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    DRUG:

    LNS8801

    i
    Other names: LNS8801, LNS-8801, LNS 8801
    Associations

    News

    Trials
    Company:
    Linnaeus Therap
    Drug class:
    GPER agonist
    Associations

    News

    Trials
    6ms
    A Trial of LNS8801 With or Without Pembrolizumab in Patients With Refractory Melanoma (clinicaltrials.gov)
    P2/3, N=135, Recruiting, Linnaeus Therapeutics, Inc. | Not yet recruiting --> Recruiting | Trial completion date: Aug 2030 --> Feb 2031 | Initiation date: Nov 2024 --> Aug 2025 | Trial primary completion date: Aug 2028 --> Feb 2029
    Enrollment open • Trial completion date • Trial initiation date • Trial primary completion date
    |
    Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • temozolomide • dacarbazine • relatlimab (BMS-986016) • LNS8801
    12ms
    LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development. (PubMed, Cancer Res Commun)
    In addition, an attenuated response to LNS8801 is observed in a common germline coding variant in human GPER. These findings support ongoing human cancer trials with LNS8801 and suggest that the germline GPER genotype may serve as a predictive biomarker of therapeutic response.
    Journal
    |
    ER (Estrogen receptor)
    |
    LNS8801
    1year
    KEYNOTE-B47: Study Assessing MTD, Safety, Tolerability, PK and Anti-tumor Effects of LNS8801alone and with Pembrolizumab (clinicaltrials.gov)
    P1/2, N=200, Recruiting, Linnaeus Therapeutics, Inc. | Trial completion date: Dec 2024 --> Dec 2027 | Trial primary completion date: Mar 2024 --> Dec 2026
    Trial completion date • Trial primary completion date • IO biomarker • Metastases
    |
    PD-L1 (Programmed death ligand 1) • MYC (V-myc avian myelocytomatosis viral oncogene homolog)
    |
    PD-L1 expression
    |
    Keytruda (pembrolizumab) • LNS8801
    1year
    LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development. (PubMed, bioRxiv)
    In addition, an attenuated response to LNS8801 is observed in a common germline coding variant in human GPER. These findings support ongoing human cancer trials with LNS8801 and suggest that the germline GPER genotype may serve as a predictive biomarker of therapeutic response.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER expression
    |
    LNS8801
    over1year
    A Trial of LNS8801 with or Without Pembrolizumab in Patients with Refractory Melanoma (clinicaltrials.gov)
    P2/3, N=135, Not yet recruiting, Linnaeus Therapeutics, Inc. | Phase classification: P3 --> P2/3
    Phase classification
    |
    Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • temozolomide • dacarbazine • relatlimab (BMS-986016) • LNS8801
    over1year
    Effect of LNS8801 (with or Without Pembrolizumab) on Melanoma (clinicaltrials.gov)
    P3, N=135, Not yet recruiting, Linnaeus Therapeutics, Inc.
    New P3 trial
    |
    Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • temozolomide • dacarbazine • relatlimab (BMS-986016) • LNS8801
    over2years
    LNS8801 inhibits Acute Myeloid Leukemia by Inducing the Production of Reactive Oxygen Species and Activating the Endoplasmic Reticulum Stress Pathway. (PubMed, Cancer Res Commun)
    Previous work demonstrated that LNS8801 inhibits cancer via GPER activation, especially in solid tumors. Here we show that LNS8801 inhibits AML via GPER-independent mechanisms that include ROS induction and ER activation.
    Journal
    |
    LNS8801
    over2years
    The effect of LNS8801 in combination with pembrolizumab in patients with treatment-refractory cutaneous melanoma (ESMO 2023)
    Consensus germline GPER is a promising predictive biomarker, and is associated with improved outcomes in patients treated with LNS8801. These data support further development of LNS8801 in combination with pembrolizumab treat advanced CM patients.
    Clinical • Combination therapy • PD(L)-1 Biomarker • IO biomarker
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • PD-1 (Programmed cell death 1) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4)
    |
    Keytruda (pembrolizumab) • LNS8801
    almost3years
    The GPER Agonist LNS8801 Induces Mitotic Arrest and Apoptosis in Uveal Melanoma Cells. (PubMed, Cancer Res Commun)
    Here, we demonstrate that the GPER agonist LNS8801 induced both GPER-dependent and GPER-independent effects and elicited potent anticancer activities in vitro and in vivo. Our results complement and support the ongoing clinical trial of LNS8801 in advanced uveal melanoma.
    Journal
    |
    TP53 (Tumor protein P53) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • GPER1 (G Protein-Coupled Estrogen Receptor 1)
    |
    TP53 expression
    |
    LNS8801
    almost3years
    Study Assessing MTD, Safety, Tolerability, PK and Anti-tumor Effects of LNS8801alone and With Pembrolizumab (clinicaltrials.gov)
    P1/2, N=200, Recruiting, Linnaeus Therapeutics, Inc. | Trial primary completion date: Oct 2023 --> Mar 2024
    Trial primary completion date • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    Keytruda (pembrolizumab) • LNS8801
    almost4years
    Study Assessing MTD, Safety, Tolerability, PK and Anti-tumor Effects of LNS8801alone and With Pembrolizumab (clinicaltrials.gov)
    P1/2, N=200, Recruiting, Linnaeus Therapeutics, Inc. | Trial completion date: Nov 2023 --> Nov 2024 | Trial primary completion date: Oct 2022 --> Oct 2023
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase)
    |
    PD-L1 expression • ALK positive • ALK mutation
    |
    Keytruda (pembrolizumab) • LNS8801