^
    2d
    CheckMate 040: An Immuno-therapy Study to Evaluate the Effectiveness, Safety and Tolerability of Nivolumab or Nivolumab in Combination With Other Agents in Patients With Advanced Liver Cancer (clinicaltrials.gov)
    P1/2, N=659, Completed, Bristol-Myers Squibb | Active, not recruiting --> Completed | Trial completion date: Jun 2024 --> Nov 2024 | Trial primary completion date: Jun 2024 --> Nov 2024
    Trial completion • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • sorafenib • Cabometyx (cabozantinib tablet)
    2d
    CABRAMET: Evaluation of Cabozantinib in Metastatic Renal Cell Carcinoma (mRCC) With Brain Metastases (clinicaltrials.gov)
    P2, N=26, Completed, Centre Leon Berard | Recruiting --> Completed | N=77 --> 26 | Trial primary completion date: Nov 2023 --> Oct 2024
    Trial completion • Enrollment change • Trial primary completion date • Metastases
    |
    Cabometyx (cabozantinib tablet)
    3d
    Cabozantinib inhibits tumor growth in mice with ovarian cancer. (PubMed, Am J Cancer Res)
    Improved outcome in cabozantinib treated mice was associated with a significantly higher percentage of CD69 early activated T cells, a higher percentage of granzyme B secreting CD8 T cells, the enhanced release of cytokines and chemokines known to recruit CD8 T cells and amplify T cell function, as well as reduced VEGFR-2. Findings suggest that cabozantinib is an important clinical agent capable of improving ovarian cancer in mice potentially in part by priming the autologous immune system to promote anti-tumor immunity.
    Preclinical • Journal
    |
    CD8 (cluster of differentiation 8) • KDR (Kinase insert domain receptor) • CD69 (CD69 Molecule) • GZMB (Granzyme B)
    |
    Cabometyx (cabozantinib tablet)
    3d
    Study of Targeted Therapy vs. Chemotherapy in Patients With Thyroid Cancer (clinicaltrials.gov)
    P3, N=264, Recruiting, ECOG-ACRIN Cancer Research Group | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Cabometyx (cabozantinib tablet)
    6d
    Cabozantinib S-malate in Treating Patients with Metastatic Pheochromocytomas or Paragangliomas That Cannot Be Removed by Surgery (clinicaltrials.gov)
    P2, N=21, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed
    Trial completion • Surgery • Metastases
    |
    Cabometyx (cabozantinib tablet) • Cometriq (cabozantinib capsule)
    8d
    Cabozantinib and Abiraterone With Checkpoint Inhibitor Immunotherapy in Metastatic Hormone Sensitive Prostate Cancer (CABIOS Trial) (clinicaltrials.gov)
    P1, N=18, Active, not recruiting, Washington University School of Medicine | Trial completion date: Mar 2026 --> Sep 2025
    Trial completion date
    |
    Opdivo (nivolumab) • Cabometyx (cabozantinib tablet) • abiraterone acetate • prednisone
    15d
    Rapid Sequencing of Approved Therapies in Patients with Metastatic or Unresectable Clear Cell Renal Cell Carcinoma (clinicaltrials.gov)
    P1, N=20, Recruiting, Icahn School of Medicine at Mount Sinai | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Sep 2026
    Trial completion date • Trial primary completion date • Metastases
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • everolimus • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet)
    17d
    Testing the Addition of the Pill Chemotherapy, Cabozantinib, to the Standard Immune Therapy Nivolumab Compared to Standard Chemotherapy for Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=117, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2024 --> Jun 2025 | Trial primary completion date: Dec 2024 --> Jun 2025
    Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    KRAS G12C • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • ALK rearrangement • EGFR L861Q • ROS1 positive • KRAS G12 • EGFR exon 20 mutation • MET positive • EGFR negative
    |
    Opdivo (nivolumab) • gemcitabine • docetaxel • Cabometyx (cabozantinib tablet) • albumin-bound paclitaxel • Cyramza (ramucirumab) • Cometriq (cabozantinib capsule) • ABP 206 (nivolumab biosimilar)
    22d
    Type I MET inhibitors cooperate with PD-1 blockade to promote rejection of hepatocellular carcinoma. (PubMed, J Immunother Cancer)
    In vitro studies of antigen-specific T cell activation reveal significantly less inhibition of effector cytokine production and proliferation by capmatinib versus by type II or type III MET inhibitors. These findings suggest significant potential for clinical HCC combination studies of type I MET inhibitors and PD-1 blockade where prior trials using type II inhibitors have yielded limited benefit.
