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    DRUG:

    tersolisib (LY4064809)

    i
    Other names: LY4064809, STX-478, ST-814, LY-4064809, STX-H1047-PI3Kα
    Company:
    Eli Lilly
    Drug class:
    PI3Kα H1047R mutation inhibitor
    Related drugs:
    16d
    Benzothiophene-based, orally active PIK3CA H1047R mutant-selective inhibitors for the treatment of HR+/HER2- breast cancer. (PubMed, Eur J Med Chem)
    Although two orthosteric PI3Kα inhibitors including Alpelisib and Inavolisib have been launched onto market, they often cause toxic and side effects due to insufficient selectivity for PIK3CA mutant protein...Our research focuses on optimizing a novel series of allosteric PI3Kα inhibitors derived from STX-478...The inhibitor demonstrates high selectivity for PIK3CA mutant protein, low hERG inhibition, minimal CYP inhibition, excellent in vivo efficacy, good safety and no impact on insulin balance. Collectively, these findings confirm that compound 11f is a highly promising drug candidate for the targeted therapy of PIK3CA H1047R mutant HR+/HER2-breast cancer.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation
    |
    Piqray (alpelisib) • Itovebi (inavolisib) • tersolisib (LY4064809)
    17d
    PIKALO-1: First-in-Human Study of Tersolisib (STX-478) as Monotherapy and in Combination With Other Antineoplastic Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=880, Recruiting, Eli Lilly and Company | N=178 --> 880
    Enrollment change • First-in-human
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • letrozole • anastrozole • exemestane • metformin • Inluriyo (imlunestrant) • tersolisib (LY4064809) • Soltamox (tamoxifen citrate)
    20d
    A Study of LY4064809 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=24, Completed, Eli Lilly and Company | Active, not recruiting --> Completed
    Trial completion
    |
    tersolisib (LY4064809)
    23d
    PIKALO-2: A Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA) (clinicaltrials.gov)
    P3, N=920, Recruiting, Eli Lilly and Company | N=274 --> 920
    Enrollment change • Trial initiation date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor)
    |
    ER positive • PIK3CA mutation • PGR positive
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • letrozole • anastrozole • exemestane • tersolisib (LY4064809)
    1m
    A Study of [14C]-LY4064809 in Healthy Participants (clinicaltrials.gov)
    P1, N=8, Recruiting, Eli Lilly and Company
    New P1 trial
    |
    tersolisib (LY4064809)
    1m
    PIKALO-2: A Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA) (clinicaltrials.gov)
    P3, N=193, Recruiting, Eli Lilly and Company
    New P3 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor)
    |
    ER positive • PIK3CA mutation • PGR positive
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • letrozole • anastrozole • exemestane • tersolisib (LY4064809)
    2ms
    J6M-MC-JSGD: A Study of LY4064809 With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA) (2025-522791-92-00)
    P2/3, N=36, Not yet recruiting, Eli Lilly & Co.
    New P2/3 trial
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    ER positive • PIK3CA mutation
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • letrozole • anastrozole • exemestane • tersolisib (LY4064809)
    2ms
    A Study of LY4064809 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=24, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    tersolisib (LY4064809)
    4ms
    A Study of LY4064809 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=24, Recruiting, Eli Lilly and Company | Not yet recruiting --> Recruiting
    Enrollment open
    |
    tersolisib (LY4064809)
    4ms
    A Study of LY4064809 in Healthy Adult Chinese Participants (clinicaltrials.gov)
    P1, N=10, Completed, Eli Lilly and Company | Active, not recruiting --> Completed
    Trial completion
    |
    tersolisib (LY4064809)
    4ms
    A Study of LY4064809 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, Eli Lilly and Company
    New P1 trial
    |
    tersolisib (LY4064809)
    5ms
    A Study of LY4064809 in Healthy Adult Chinese Participants (clinicaltrials.gov)
    P1, N=10, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    tersolisib (LY4064809)