^
    5d
    Blockade of Discoidin Domain Receptor Signaling with Sitravatinib Reveals DDR2 as a Mediator of Neuroblastoma Pathogenesis and Metastasis. (PubMed, Mol Cancer Ther)
    Analysis of single cell sequencing data demonstrated that DDR2 is restricted to mesenchymal-type tumor subpopulations and is enriched in Schwann Cell Precursor (SCP) subpopulations found in high-risk disease. These data define an unsuspected role for sitravatinib as a therapeutic agent in neuroblastoma and reveal a novel function for DDR2 as a driver of tumor growth and metastasis.
    Journal
    |
    ALK (Anaplastic lymphoma kinase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • DDR2 (Discoidin domain receptor 2)
    |
    sitravatinib (MGCD516)
    10d
    MRTX-500: Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=161, Terminated, Mirati Therapeutics Inc. | Completed --> Terminated; This study was terminated as a result of Sponsor portfolio reprioritization.
    Trial termination • Combination therapy • Metastases
    |
    Opdivo (nivolumab) • sitravatinib (MGCD516) • glesatinib (MGCD265) • mocetinostat (MGCD0103)
    14d
    BTC-BGB: Phase II Study of Sitravatinib in Combination With Tislelizumab in Patients With Advanced Biliary Tract Cancer (clinicaltrials.gov)
    P2, N=43, Active, not recruiting, Seoul National University Hospital | Trial completion date: Jun 2024 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Jul 2023
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    2ms
    H-43432: Sitravatinib in Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=0, Withdrawn, C. Kent Osborne, MD | Terminated --> Withdrawn
    Trial withdrawal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • ER (Estrogen receptor) • PGR (Progesterone receptor) • PTPN12 (Protein Tyrosine Phosphatase Non-Receptor Type 12)
    |
    sitravatinib (MGCD516)
    2ms
    SITISVEAL: Sitravatinib and Tislelizumab in Patients With Metastatic Uveal Melanoma With Liver Metastases. (clinicaltrials.gov)
    P2, N=16, Active, not recruiting, Grupo Español Multidisciplinar de Melanoma | Recruiting --> Active, not recruiting | N=34 --> 16 | Trial completion date: Aug 2024 --> May 2024
    Enrollment closed • Enrollment change • Trial completion date • Combination therapy • Metastases
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    2ms
    Study To Investigate the Efficacy and Safety of Sitravatinib in Combination With Tislelizumab in Participants With Esophageal Squamous Cell Carcinoma (clinicaltrials.gov)
    P2, N=96, Terminated, BeiGene
    Trial completion date • Trial termination • Trial primary completion date • Combination therapy • Metastases
    |
    docetaxel • Tevimbra (tislelizumab) • irinotecan • sitravatinib (MGCD516)
    2ms
    BGB-A317-Sitra-301: Tislelizumab in Combination With Sitravatinib in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=377, Terminated, BeiGene | Completed --> Terminated; Due to safety risks and unfavorable risk-benefit assessment results, the sponsor has decided to voluntarily terminate the study.
    Trial termination • Combination therapy • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • ALK rearrangement
    |
    docetaxel • Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    2ms
    Disruption of MerTK increases the efficacy of checkpoint inhibitor by enhancing ferroptosis and immune response in hepatocellular carcinoma. (PubMed, Cell Rep Med)
    Sitravatinib, an inhibitor of MerTK, sensitizes resistant HCC to anti-PD-L1 therapy by promoting tumor ferroptosis and decreasing MDSC infiltration into the TME. In conclusion, we find that MerTK could serve as a predictive biomarker for patient stratification and as a promising target to overcome anti-PD-1/PD-L1 resistance in HCC.