    Journal
    |
    PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • MAGEE1 (MAGE family member E1)
    |
    Cabometyx (cabozantinib tablet) • Tabrecta (capmatinib)
    22d
    Clinical significance of upregulated Rho GTPase activating protein 12 causing resistance to tyrosine kinase inhibitors in hepatocellular carcinoma. (PubMed, World J Gastrointest Oncol)
    ARHGAP12 expression is elevated in HCC and TKI-resistant HCC, and its regulatory role in FA may underlie the TKI-resistant phenotype.
    Journal • IO biomarker
    |
    ITGA6 (Integrin, alpha 6) • ITGB1 (Integrin Subunit Beta 1)
    |
    sorafenib • Cabometyx (cabozantinib tablet) • Stivarga (regorafenib)
    22d
    COSMIC-313: Study of Cabozantinib in Combination With Nivolumab and Ipilimumab in Patients With Previously Untreated Advanced or Metastatic Renal Cell Carcinoma (clinicaltrials.gov)
    P3, N=855, Completed, Exelixis | Active, not recruiting --> Completed | Trial completion date: Mar 2025 --> May 2024
    Trial completion • Trial completion date • Combination therapy • Metastases
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet)
    24d
    Immunotherapy With Nivolumab and Ipilimumab Followed by Nivolumab or Nivolumab With Cabozantinib for Patients With Advanced Kidney Cancer, The PDIGREE Study (clinicaltrials.gov)
    P3, N=1175, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Sep 2024 --> Sep 2025 | Trial primary completion date: Sep 2024 --> Sep 2025
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet) • ABP 206 (nivolumab biosimilar)
    1m
    CaboTx: Cabozantinib to Treat Recurrent Liver Cancer Post Transplant (clinicaltrials.gov)
    P2, N=20, Recruiting, University Health Network, Toronto | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Aug 2024 --> Aug 2025
    Trial completion date • Trial primary completion date • Post-transplantation
    |
    Cabometyx (cabozantinib tablet)
    1m
    A Phase II Study of Nivolumab with Ipilimumab and Cabozantinib in Patients with Untreated Renal Cell Carcinoma Brain Metastases (clinicaltrials.gov)
    P2, N=40, Recruiting, M.D. Anderson Cancer Center | Suspended --> Recruiting
    Enrollment open
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet)
    1m
    Atezolizumab and Cabozantinib for the Treatment of Adolescents and Young Adults with Recurrent or Metastatic Osteosarcoma, TACOS Study (clinicaltrials.gov)
    P2, N=40, Recruiting, M.D. Anderson Cancer Center | Suspended --> Recruiting
    Enrollment open • Metastases
    |
    Tecentriq (atezolizumab) • Cabometyx (cabozantinib tablet)
    1m
    Cabozantinib prevents the progression of metabolic dysfunction-associated steatohepatitis by inhibiting the activation of hepatic stellate cell and macrophage and attenuating angiogenic activity. (PubMed, Heliyon)
    Treatment with cabozantinib also reduced the placental glutathione transferase+ preneoplastic lesions in CDAHFD-fed rats. In conclusion, cabozantinib shows promise as a novel option for preventing MASH progression.
