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    DRUG:

    LOXO-783

    i
    Other names: LOXO 783, LOXO783, LOXO-783, LOX-22783, LY3849524
    Company:
    Eli Lilly
    Drug class:
    PI3Kα H1047R mutation inhibitor
    Related drugs:
    4ms
    PIKASSO-01: A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors (clinicaltrials.gov)
    P1, N=193, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting | N=400 --> 193
    Enrollment closed • Enrollment change • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation • PIK3CA H1047R
    |
    paclitaxel • Verzenio (abemaciclib) • fulvestrant • letrozole • anastrozole • exemestane • imlunestrant (LY3484356) • LOXO-783
    5ms
    A Study of [14C]-LOXO-783 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=16, Completed, Eli Lilly and Company | Not yet recruiting --> Completed
    Trial completion
    |
    LOXO-783
    5ms
    A Study to Evaluate the Effect of Food on LOXO-783 in Healthy Participants (clinicaltrials.gov)
    P1, N=42, Completed, Eli Lilly and Company | Recruiting --> Completed
    Trial completion
    |
    LOXO-783
    1year
    A Study of [14C]-LOXO-783 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=16, Not yet recruiting, Eli Lilly and Company
    New P1 trial
    |
    LOXO-783
    over1year
    PIKASSO-01: A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors (clinicaltrials.gov)
    P1, N=400, Recruiting, Eli Lilly and Company | N=300 --> 400
    Enrollment change • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation • PIK3CA H1047R
    |
    paclitaxel • Verzenio (abemaciclib) • fulvestrant • letrozole • anastrozole • exemestane • imlunestrant (LY3484356) • LOXO-783
    2years
    A phase 1 trial of LOXO-783, a potent, highly mutant-selective, brain-penetrant allosteric PI3Kα H1047R inhibitor in PIK3CA H1047R-mutant advanced breast cancer (aBC) and other solid tumors (PIKASSO-01, trial in progress) (SABCS 2022)
    Table. Dose Expansion (Phase 1b)
    P1 data
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation • PIK3CA H1047R
    |
    LOXO-783
    2years
    LOXO-783: A potent, highly mutant selective and brain-penetrant allosteric PI3Kα H1047R inhibitor in combination with standard of care (SOC) treatments in preclinical PI3Kα H1047R-mutant breast cancer models (SABCS 2022)
    Results Combining LOXO-783 with either fulvestrant (FUL; CI at 50% inhibition = 0.28) or imlunestrant (CI at 50% inhibition = 0.43) showed increased efficacy in cell proliferation assays using the HR+, HER2-, PI3Kα H1047R- mutant T47D model...Similar results were observed in a T47D model engineered to express ESR1 D538G, as well as in an HR+, HER2- PI3Kα double in-cis mutant model (H1047R/D350G) also harboring ESR1 D538G and derived from a patient who had progressed on prior letrozole plus taselisib...Extending these studies to additional treatment settings, LOXO-783 was similarly efficacious as a single agent in abemaciclib-resistant and abemaciclib/FUL double-resistant models, and was additive in combination with paclitaxel in a triple negative breast cancer model in vitro and in vivo...LOXO-783 is also efficacious in ESR1 mutant as well as in abemaciclib and abemaciclib/FUL double-resistant models. A phase 1 trial of LOXO-783 alone or in combination with anticancer therapies is ongoing (PIKASSO-01; NCT05307705).
    Preclinical • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation • PIK3CA H1047R • ER D538G • ESR1 mutation • PIK3CA D350G
    |
    paclitaxel • Verzenio (abemaciclib) • fulvestrant • letrozole • taselisib (GDC-0032) • imlunestrant (LY3484356) • LOXO-783
    over2years
    A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors (clinicaltrials.gov)
    P1, N=260, Recruiting, Eli Lilly and Company | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation • PIK3CA H1047R
    |
    paclitaxel • Verzenio (abemaciclib) • fulvestrant • letrozole • anastrozole • exemestane • imlunestrant (LY3484356) • LOXO-783
    over2years
    A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors (clinicaltrials.gov)
    P1, N=260, Not yet recruiting, Eli Lilly and Company
    New P1 trial • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation • PIK3CA H1047R
    |
    paclitaxel • Verzenio (abemaciclib) • fulvestrant • letrozole • anastrozole • exemestane • imlunestrant (LY3484356) • LOXO-783