    Journal • Checkpoint inhibition • PD(L)-1 Biomarker • IO biomarker
    |
    MERTK (MER Proto-Oncogene, Tyrosine Kinase) • SLC7A11 (Solute Carrier Family 7 Member 11)
    |
    MERTK expression
    |
    sitravatinib (MGCD516)
    3ms
    Sitravatinib Plus Pembrolizumab in Patients With Advanced Treatment-Naïve PD-L1+ Non-Squamous NSCLC (clinicaltrials.gov)
    P2, N=9, Terminated, Sarah Goldberg | Trial completion date: Feb 2025 --> Oct 2023 | Active, not recruiting --> Terminated | Trial primary completion date: Feb 2025 --> Jun 2023; Sponsor decision based on data from other clinical trials
    Trial completion date • Trial termination • Trial primary completion date • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • sitravatinib (MGCD516)
    3ms
    STELLAR: Tislelizumab Combined With Sitravatinib as Consolidation Treatment Following Concurrent Chemoradiation in Patients With Locally Advanced, Unresectable NSCLC (clinicaltrials.gov)
    P2, N=5, Terminated, Fudan University | N=36 --> 5 | Recruiting --> Terminated; The trial was terminated per sponsor recommendation
    Enrollment change • Trial termination • Metastases
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    3ms
    BGB-A317-Sitra-301: Tislelizumab in Combination With Sitravatinib in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=377, Completed, BeiGene | Active, not recruiting --> Completed | Trial completion date: Jun 2024 --> Dec 2023 | Trial primary completion date: Jun 2024 --> Dec 2023
    Trial completion • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • ALK rearrangement
    |
    docetaxel • Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    5ms
    A Phase 2 Study of Sitravatinib in Combination with Nivolumab in Patients with Advanced or Metastatic Urothelial Carcinoma. (PubMed, Eur Urol Oncol)
    Sitravatinib plus nivolumab demonstrated a manageable safety profile but did not result in clinically meaningful ORRs in patients with advanced/metastatic UC in the eight cohorts studied.
    P2 data • Journal • Combination therapy • Metastases
    |
    AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • MERTK (MER Proto-Oncogene, Tyrosine Kinase)
    |
    Opdivo (nivolumab) • sitravatinib (MGCD516)
    5ms
    Sitravatinib combined with PD1 blockade enhances cytotoxic T-Cell infiltration by M2 to M1 tumor macrophage repolarization in esophageal adenocarcinoma. (PubMed, Carcinogenesis)
    Additionally, pre-treatment gene expression of TAM receptors and PD-L1 were significantly higher in major responders compared to the non-responders, in animals that received sitravatinib and AUNP-12 (P < 0.02), confirming that TAM suppression enhances the efficacy of PD-1 blockade. In conclusion, this study proposes a promising immunomodulatory strategy using a multi-gene TKI to overcome developed resistance to an ICI in EAC, establishing rationale for future clinical development.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • CD8 (cluster of differentiation 8) • CASP3 (Caspase 3)
    |
    sitravatinib (MGCD516) • AUNP-12
    5ms
    BTC-BGB: Phase II Study of Sitravatinib in Combination With Tislelizumab in Patients With Advanced Biliary Tract Cancer (clinicaltrials.gov)
    P2, N=43, Active, not recruiting, Seoul National University Hospital | Trial completion date: Dec 2023 --> Jun 2024 | Trial primary completion date: Jun 2023 --> Dec 2023
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    6ms
    BGB-900-2001-IIT: A Phase II Study to Explore the Safety, Tolerability, and Preliminary Antitumor Activity of Sitravatinib Plus Tislelizumab or Combination With Nab-paclitaxel in Patients With Locally Recurrent or Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=98, Active, not recruiting, Fudan University | Completed --> Active, not recruiting | Trial completion date: Jun 2023 --> Jun 2024 | Trial primary completion date: Jun 2023 --> Jun 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER negative • PGR negative
    |
    Tevimbra (tislelizumab) • albumin-bound paclitaxel • sitravatinib (MGCD516)
    6ms
    BGB-900-2001-IIT: A Phase II Study to Explore the Safety, Tolerability, and Preliminary Antitumor Activity of Sitravatinib Plus Tislelizumab or Combination With Nab-paclitaxel in Patients With Locally Recurrent or Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=98, Completed, Fudan University | Recruiting --> Completed | Trial primary completion date: Oct 2022 --> Jun 2023