    Journal
    |
    AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • ACTA2 (Actin Alpha 2 Smooth Muscle) • CD34 (CD34 molecule) • CD68 (CD68 Molecule) • GAS6 (Growth arrest specific 6) • TGFB1 (Transforming Growth Factor Beta 1) • COL1A1 (Collagen Type I Alpha 1 Chain) • IL1B (Interleukin 1, beta)
    |
    KDR expression
    |
    Cabometyx (cabozantinib tablet)
    1m
    Preparation of dual drug-loaded polymer nanoconjugate to enhance treatment efficacy for ovarian cancer cells. (PubMed, Eur J Pharm Biopharm)
    In vitro studies have demonstrated that Ki-PEG-CBZ is highly effective against ovarian cancer. We suggest that the developed polymer-drug nanoconjugate is an effective and safe nanoconjugate for the treatment of ovarian cancer.
    Journal
    |
    FLT3 (Fms-related tyrosine kinase 3) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • FLT1 (Fms-related tyrosine kinase 1)
    |
    Cabometyx (cabozantinib tablet)
    1m
    Testing Ipilimumab and Nivolumab Combination With or Without Cabozantinib in People >= 18 Years Old With Advanced Soft Tissue Sarcoma (clinicaltrials.gov)
    P2, N=66, Recruiting, National Cancer Institute (NCI) | Suspended --> Recruiting
    Enrollment open • Tumor mutational burden • IO biomarker • Metastases
    |
    TMB (Tumor Mutational Burden) • CD68 (CD68 Molecule)
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet) • ABP 206 (nivolumab biosimilar)
    1m
    Silmitasertib in Combination With Cabozantinib Impairs Liver Cancer Cell Cycle Progression, Induces Apoptosis, and Delays Tumor Growth in a Preclinical Model. (PubMed, Mol Carcinog)
    Next, we observed that a combination therapy significantly delayed the progression of HCC xenograft growth as compared to vehicle control. Together, our results suggested combining cabozantinib and silmitasertib would be a promising treatment option for HCC.
    Preclinical • Journal • Combination therapy
    |
    BCL2L11 (BCL2 Like 11) • CCNA2 (Cyclin A2) • CASP9 (Caspase 9) • RPS6 (Ribosomal Protein S6) • CDC25C (Cell Division Cycle 25C) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)
    |
    Cabometyx (cabozantinib tablet) • silmitasertib (CX-4945)
    2ms
    Cabozantinib enhances CAIX specific CAR-T cells against renal cancer by improving effector functions and augmenting tumor immune microenvironment. (PubMed, Biochem Biophys Res Commun)
    Furthermore, Cabozantinib promoted CAR-T cell effector function and reduced T cell exhaustion. This combination therapy represents a novel approach to enhancing CAR-T cell efficacy against solid tumors and holds significant promise for advancing CAR-T cell therapy in clinical settings.
    Journal • CAR T-Cell Therapy • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • CA9 (Carbonic anhydrase 9)
    |
    PD-L1 expression
    |
    Cabometyx (cabozantinib tablet)
    2ms
    Cabozantinib-encapsulated and maytansine-conjugated high-density lipoprotein for immunotherapy in colorectal cancer. (PubMed, J Control Release)
    ECCD-sHDL increased the densities of active cytotoxic T lymphocytes (CTLs) and M1 macrophages in the tumors, effectively inhibiting tumor growth and metastasis, thereby prolonging survival in murine CRC models. Our study sheds light on the mechanism of treatment-induced immunosuppression in orthotopic CRC and demonstrates that this combinatorial therapy could be an effective treatment for CRC.
    Journal
    |
    IL13 (Interleukin 13)
    |
    Cabometyx (cabozantinib tablet)
    2ms
    CABOTHYROID: Cabozantinib In Advanced Radioactive-Iodine Refractory Differentiated Thyroid Cancer. (clinicaltrials.gov)
    P2, N=41, Active, not recruiting, Grupo Espanol de Tumores Neuroendocrinos | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    sunitinib • Cabometyx (cabozantinib tablet)
    2ms
    Design, synthesis and biological evaluation of thienopyridine derivatives as c-Met kinase inhibitors. (PubMed, Mol Divers)
    The AO/EB assay demonstrated that compound 10 possesses the capability to effectively trigger apoptosis in a concentration-dependent manner. The elementary structure-activity relationship, molecular docking and pharmacokinetics studies revealed the significance of thieno [2,3-b] pyridine derivatives in anti-tumor activity.
    Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    Cabometyx (cabozantinib tablet)
    2ms
    Lenvatinib with Everolimus Versus Cabozantinib for Second-Line or Third-Line Treatment of Metastatic Renal Cell Cancer (clinicaltrials.gov)
    P2, N=90, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    PD-L1 (Programmed death ligand 1)
    |
    everolimus • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet)
    2ms
    CaboCombo: A Study of the Effectiveness of Cabozantinib in Combination With Nivolumab as First-line Treatment of Advanced Renal Cell Carcinoma (aRCC) in Adults (clinicaltrials.gov)
    P=N/A, N=311, Active, not recruiting, Ipsen | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    Opdivo (nivolumab) • Cabometyx (cabozantinib tablet)
    2ms
    Screening of differential gene expression patterns through survival analysis for diagnosis, prognosis and therapies of clear cell renal cell carcinoma. (PubMed, PLoS One)
    Then we detected 10 repurposable drug molecules (Irinotecan, Imatinib, Telaglenastat, Olaparib, RG-4733, Sorafenib, Sitravatinib, Cabozantinib, Abemaciclib, and Dovitinib.) by molecular docking with KGs-mediated receptor proteins. Their ADME/T analysis and cross-validation with the independent receptors, also supported their potent against ccRCC. Therefore, these outputs might be useful inputs/resources to the wet-lab researchers and clinicians for considering an effective treatment strategy against ccRCC.
    Journal • PARP Biomarker
    |
    CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • SERPINA5 (Serpin Family A Member 5)
    |
    Lynparza (olaparib) • sorafenib • imatinib • Verzenio (abemaciclib) • Cabometyx (cabozantinib tablet) • irinotecan • dovitinib (TKI258) • telaglenastat (CB-839) • sitravatinib (MGCD516) • RG4733
    2ms
    Molecular genetics, therapeutics and RET inhibitor resistance for medullary thyroid carcinoma and future perspectives. (PubMed, Cell Commun Signal)
    Two multi-kinase inhibitors (MKIs) including Cabozantinib and Vandetanib have been shown to increase progression-free survival (PFS) for patients with metastatic MTC and have been approved as choices of first-line treatment...Recently, new generation TKIs, including Selpercatinib and Pralsetinib, have demonstrated highly selective efficacy against RET and more favorable side effect profiles, and gained approval as second-line treatment options...Besides, new promising therapeutic approaches, such as novel drug combinations and next generation RET inhibitors are under development. Herein, we overview the pathogenesis, molecular genetics and current management approaches of MTC, and focus on the recent advances of RET inhibitors, summarize the current situation and unmet needs of these RET inhibitors in MTC, and provide an overview of novel strategies for optimizing therapeutic effects.
    Review • Journal
    |
    RET (Ret Proto-Oncogene)
    |
    RET mutation • RET rearrangement
    |
    Cabometyx (cabozantinib tablet) • Retevmo (selpercatinib) • Gavreto (pralsetinib) • Caprelsa (vandetanib)
    2ms
    Cabozantinib Plus Atezolizumab or Cabozantinib Alone in Patients With Advanced NSCLC Previously Treated With an Immune Checkpoint Inhibitor: Results From the Phase 1b COSMIC-021 Study. (PubMed, JTO Clin Res Rep)
    Neither PD-L1 expression in tumor cells nor tumor mutation burden correlated with outcomes. Cabozantinib plus atezolizumab demonstrated modest clinical activity and manageable toxicity in advanced NSCLC after progression on prior ICI.
