets for combination therapies. While many correlations were not specific to SCLC lineages, several lineage markers were associated with specific agents."

IO Biomarker • Journal • Preclinical • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor • Thoracic Cancer • ATR • EPAS1 • EPHA2 • EZH2 • SLFN11 • STING • YAP1

Study of TAK-901 in adults with advanced solid tumors or lymphoma (clinicaltrials.gov) - P1, N=20; N=54 -> 20; Active, not recruiting -> Completed

Enrollment • Trial completion • Hematological Malignancies • Oncology

Study of TAK-901 in adults with advanced solid tumors or lymphoma (clinicaltrials.gov) - P1, N=54; Recruiting → Active, not recruiting

Enrollment closed • Hematological Malignancies

The investigational multi-targeted kinase inhibitor TAK-901 antagonizes acute myeloid leukemia pathogenesis: Results of preclinical studies (ASH 2011) - Presentation Time: Monday, December 12, 2011: 3:45 PM; TAK-901 potently diminished the viability of a panel of 8 AML cell lines & primary cells obtained from patients with AML; Acute exposure to TAK-901 ablated clonogenic survival, triggered the accumulation of polyploid cells, & induced apoptosis; The cytostatic & cytotoxic effects of TAK-901 were associated with significantly increased expression of the cyclin-dependent kinase inhibitor p27, growth arrest & DNA-damage-inducible 45a (GADD45a), & BH3-only pro-apoptotic protein PUMA

Preclinical-animal • Preclinical-other • Oncology

Associations of epigenome-wide DNA methylation patterns with chemosensitivity and chemoresistance of small cell lung cancer cell lines (AACR-NCI-EORTC 2019) - "Increased methylation and low expression of TREX1 were associated with SCLC cell line sensitivity to multiple Aurora kinase inhibitors AZD-1152, SCH-1473759, SNS-314, and TAK-901, as well as to the CDK inhibitor R-547, Vertex ATR inhibitor Cpd 45, and the mitotic spindle disruptor vinorelbine...Among other examples, EPAS1 (HIF2A) was associated with several Aurora kinase inhibitors, the PLK1 inhibitor GSK-461364, and the Bcl-2 inhibitor ABT-737...IGFBP5, which is expressed in the tuft cell-like SCLC subtype, was associated with the mTOR inhibitor INK-128...Methylation and expression of YAP1, a SCLC lineage driver regulating the Hippo pathway, were correlated with the MTOR inhibitor rapamycin...The 5’ UTR region of the epigenetic modifier EZH2 was associated with Aurora kinase inhibitors and the FGFR inhibitor BGJ-398. These and multiple other associations identified in this study provide a novel understanding of epigenetic mechanisms which may modulate SCLC response to..."

IO Biomarker • Preclinical • EPAS1 • EPHA2 • EZH2