    Trial completion • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER negative • PGR negative
    |
    Tevimbra (tislelizumab) • albumin-bound paclitaxel • sitravatinib (MGCD516)
    6ms
    A Study of BGB-A445 in Combination With Other Investigational Agents in Participants With Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=100, Recruiting, BeiGene | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy
    |
    docetaxel • Tevimbra (tislelizumab) • Cyramza (ramucirumab) • sitravatinib (MGCD516) • BGB-15025 • BGB-A445
    6ms
    Study To Investigate the Efficacy and Safety of Sitravatinib in Combination With Tislelizumab in Participants With Esophageal Squamous Cell Carcinoma (clinicaltrials.gov)
    P2, N=100, Recruiting, BeiGene | Active, not recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    docetaxel • Tevimbra (tislelizumab) • irinotecan • sitravatinib (MGCD516)
    6ms
    SAPPHIRE: Phase 3 Study of Sitravatinib Plus Nivolumab vs Docetaxel in Patients With Advanced Non-Squamous Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=532, Active, not recruiting, Mirati Therapeutics Inc. | Trial completion date: Jul 2023 --> Apr 2024 | Trial primary completion date: Sep 2022 --> Mar 2023
    Trial completion date • Trial primary completion date • Combination therapy • Checkpoint inhibition • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Opdivo (nivolumab) • docetaxel • sitravatinib (MGCD516)
    6ms
    Study of Sitravatinib, Nivolumab and Ipilimumab in Advanced or Metastatic Clear-Cell Renal Cell Carcinoma or Other Solid Malignancies (clinicaltrials.gov)
    P1, N=92, Active, not recruiting, Mirati Therapeutics Inc. | Trial completion date: Jun 2023 --> Feb 2024 | Trial primary completion date: Mar 2023 --> Jun 2023
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • sitravatinib (MGCD516)
    6ms
    A Study to Evaluate the Effect of Mild, Moderate, and Severe Hepatic Impairment on Pharmacokinetics of Sitravatinib (clinicaltrials.gov)
    P1, N=30, Completed, Mirati Therapeutics Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    sitravatinib (MGCD516)
    6ms
    PK Study to Assess Drug-drug Interaction and QTc Between Sitravatinib and a Cocktail of Substrates (clinicaltrials.gov)
    P1, N=40, Completed, Mirati Therapeutics Inc. | Active, not recruiting --> Completed | Trial completion date: Dec 2023 --> Dec 2022 | Trial primary completion date: Jun 2023 --> Dec 2022
    Trial completion • Trial completion date • Trial primary completion date • Metastases
    |
    Opdivo (nivolumab) • sitravatinib (MGCD516)
    6ms
    Study To Investigate the Efficacy and Safety of Sitravatinib in Combination With Tislelizumab in Participants With Esophageal Squamous Cell Carcinoma (clinicaltrials.gov)
    P2, N=100, Active, not recruiting, BeiGene | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy • Metastases
    |
    docetaxel • Tevimbra (tislelizumab) • irinotecan • sitravatinib (MGCD516)
    7ms
    Neoadjuvant Sitravatinib in Combination With Nivolumab in Patients With Clear Cell Renal Cell Carcinoma (clinicaltrials.gov)
    P2, N=25, Completed, Mirati Therapeutics Inc. | Active, not recruiting --> Completed
    Trial completion • Combination therapy • IO biomarker • Metastases
    |
    PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD4 (CD4 Molecule) • CD27 (CD27 Molecule)
    |
    PD-L1 expression
    |
    Opdivo (nivolumab) • sitravatinib (MGCD516)
    8ms
    Sitravatinib is a potential EGFR inhibitor and induce a new death phenotype in Glioblastoma. (PubMed, Invest New Drugs)
    Our study also revealed that Sitravatinib effectively inhibited GBM invasive and induced DNA damage and cellular senescence. Furthermore, we observed a novel cell death phenotype induced by Sitravatinib, which differed from previously reported programmed death patterns such as apoptosis, pyroptosis, ferroptosis, and necrosis.
    Journal
    |
    sitravatinib (MGCD516)
    9ms
    SAPPHIRE: Phase III study of sitravatinib plus nivolumab versus docetaxel in patients with previously treated advanced non-squamous non-small cell lung cancer (NSCLC) (ESMO 2023)
    Conclusions The primary endpoint of OS was not met in pts with previously treated adv nsq NSCLC. Safety profiles for sitra/nivo and doce were consistent with prior reports for each regimen.