    Clinical • P1 data • Journal • Checkpoint inhibition • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker • Metastases
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TMB (Tumor Mutational Burden) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • BRAF V600E • BRAF V600
    |
    Tecentriq (atezolizumab) • Cabometyx (cabozantinib tablet)
    2ms
    Cabozantinib and Temozolomide for the Treatment of Unresectable or Metastatic Leiomyosarcoma or Other Soft Tissue Sarcoma (clinicaltrials.gov)
    P2, N=72, Active, not recruiting, City of Hope Medical Center | Trial completion date: Sep 2024 --> Dec 2024 | Trial primary completion date: Sep 2024 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    temozolomide • Cabometyx (cabozantinib tablet)
    2ms
    Cabozantinib and Pembrolizumab for Advanced Metastatic Melanoma (clinicaltrials.gov)
    P1/2, N=28, Active, not recruiting, John Rieth | Recruiting --> Active, not recruiting | N=62 --> 28 | Trial primary completion date: Dec 2026 --> Jun 2024
    Enrollment closed • Enrollment change • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1) • BRAF (B-raf proto-oncogene)
    |
    Keytruda (pembrolizumab) • Cabometyx (cabozantinib tablet) • Cometriq (cabozantinib capsule)
    2ms
    Testing the Addition of the Pill Chemotherapy, Cabozantinib, to the Standard Immune Therapy Nivolumab Compared to Standard Chemotherapy for Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=117, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Sep 2024 --> Dec 2024 | Trial primary completion date: Sep 2024 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    KRAS G12C • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • ALK rearrangement • EGFR L861Q • ROS1 positive • KRAS G12 • EGFR exon 20 mutation • MET positive • EGFR negative
    |
    Opdivo (nivolumab) • gemcitabine • docetaxel • Cabometyx (cabozantinib tablet) • albumin-bound paclitaxel • Cyramza (ramucirumab) • Cometriq (cabozantinib capsule) • ABP 206 (nivolumab biosimilar)
    2ms
    A Phase II Study of Nivolumab With Ipilimumab and Cabozantinib in Patients With Untreated Renal Cell Carcinoma Brain Metastases (clinicaltrials.gov)
    P2, N=40, Suspended, M.D. Anderson Cancer Center | Recruiting --> Suspended
    Trial suspension
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet)
    2ms
    Study of Ipilimumab, Nivolumab, and Cabozantinib in Patients With Cutaneous Melanoma (clinicaltrials.gov)
    P2, N=4, Terminated, Providence Health & Services | Completed --> Terminated; Withdrawn support from BMS.
    Trial termination
    |
    BRAF (B-raf proto-oncogene)
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet)
    2ms
    CA209-9KU: A Study of Nivolumab In Combination With Cabozantinib in Patients With Non-Clear Cell Renal Cell Carcinoma (clinicaltrials.gov)
    P2, N=60, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Aug 2024 --> Aug 2025 | Trial primary completion date: Aug 2024 --> Aug 2025
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Opdivo (nivolumab) • Cabometyx (cabozantinib tablet)
    3ms
    Cabozantinib for Patients With Hepatocellular Carcinoma (HCC) Refractory to First Line Treatment (clinicaltrials.gov)
    P2, N=22, Active, not recruiting, Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest | Recruiting --> Active, not recruiting | N=45 --> 22 | Trial completion date: Dec 2025 --> Jan 2025 | Trial primary completion date: Jun 2025 --> Dec 2024
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    Cabometyx (cabozantinib tablet)
    3ms
    Niraparib in Combination With Cabozantinib (XL184) in Patients With Advanced Urothelial Cancer (NICARAGUA) (clinicaltrials.gov)
    P1/2, N=67, Completed, Fundacion CRIS de Investigación para Vencer el Cáncer | Active, not recruiting --> Completed | N=20 --> 67 | Trial completion date: Apr 2024 --> Jul 2024 | Trial primary completion date: Apr 2024 --> Jul 2024
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    Zejula (niraparib) • Cabometyx (cabozantinib tablet)
    3ms
    CONTACT-01: Study of Atezolizumab in Combination With Cabozantinib Versus Docetaxel in Patients With Metastatic Non-Small Cell Lung Cancer Previously Treated With an Anti-PD-L1/PD-1 Antibody and Platinum-Containing Chemotherapy (clinicaltrials.gov)
    P3, N=366, Active, not recruiting, Hoffmann-La Roche | Trial completion date: Oct 2024 --> Jan 2025
    Trial completion date • Combination therapy • Metastases
    |
    Tecentriq (atezolizumab) • docetaxel • Cabometyx (cabozantinib tablet)
    3ms
    Sequential therapy for hereditary leiomyomatosis and renal cell cancer-associated renal cell carcinoma: a case report and report of a new family pedigree. (PubMed, Oxf Med Case Reports)
    Here, we report a patient with HLRCC-associated RCC treated with sequential therapy, including ipilimumab plus nivolumab combination and cabozantinib, after diagnosis of HLRCC-associated RCC using FoundationOne Liquid CDx and single-site analysis. We also investigated familial FH mutations and describe a new family pedigree for HLRCC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    FH (Fumarate Hydratase)
    |
    FoundationOne® Liquid CDx
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet)
    3ms
    Recent advancements in the small-molecule drugs for hepatocellular carcinoma (HCC): Structure-activity relationships, pharmacological activities, and the clinical trials. (PubMed, Biomed Pharmacother)
    By revealing their structure-activity relationships, pharmacological actions, and clinical trials, small-molecule drugs can offer broad prospects for the development of new medications.
