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    DRUG:

    serabelisib (MLN1117)

    i
    Other names: MLN1117, MLN-1117, INK-1117, TAK-117, PETRA 06, PETRA-06, INK1117, TAK 117, INK 1117, MLN 1117, PETRA06, TAK117, FTH-001, FTH001, FTH 001
    Associations

    News

    Trials
    Company:
    Eli Lilly, Faeth Therap, Takeda
    Drug class:
    PI3Kα inhibitor
    Related drugs:
    Associations

    News

    Trials
    27d
    PI3K inhibitors: Efficacy in diverse cancer forms. (PubMed, Cancer Treat Res Commun)
    The PI3K inhibitors GDC-0032 and INK1117 for PI3K-α and AZD8186 for PI3K-β are now being studied in clinical trials. Research on the clinical development, therapeutic utility, and structural insights of new PI3K inhibitors is the main emphasis of this review. The inhibitors have been shown promising anticancer activity relationships.
    Review • Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
    |
    taselisib (GDC-0032) • AZD8186 • serabelisib (MLN1117)
    2ms
    Combination of Serabelisib and Insulin Suppressing Diet With or Without Nab-paclitaxel in Subjects With Advanced Solid Tumors With PIK3CA Mutations (clinicaltrials.gov)
    P1, N=34, Completed, Faeth Therapeutics | Active, not recruiting --> Completed | N=68 --> 34 | Trial completion date: Dec 2025 --> Apr 2025 | Trial primary completion date: Dec 2025 --> Apr 2025
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    albumin-bound paclitaxel • serabelisib (MLN1117)
    7ms
    Multi-node inhibition targeting mTORC1, mTORC2 and PI3Kα potently inhibits the PI3K/AKT/mTOR pathway in endometrial and breast cancer models. (PubMed, Br J Cancer)
    Multi-node PI3K/AKT/mTOR pathway inhibition with serabelisib, sapanisertib and ISD is highly effective in preclinical models of endometrial and breast cancer, supporting continued clinical development in these and other solid tumours.
    Preclinical • Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
    |
    paclitaxel • everolimus • Piqray (alpelisib) • Truqap (capivasertib) • sapanisertib (CB-228) • RLY-2608 • Itovebi (inavolisib) • LY4064809 • serabelisib (MLN1117)
    9ms
    Combination of Serabelisib and Insulin Suppressing Diet with or Without Nab-paclitaxel in Subjects with Advanced Solid Tumors with PIK3CA Mutations (clinicaltrials.gov)
    P1, N=68, Active, not recruiting, Faeth Therapeutics | Trial completion date: Sep 2024 --> Dec 2025 | Trial primary completion date: Sep 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    albumin-bound paclitaxel • serabelisib (MLN1117)
    12ms
    Sapanisertib and Serabelisib (PIKTOR) With Paclitaxel and a Substudy With Diet in Patients With Advanced/Recurrent Endometrial Cancer (clinicaltrials.gov)
    P2, N=40, Recruiting, Faeth Therapeutics | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    paclitaxel • sapanisertib (CB-228) • serabelisib (MLN1117)
    1year
    Sapanisertib and Serabelisib (PIKTOR) With Paclitaxel and a Substudy With Diet in Patients With Advanced/Recurrent Endometrial Cancer (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Faeth Therapeutics | N=120 --> 40 | Initiation date: Sep 2024 --> Dec 2024
    Enrollment change • Trial initiation date • Metastases
    |
    paclitaxel • sapanisertib (CB-228) • serabelisib (MLN1117)
    1year
    Enhancing immunotherapy through PD-L1 upregulation: the promising combination of anti-PD-L1 plus mTOR inhibitors. (PubMed, Mol Oncol)
    In our study, we investigated how phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway inhibitors (TAK-228, everolimus and TAK-117) affect PD-L1 expression and function in preclinical bladder cancer cell models. These preclinical findings suggest that mTOR inhibition with TAK-228 can increase PD-L1 levels, potentially impacting the specific immune response against UC cells. This highlights the rationale for exploring the combination of mTOR inhibitors with ICIs in patients with advanced UC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • EGF (Epidermal growth factor) • IFNB1 (Interferon Beta 1)
    |
    PD-L1 expression • IFNG expression
    |
    everolimus • sapanisertib (CB-228) • serabelisib (MLN1117)
    over1year
    Design, synthesis and bioevaluation of dual EGFR-PI3Kα inhibitors for potential treatment of NSCLC. (PubMed, Bioorg Chem)
    A series of dual EGFR/PI3Kα inhibitors was synthesized using pharmacophore hybridization of the third-generation EGFR inhibitor olmutinib and the PI3Kα selective inhibitor TAK-117. Compound 30k exhibited a significant antiproliferative effect in NCI-H1975 cells with a higher selectivity profile than olmutinib. The potential antitumor mechanism, molecular binding modes, and in vitro metabolic stability of compound 30k were also clarified.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    Olita (olmutinib) • serabelisib (MLN1117)
    over1year
    X31025: Evaluation of the Safety and Tolerability of TAK-228 With TAK-117 and Paclitaxel in Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=19, Completed, Avera McKennan Hospital & University Health Center | Active, not recruiting --> Completed | N=30 --> 19
    Trial completion • Enrollment change • Combination therapy • Metastases
    |
    PI3K (Phosphoinositide 3-kinases)
    |
    paclitaxel • sapanisertib (CB-228) • serabelisib (MLN1117)
    over1year
    Sapanisertib and Serabelisib (PIKTOR) With Paclitaxel, Serabelisib With Paclitaxel, and Paclitaxel Alone in Patients With Advanced/Recurrent Endometrial Cancer (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Faeth Therapeutics
    New P2 trial • Metastases
    |
    paclitaxel • sapanisertib (CB-228) • serabelisib (MLN1117)
    almost2years
    Combination of Serabelisib and Insulin Suppressing Diet With or Without Nab-paclitaxel in Subjects With Advanced Solid Tumors With PIK3CA Mutations (clinicaltrials.gov)
    P1, N=68, Active, not recruiting, Faeth Therapeutics | Recruiting --> Active, not recruiting | Phase classification: P1b --> P1
    Enrollment closed • Phase classification • Combination therapy • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    albumin-bound paclitaxel • serabelisib (MLN1117)
    2years
    Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs. (PubMed, Eur J Med Chem)
    In this study, we have designed and synthesized three series of substituted benzoxazole derivatives based on the clinical candidate TAK-117 (8a)...The potential antitumor mechanism and in vitro metabolic stability of 18a were also investigated. Notably, pharmacokinetic assays indicated that 18a had a higher plasma exposure, a higher maximum concentration and shorter elimination time compared to 8a.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    serabelisib (MLN1117)