    Clinical • P3 data • Late-breaking abstract • Metastases
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    Opdivo (nivolumab) • docetaxel • sitravatinib (MGCD516)
    10ms
    BGB-900-2003-IIT: A Study to Investigate the Efficacy and Safety of Tislelizumab Combined With Sitravatinib as Maintenance Therapy for ES-SCLC (clinicaltrials.gov)
    P2, N=21, Recruiting, Zhejiang Cancer Hospital | N=59 --> 21 | Trial primary completion date: Dec 2024 --> Jul 2023
    Enrollment change • Trial primary completion date
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    10ms
    ITTACC: Tislelizumab in Combination With Sitravatinib for Recurrent/Metastatic Cervical Cancer After Platinum-Based Chemotherapy (clinicaltrials.gov)
    P2, N=0, Withdrawn, Australia New Zealand Gynaecological Oncology Group | N=57 --> 0 | Trial completion date: Dec 2025 --> Jun 2023 | Initiation date: Mar 2023 --> Jun 2023 | Not yet recruiting --> Withdrawn | Trial primary completion date: Dec 2025 --> Jun 2023
    Enrollment change • Trial completion date • Trial initiation date • Trial withdrawal • Trial primary completion date • Combination therapy • Metastases
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    11ms
    Sitravatinib Plus Pembrolizumab in Patients With Advanced Treatment-Naïve PD-L1+ Non-Squamous NSCLC (clinicaltrials.gov)
    P2, N=9, Active, not recruiting, Sarah Goldberg | Recruiting --> Active, not recruiting | N=70 --> 9
    Enrollment closed • Enrollment change • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • sitravatinib (MGCD516)
    11ms
    BGB-A317-Sitra-301: Tislelizumab in Combination With Sitravatinib in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=351, Recruiting, BeiGene | Active, not recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • ALK rearrangement
    |
    docetaxel • Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    11ms
    Efficacy and Safety of Sitravatinib Plus Tislelizumab or Placebo Plus Tislelizumab Versus Placebo as Adjuvant Treatment in Participants With Hepatocellular Carcinoma (clinicaltrials.gov)
    P3, N=0, Withdrawn, BeiGene | N=684 --> 0 | Not yet recruiting --> Withdrawn
    Enrollment change • Trial withdrawal
    |
    Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    12ms
    A phase II, open-label, single-arm, multi-center, prospective clinical study to investigate the efficacy and safety of tislelizumab combined with sitravatinib and docetaxel in patients with locally advanced or metastatic non-small cell lung cancer (ChiCTR2200065547)
    P2, N=43, Not yet recruiting, West China Hospital of Sichuan University
    New P2 trial • Metastases
    |
    docetaxel • Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    12ms
    Phase II trial of neoadjuvant sitravatinib plus nivolumab in patients undergoing nephrectomy for locally advanced clear cell renal cell carcinoma. (PubMed, Nat Commun)
    Correlative blood and tissue analyses showed changes in the tumour microenvironment resulting in an immunologically active tumour by the time of surgery (median time-to-surgery: 50 days). The primary endpoint of this study was not met as short-term neoadjuvant sitravatinib and nivolumab did not substantially increase ORR.
    P2 data • Journal • PD(L)-1 Biomarker • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Opdivo (nivolumab) • sitravatinib (MGCD516)
    12ms
    MODULE 6: Future Directions in the Management of Metastatic NSCLC (ASCO 2023)
    This event is organized and accredited by Research to Practice and supported through educational grants provided by AstraZeneca Pharmaceuticals LP, Daiichi Sankyo Inc, Janssen Biotech Inc, administered by Janssen Scientific Affairs LLC, Lilly, Novocure Inc, Regeneron Pharmaceuticals Inc, and Takeda Pharmaceuticals USA Inc. Biologic rationale for targeting TROP2 in lung cancer; mechanism of action of the TROP2-directed antibody-drug conjugate datopotamab deruxtecan (dato-DXd) Clinical activity observed with dato-DXd as monotherapy and in combination with other systemic anticancer therapies for advanced NSCLC; ongoing Phase III studies Incidence and severity of toxicities associated with dato-DXd, including interstitial lung disease Mechanism of action of tumor treating fields; preclinical and early clinical data supporting the investigation of this treatment modality in NSCLC Emerging positive results from the Phase III LUNAR study of tumor treating fields concurrent with immune checkpoint inhibition or docetaxel for metastatic NSCLC after failure of platinum-based therapy Potential clinical role of tumor treating fields in the care of patients with progressive NSCLC Early-phase data with anti-PD-1/PD-L1 antibodies in combination with other systemic therapies (eg, ramucirumab/pembrolizumab, lenvatinib/pembrolizumab, sitravatinib/nivolumab, durvalumab/ceralasertib) for progressive advanced NSCLC Other promising novel agents and strategies in clinical development for advanced NSCLC
