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    DRUG:

    varlitinib (ASLAN001)

    i
    Other names: ASLAN001, ARRY 334543, ARRY-543, ARRY-334543, ASLAN-001, ASLAN 001, AR 00334543, ARRY334543, ARRY543, ARRY 543, SPS-4370, QBT-01, QBT01
    Company:
    ASLAN Pharma, Blade Entertaintment, Pfizer
    Drug class:
    EGFR inhibitor, HER2 inhibitor, HER4 inhibitor
    Related drugs:
    3ms
    Phase II Study to Assess the Efficacy of ASLAN001 Plus Capecitabine in CNS Metastases for HER2+ Breast Cancer (clinicaltrials.gov)
    P2, N=3, Terminated, National Cancer Centre, Singapore
    New P2 trial
    |
    capecitabine • varlitinib (ASLAN001)
    over1year
    Varlitinib and Paclitaxel for EGFR/HER2 Co-Expressing Advanced Gastric Cancer: a Multicenter Phase Ib/II Study (K-MASTER-13). (PubMed, Cancer Res Treat)
    No treatment-related deaths or unexpected AEs resulting from treatment cessation were observed in patients with RP2D. A combination of varlitinib and paclitaxel displayed manageable toxicity and modest antitumor activity in patients with EGFR/HER2 co-expressing AGC who progressed after first-line chemotherapy.
    P1/2 data • Journal • Metastases
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ERBB4 (erb-b2 receptor tyrosine kinase 4)
    |
    HER-2 overexpression • HER-2 expression • EGFR expression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
    |
    paclitaxel • varlitinib (ASLAN001)
    2years
    Two-Part, Phase Ib/II, Open Label, Single-Arm, Multi-center Study to Evaluate the Safety and Efficacy of Varlitinib in Combination With Weekly Paclitaxel in EGFR/HER2 Co-expressing Advanced or Metastatic Gastric Cancer Patients (clinicaltrials.gov)
    P1/2, N=27, Completed, Yonsei University | Active, not recruiting --> Completed | N=62 --> 27
    Trial completion • Enrollment change • Combination therapy • Metastases
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 amplification • HER-2 expression • EGFR amplification • EGFR expression
    |
    paclitaxel • varlitinib (ASLAN001)
    over2years
    Differential Protein Expression in Response to Varlitinib Treatment in Oral Cancer Cell Line: an In Vitro Therapeutic Approach. (PubMed, Appl Biochem Biotechnol)
    Oral cancer cells show proteome shift based on varlitinib treatment compared to corresponding controls. Our data suggest candidature of varlitinib as a potent therapeutic agent and BiP, PDIA1, HSP7C, VIME, and β-Actin as complementary/prognostic markers of OSCC.
    Preclinical • Journal
    |
    VIM (Vimentin) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5)
    |
    varlitinib (ASLAN001)
    3years
    Differences in sensitivity to new therapies between primary and metastatic breast cancer: A need to stratify the tumor response? (PubMed, Cancer Med)
    The therapeutic responses differed across tumors' locations; the magnitude of the differences of responses across the tumors' locations were drug-dependent. Stratified analysis of the response by tumor location improved drug comparisons and is a powerful tool to understand TL heterogeneity.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR positive
    |
    Herceptin (trastuzumab) • lapatinib • capecitabine • varlitinib (ASLAN001)
    over3years
    Multicenter phase Ib/II study of second-line varlitinib and paclitaxel in patients with EGFR/HER2 co-expressing advanced gastric cancer (K-MASTER-13) (ESMO 2022)
    Conclusions Varlitinib combined with paclitaxel revealed manageable toxicities and antitumor activity in patients with EGFR/HER2 co-expressing AGC who progressed after first-line chemotherapy. Updated outcomes for ongoing patients and biomarker analysis will be presented.
    Clinical • P1/2 data
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ERBB4 (erb-b2 receptor tyrosine kinase 4)
    |
    HER-2 overexpression • HER-2 expression • EGFR expression • EGFR overexpression • EGFR overexpression + HER-2 overexpression • HER-2-H
    |
    paclitaxel • varlitinib (ASLAN001)
    over3years
    Two-Part, Phase Ib/II, Open Label, Single-Arm, Multi-center Study to Evaluate the Safety and Efficacy of Varlitinib in Combination With Weekly Paclitaxel in EGFR/HER2 Co-expressing Advanced or Metastatic Gastric Cancer Patients (clinicaltrials.gov)
    P1/2, N=62, Active, not recruiting, Yonsei University
    New P1/2 trial • Combination therapy
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 amplification • HER-2 expression • EGFR amplification • EGFR expression
    |
    paclitaxel • varlitinib (ASLAN001)
    over3years
    Phase Ib Dose-Finding Study of Varlitinib Combined with Weekly Paclitaxel With or Without Carboplatin ± Trastuzumab in Advanced Solid Tumors. (PubMed, Target Oncol)
    The recommended phase II dose of varlitinib with paclitaxel is 300 mg twice daily intermittently dosed. This is active in HER2+ metastatic breast cancer. Subcutaneous trastuzumab can be added safely to varlitinib and paclitaxel. This combination is currently being evaluated as neoadjuvant therapy in HER2+ breast cancer (NCT02396108).
    P1 data • Clinical Trial,Phase I • Journal
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ERBB4 (erb-b2 receptor tyrosine kinase 4)
    |
    carboplatin • paclitaxel • varlitinib (ASLAN001) • Herceptin Hylecta (trastuzumab/hyaluronidase-oysk)
    almost4years
    Varlitinib in Combination With mFOLFOX6 for Advanced or Metastatic Gastric Cancer (First Line) (clinicaltrials.gov)
    P2/3, N=52, Completed, Aslan Pharmaceuticals | Active, not recruiting --> Completed | N=400 --> 52
    Trial completion • Enrollment change • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 overexpression • HER-2 amplification
    |
    oxaliplatin • varlitinib (ASLAN001)
    almost4years
    Varlitinib plus capecitabine in second-line advanced biliary tract cancer: a randomized, phase II study (TreeTopp). (PubMed, ESMO Open)
    In patients with advanced biliary tract cancer, second-line treatment with varlitinib plus capecitabine was well tolerated but did not improve efficacy versus capecitabine alone. A PFS benefit was suggested in female patients and those with gallbladder cancer.
    Clinical • P2 data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    gemcitabine • capecitabine • varlitinib (ASLAN001)
    4years
    Upregulation of the ErbB family by EZH2 in hepatocellular carcinoma confers resistance to FGFR inhibitor. (PubMed, J Cancer Res Clin Oncol)
    The upregulation of the ErbB family by EZH2 appears to contribute to infigratinib resistance. The combination of infigratinib and varlitinib showed a potent antitumour effect and did not result in additional toxicity, warranting further clinical investigation.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
    |
    EZH2 overexpression
    |
    Truseltiq (infigratinib) • varlitinib (ASLAN001)