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    DRUG:

    Stivarga (regorafenib)

    i
    Other names: BAY 73-4506, BAY-734506, BAY 734506, BAY734506
    Company:
    Amgen, Bayer
    Drug class:
    Multi-tyrosine kinase inhibitor
    Related drugs:
    20h
    STREAM-2: Second-line Treatment With REgorafenib in Advanced RAS-Mutant Colorectal Cancer (clinicaltrials.gov)
    P2, N=60, Recruiting, National Cancer Institute, Naples
    Trial initiation date
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    MSI (Microsatellite instability) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • DPYD (Dihydropyrimidine Dehydrogenase)
    |
    RAS mutation
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    Avastin (bevacizumab) • capecitabine • Stivarga (regorafenib) • oxaliplatin • irinotecan
    4d
    Predictive factors for early mortality after regorafenib or trifluridine/tipiracil initiation in metastatic colorectal cancer. (PubMed, Oncologist)
    Our predictive model may help identify patients at high risk of early mortality after regorafenib or trifluridine/tipiracil initiation and support shared decision-making between clinicians and patients regarding further chemotherapy or best supportive care.
    Retrospective data • Journal
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    CRP (C-reactive protein)
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    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    5d
    Macrophage-Derived PDGF-BB and GDF-15 Promote Drug Resistance in KRAS-Mutant Colorectal Cancer. (PubMed, bioRxiv)
    In contrast, macrophage-conditioned medium had little effect on regorafenib and increased sensitivity to dabrafenib, suggesting that resistance depends on the inhibitory profile of each drug. The multi-kinase inhibitor masitinib-which targets several kinases along this resistance network-strongly restored sensitivity to trametinib and RMC-6236. Together, these data define a macrophage-driven resistance network in KRAS-mutant colorectal cancer organoids and support combined inhibition of RAS-pathway and tyrosine kinase signalling.
    Journal
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    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • GDF15 (Growth differentiation factor 15)
    |
    KRAS mutation
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    Mekinist (trametinib) • Tafinlar (dabrafenib) • Stivarga (regorafenib) • daraxonrasib (RMC-6236) • Kinaction (masitinib)
    5d
    Clinical Study of Novel Therapeutic Vaccine for Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=54, Recruiting, West China Hospital | Not yet recruiting --> Recruiting
    Enrollment open • IO biomarker • First-in-human
    |
    RAS wild-type
    |
    Stivarga (regorafenib)
    6d
    Clinical Study of Novel Therapeutic Vaccine for Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=54, Not yet recruiting, West China Hospital
    New P1 trial • IO biomarker • First-in-human
    |
    RAS wild-type
    |
    Stivarga (regorafenib)
    10d
    Regorafenib and Yttrium-90 Radioembolization for Unresectable Hepatocellular Carcinoma (clinicaltrials.gov)
    P2, N=30, Recruiting, University of Miami | Trial completion date: May 2031 --> Aug 2031 | Trial primary completion date: May 2031 --> Aug 2031
    Trial completion date • Trial primary completion date
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    Stivarga (regorafenib) • TheraSphere (yttrium 90 microspheres)
    11d
    Prior response to anti-VEGF agents predicts the efficacy of trifluridine/tipiracil plus bevacizumab in patients with metastatic colorectal cancer. (PubMed, Int J Clin Oncol)
    The response to anti-VEGF agents in second-line therapy may predict the efficacy of FTD/TPI + Bev in subsequent treatments.
