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    DRUG:

    BLU-222

    i
    Other names: BLU-222, BLU222, BLU 222
    Company:
    Blueprint Medicines, UT MD Anderson Cancer Center
    Drug class:
    CDK2 inhibitor
    Related drugs:
    over2years
    A first-in-human phase I/II study of BLU-222, a potent, selective CDK2 inhibitor in patients with CCNE1-amplified or CDK4/6 inhibitor-resistant advanced solid tumors (ESMO 2022)
    Preclinically, BLU-222 has shown potent CDK2 inhibition and antitumor activity, and combination with carboplatin/paclitaxel led to significant tumor regression. Phase II dose expansion: part 2A (CCNE1-amplified tumors including EC [≥2 prior therapies], platinum-resistant/refractory OC, or other advanced solid tumors [progression on SOC]; BLU-222], part 2B and 2D (CDK4/6i-resistant ER+HER2- BC; BLU-222 and fulvestrant with/without ribociclib), part 2C (CCNE1-amplified platinum-resistant/refractory OC; BLU-222 and carboplatin). Approximately 50 sites are anticipated to enroll patients across North America, Europe, and Asia/Pacific.
    Clinical • P1/2 data
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CCNE1 (Cyclin E1)
    |
    ER positive • HER-2 negative • CCNE1 amplification • CDK4 amplification • CCNE1 expression
    |
    carboplatin • paclitaxel • Kisqali (ribociclib) • fulvestrant • BLU-222
    over2years
    (VELA) Study of BLU-222 in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=366, Recruiting, Blueprint Medicines Corporation | Trial completion date: Dec 2025 --> Sep 2026
    Trial completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • RB1 (RB Transcriptional Corepressor 1) • CCNE1 (Cyclin E1)
    |
    HER-2 negative • CCNE1 amplification
    |
    carboplatin • Kisqali (ribociclib) • fulvestrant • BLU-222
    over2years
    BLU-222, an investigational, potent, and selective CDK2 inhibitor, demonstrated robust antitumor activity in CCNE1-amplified ovarian cancer models (AACR 2022)
    These data provide a strong rationale for advancing BLU-222 towards clinical development in patients with CCNE1-amplified ovarian cancer.
    Preclinical
    |
    CCNE1 (Cyclin E1) • CDK1 (Cyclin-dependent kinase 1)
    |
    CCNE1 amplification • CCNE1 overexpression
    |
    carboplatin • BLU-222
    over2years
    (VELA) Study of BLU-222 in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=366, Recruiting, Blueprint Medicines Corporation
    New P1/2 trial • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • RB1 (RB Transcriptional Corepressor 1) • CCNE1 (Cyclin E1)
    |
    HER-2 negative • CCNE1 amplification
    |
    carboplatin • Kisqali (ribociclib) • fulvestrant • BLU-222