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    9ms
    Results from a first-in-human phase Ia/b study of LX-039, an oral selective estrogen receptor (ER) degrader (SERD), in postmenopausal patients with ER+, HER2- advanced breast cancer (ABC) (ESMO 2023)
    All pts received prior endocrine therapy (range: 1-7 lines, 56.8% fulvestrant) and/or CDK4.6i(40.9%), chemotherapy(54.5%) in the advanced setting. Conclusions LX-039 was well tolerated with preliminary anti-tumor activity in ER+, HER2- ABC. RP2D was determined at 600 mg QD and a phase II trial is being planned.
    Clinical • P1 data • Metastases
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
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    HER-2 negative
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    fulvestrant • LX-039
    1year
    A Phase I Study of LX-039 Tablets (clinicaltrials.gov)
    P1, N=44, Completed, Shandong Luoxin Pharmaceutical Group Stock Co., Ltd. | Enrolling by invitation --> Completed | N=68 --> 44 | Trial completion date: Jul 2023 --> Feb 2023
    Trial completion • Enrollment change • Trial completion date • Metastases
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive
    |
    LX-039
    2years
    Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD). (PubMed, Bioorg Med Chem Lett)
    We report herein its profound anti-tumor activity, desirable ER antagonistic characteristics combined with favorable pharmacokinetic and preliminary safety properties. LX-039 is currently in clinical trial (NCT04097756).
    Preclinical • Journal
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    ER (Estrogen receptor)
    |
    ER positive
    |
    LX-039
    4years
    A Phase I Study of LX-039 Tablets (clinicaltrials.gov)
    P1, N=68, Enrolling by invitation, Shandong Luoxin Pharmaceutical Group Stock Co., Ltd. | Not yet recruiting --> Enrolling by invitation | Initiation date: Sep 2019 --> Jan 2020
    Clinical • Enrollment open • Trial initiation date
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive
    |
    LX-039