    Review • Journal
    |
    EGFR (Epidermal growth factor receptor) • FGFR (Fibroblast Growth Factor Receptor)
    |
    sorafenib • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet) • Stivarga (regorafenib)
    3ms
    Savolitinib conferred sensitivity in a patient with D1228H mutation-induced capmatinib-resistant MET exon 14 skipping mutated lung adenocarcinoma. (PubMed, J Cancer Res Clin Oncol)
    The switch of resistance mutations indicated that different type Ib MET inhibitors may exhibit distinct mechanisms of resistance. We call for futher studies on resistance based on patient-derived pre-clinical models including patient-derived tumor-like cell clusters, patient-derived organoids, and patient-derived xenografts.
    Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    Cabometyx (cabozantinib tablet) • Orpathys (savolitinib) • Tabrecta (capmatinib)
    3ms
    Interaction of Purine and its Derivatives with A1, A2-Adenosine Receptors and Vascular Endothelial Growth Factor Receptor-1 (Vegf-R1) as a Therapeutic Alternative to Treat Cancer. (PubMed, Drug Res (Stuttg))
    Besides, adenosine, cgs-15943, rolofylline, cvt-124, wrc-0571, luf-5834, cvt-6883, AZD-4635, cabozantinib, pazopanib, regorafenib, and sorafenib drugs were used as controls...Besides, the inhibition constants (Ki) values for purine and their derivatives 5: , 9: , 10: , 14: , 15: , 16: , and 20: were lower compared with the controls Theoretical data suggest that purine and their derivatives 5: , 9: , 10: , 14: , 15: , 16: , and 20: could produce changes in cancer cell growth through inhibition of A1, A2-adenosine receptors and VEGFR-1 inhibition. These data indicate that these purine derivatives could be a therapeutic alternative to treat some types of cancer.
    Journal
    |
    VEGFA (Vascular endothelial growth factor A) • FLT1 (Fms-related tyrosine kinase 1)
    |
    sorafenib • pazopanib • Cabometyx (cabozantinib tablet) • Stivarga (regorafenib) • imaradenant (AZD4635)
    3ms
    Pembrolizumab and cabozantinib in recurrent and/or metastatic head and neck squamous cell carcinoma (RMHNSCC): long-term survival update with a biomarker analysis. (PubMed, Clin Cancer Res)
    Pembrolizumab and cabozantinib provided prolonged encouraging long-term disease control and survival with a maintained favorable safety profile. The prognostic significance of increased CD8+, CD103+ and CSF1-R+ cell density in TIME deserve further evaluation in similar clinical settings.
    Journal • PD(L)-1 Biomarker • IO biomarker • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • CD8 (cluster of differentiation 8) • CSF1 (Colony stimulating factor 1) • CSF1R (Colony stimulating factor 1 receptor) • ITGAE (Integrin Subunit Alpha E)
    |
    Keytruda (pembrolizumab) • Cabometyx (cabozantinib tablet)