    Metastases
    |
    TROP2 (Trophoblast Cell Surface Antigen 2)
    |
    Keytruda (pembrolizumab) • Opdivo (nivolumab) • Imfinzi (durvalumab) • docetaxel • Lenvima (lenvatinib) • Cyramza (ramucirumab) • ceralasertib (AZD6738) • datopotamab deruxtecan (DS-1062a) • sitravatinib (MGCD516)
    12ms
    National Lung Matrix Trial: Multi-drug Phase II Trial in Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=423, Active, not recruiting, University of Birmingham | Trial completion date: Mar 2023 --> Sep 2023 | Trial primary completion date: Mar 2023 --> Sep 2023
    Trial completion date • Trial primary completion date • IO biomarker
    |
    NKX2-1 (NK2 Homeobox 1) • TP63 (Tumor protein 63)
    |
    Xalkori (crizotinib) • Tagrisso (osimertinib) • Ibrance (palbociclib) • Imfinzi (durvalumab) • docetaxel • Koselugo (selumetinib) • Truqap (capivasertib) • fexagratinib (ABSK091) • ceralasertib (AZD6738) • sitravatinib (MGCD516) • vistusertib (AZD2014)
    1year
    BGB-A317-Sitra-301: Tislelizumab in Combination With Sitravatinib in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=351, Active, not recruiting, BeiGene | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • ALK rearrangement
    |
    docetaxel • Tevimbra (tislelizumab) • sitravatinib (MGCD516)
    1year
    Phase 1/1b Study of MGCD516 in Patients With Advanced Cancer (clinicaltrials.gov)
    P1, N=193, Completed, Mirati Therapeutics Inc. | Active, not recruiting --> Completed | Trial completion date: Dec 2022 --> Apr 2022
    Trial completion • Trial completion date • Metastases
    |
    VEGFA (Vascular endothelial growth factor A)
    |
    sitravatinib (MGCD516)
    1year
    MRTX-500 Phase 2 Trial: Sitravatinib With Nivolumab in Patients With Non-Squamous Non-Small Cell Lung Cancer Progressing On/After Checkpoint Inhibitor Therapy or Chemotherapy. (PubMed, J Thorac Oncol)
    Sitravatinib with nivolumab had a manageable safety profile. Although ORR was not met, this combination demonstrated antitumor activity and encouraging survival in CPI-experienced patients with non-squamous NSCLC.
    P2 data • Journal • Checkpoint inhibition • PD(L)-1 Biomarker
    |
    KDR (Kinase insert domain receptor)
    |
    Opdivo (nivolumab) • sitravatinib (MGCD516)
    1year
    Pembrolizumab With Sitravatinib in Recurrent Endometrial Cancer and Other Solid Tumors With Deficient Mismatch Repair System (clinicaltrials.gov)
    P2, N=0, Withdrawn, Haider Mahdi | N=30 --> 0 | Recruiting --> Withdrawn
    Enrollment change • Trial withdrawal • Mismatch repair
    |
    MLH1 (MutL homolog 1) • MSH6 (MutS homolog 6) • MSH2 (MutS Homolog 2)
    |
    MSI-H/dMMR
    |
    Keytruda (pembrolizumab) • sitravatinib (MGCD516)
    over1year
    Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia. (PubMed, Biomark Res)
    Our study reveals the potential therapeutic role of sitravatinib in FLT3 mutant AML and provides an alternative inhibitor for the treatment of AML patients who are resistant to current FLT3 inhibitors.
    Journal
    |
    FLT3 (Fms-related tyrosine kinase 3)
    |
    FLT3-ITD mutation • FLT3 mutation • FLT3 F691L • FLT3 expression • FLT3-ITD mutation + FLT3 F691L
    |
    Xospata (gilteritinib) • sitravatinib (MGCD516)
    over1year
    H-43432: Sitravatinib in Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=3, Terminated, C. Kent Osborne, MD | N=30 --> 3 | Trial completion date: Feb 2026 --> Jan 2023 | Recruiting --> Terminated | Trial primary completion date: Feb 2024 --> Jan 2023; Terminated by sponsor due to lack of interest
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • ER (Estrogen receptor) • PGR (Progesterone receptor) • PTPN12 (Protein Tyrosine Phosphatase Non-Receptor Type 12)
    |
    sitravatinib (MGCD516)
    over1year
    Tislelizumab in Combination With Sitravatinib in Patients With Locally Advanced or Metastatic Non-Small Cell Lung Cancer Tislelizumab en combinación con sitravatinib en pacientes con cáncer de pulmón no microcítico localmente avanzado o metastásico (clinicaltrialsregister.eu)
    P3, N=420, Ongoing, BeiGene, Ltd.
    New P3 trial • Combination therapy
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • EGFR mutation • BRAF mutation • ALK rearrangement • ROS1 rearrangement
    |
    docetaxel • Tevimbra (tislelizumab) • sitravatinib (MGCD516)