    Journal
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation • RAS mutation
    |
    Avastin (bevacizumab) • Stivarga (regorafenib) • Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil)
    13d
    Flavokawain A Targets CXCR4-Mediated Vasculogenic Mimicry to Reverse Hepatocellular Carcinoma Resistance to Tyrosine Kinase Inhibitors. (PubMed, Phytother Res)
    Tyrosine kinase inhibitors (TKIs), such as sorafenib, lenvatinib, and regorafenib, serve as the mainstay targeted therapies for advanced hepatocellular carcinoma (HCC), yet resistance severely limits their clinical benefits. FKA disrupted the VM phenotype by directly targeting CXCR4, and synergized with TKI to inhibit HCC growth in vitro and in vivo, with its efficacy being CXCR4-dependent. Collectively, our findings suggest that CXCR4 promotes VM to drive TKI resistance and reveal that FKA, as a potential CXCR4 inhibitor, represents a promising therapeutic strategy in combination with TKIs to overcome resistance in HCC.
    Journal
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    CDH1 (Cadherin 1) • MMP2 (Matrix metallopeptidase 2) • VIM (Vimentin) • CDH5 (Cadherin 5) • MMP14 (Matrix Metallopeptidase 14)
    |
    sorafenib • Lenvima (lenvatinib) • Stivarga (regorafenib)
    15d
    CodeBreak 300: Sotorasib and Panitumumab Versus Investigator's Choice for Participants With Kirsten Rat Sarcoma (KRAS) p.G12C Mutation (clinicaltrials.gov)
    P3, N=160, Completed, Amgen | Active, not recruiting --> Completed
    Trial completion
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    therascreen® KRAS RGQ PCR Kit
    |
    Vectibix (panitumumab) • Lumakras (sotorasib) • Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    17d
    MegaMOST: A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors. (clinicaltrials.gov)
    P2, N=455, Recruiting, Centre Leon Berard | Trial completion date: Nov 2026 --> Oct 2027 | Trial primary completion date: Feb 2026 --> Oct 2026
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • FLT3 (Fms-related tyrosine kinase 3) • MET (MET proto-oncogene, receptor tyrosine kinase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • HRAS (Harvey rat sarcoma viral oncogene homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • NF1 (Neurofibromin 1) • AXL (AXL Receptor Tyrosine Kinase) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11) • SMAD4 (SMAD family member 4) • RAF1 (Raf-1 Proto-Oncogene Serine/Threonine Kinase) • FLT1 (Fms-related tyrosine kinase 1) • CDK6 (Cyclin-dependent kinase 6) • CCND3 (Cyclin D3) • TYRO3 (TYRO3 Protein Tyrosine Kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    BRAF mutation • NRAS mutation • BRAF V600 • KIT mutation • CDKN2A deletion • HRAS mutation • KRAS G12 • PDGFRA mutation • KRAS amplification • NRAS G12
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Alecensa (alectinib) • Cabometyx (cabozantinib tablet) • Stivarga (regorafenib) • Kisqali (ribociclib) • Ayvakit (avapritinib) • siremadlin (HDM201)
    18d
    Physicochemical characteristics and anti-colorectal cancer activity of Salvia miltiorrhiza Bunge polysaccharides. (PubMed, Front Nutr)
    The anti-colorectal cancer activity and underlying mechanisms of SMP-3, both alone and in combination with regorafenib (REG), were evaluated in vitro using HCT116 colorectal cancer cells and normal FHC cells through cytotoxicity, Western blot, and immunofluorescence analyses...Mechanistically, the combination treatment upregulated p21, Bax, and caspase-3 expression while downregulating cyclin D1, CDK4, and Bcl-2, and profoundly suppressed the phosphorylation of STAT3, AKT, and ERK signaling pathways. These findings suggest that SMP-3 possesses distinct structural characteristics and significant anti-tumor efficacy, making it a promising medical food candidate for colorectal cancer treatment.
    Journal • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    |
    Stivarga (regorafenib)
    19d
    Combination of regorafenib and cadonilimab treated with local advanced or metastatic hepatocellular carcinoma after first-line treatment failure:a single-arm open study (ChiCTR2600120728)
    P2, N=50, Recruiting, Department of Oncology, Tongji Hospital Affiliated to Tongji Medical College, Huazhong University of Science and Technology; Department of Oncology, T
    New P2 trial
    |
    Stivarga (regorafenib) • Kaitanni (cadonilimab)