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    DRUG:

    izorlisib (MEN1611)

    i
    Other names: MEN1611, CH5132799, PA799, MEN-1611, MEN 1611, CH 5132799, PA-799, CH-5132799, PA 799
    Company:
    Menarini, Roche
    Drug class:
    PI3K inhibitor
    Related drugs:
    2ms
    SABINA: PIK3CA/PTEN-altered Advanced Breast Cancer Treated With MEN1611 Monotherapy or in Combination With Eribulin (clinicaltrials.gov)
    P2, N=14, Recruiting, MedSIR | Trial primary completion date: Jul 2025 --> Apr 2026
    Trial primary completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    Halaven (eribulin mesylate) • izorlisib (MEN1611)
    12ms
    SABINA: PIK3CA/PTEN-altered Advanced Breast Cancer Treated With MEN1611 Monotherapy or in Combination With Eribulin (clinicaltrials.gov)
    P2, N=14, Recruiting, MedSIR | N=28 --> 14
    Enrollment change • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    Halaven (eribulin mesylate) • izorlisib (MEN1611)
    over1year
    B-PRECISE-01: MEN1611 With Trastuzumab (+/- Fulvestrant) in Metastatic Breast Cancer (clinicaltrials.gov)
    P1, N=62, Completed, Menarini Group | Active, not recruiting --> Completed
    Trial completion • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Herceptin (trastuzumab) • fulvestrant • izorlisib (MEN1611)
    over1year
    MEN1611 With Cetuximab in Metastatic Colorectal Cancer (C-PRECISE-01) (clinicaltrials.gov)
    P1/2, N=29, Completed, Menarini Group | Active, not recruiting --> Completed | Trial completion date: Jun 2024 --> Feb 2024 | Trial primary completion date: Jun 2024 --> Jan 2024
    Trial completion • Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • RAS (Rat Sarcoma Virus)
    |
    BRAF mutation • PIK3CA mutation • BRAF wild-type
    |
    Erbitux (cetuximab) • 5-fluorouracil • oxaliplatin • irinotecan • izorlisib (MEN1611)
    almost2years
    MEN1611 With Cetuximab in Metastatic Colorectal Cancer (C-PRECISE-01) (clinicaltrials.gov)
    P1/2, N=29, Active, not recruiting, Menarini Group | Trial completion date: Dec 2023 --> Jun 2024 | Trial primary completion date: Dec 2023 --> Jun 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • RAS (Rat Sarcoma Virus)
    |
    BRAF mutation • PIK3CA mutation • BRAF wild-type
    |
    Erbitux (cetuximab) • 5-fluorouracil • oxaliplatin • irinotecan • izorlisib (MEN1611)
    2years
    The activity of a PI3K δ-sparing inhibitor, MEN1611, in non-small cell lung cancer cells with constitutive activation of the PI3K/AKT/mTOR pathway. (PubMed, Front Oncol)
    We demonstrated good efficacy of MEN1611 in NSCLC devoid of PIK3CA gene mutations but with constitutive activation of the PI3K/AKT pathway and its synergistic effect with gefitinib both in vitro and in vivo. Overall, this preclinical study indicates that the inhibitor could be a candidate for the treatment of NSCLC with an erlotinib/gefitinib-resistant phenotype and constitutive activation of the PI3K/AKT pathway, a phenotype mimicked by our model system.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    EGFR mutation • PIK3CA mutation
    |
    erlotinib • gefitinib • izorlisib (MEN1611)
    over2years
    MEN1611 With Cetuximab in Metastatic Colorectal Cancer (C-PRECISE-01) (clinicaltrials.gov)
    P1/2, N=29, Active, not recruiting, Menarini Group | N=42 --> 29
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • RAS (Rat Sarcoma Virus)
    |
    BRAF mutation • PIK3CA mutation • BRAF wild-type
    |
    Erbitux (cetuximab) • 5-fluorouracil • oxaliplatin • irinotecan • izorlisib (MEN1611)
    over2years
    SABINA: PIK3CA/PTEN-altered Advanced Breast Cancer Treated With MEN1611 Monotherapy or in Combination With Eribulin (clinicaltrials.gov)
    P2, N=28, Recruiting, MedSIR | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    Halaven (eribulin mesylate) • izorlisib (MEN1611)
    over2years
    B-PRECISE-01: MEN1611 With Trastuzumab (+/- Fulvestrant) in Metastatic Breast Cancer (clinicaltrials.gov)
    P1, N=62, Active, not recruiting, Menarini Group | Trial completion date: Jul 2022 --> Dec 2023 | Trial primary completion date: Jul 2022 --> Dec 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Herceptin (trastuzumab) • fulvestrant • izorlisib (MEN1611)
    over2years
    Antitumor activity of the PI3K δ-sparing inhibitor MEN1611 in PIK3CA mutated, trastuzumab-resistant HER2 + breast cancer. (PubMed, Breast Cancer Res Treat)
    The profile of MEN1611 and its antitumoral activity suggest an improved profile as compared to pan-inhibitors, which are limited by a less than ideal safety profile, and isoform selective molecules, which may potentially promote development of resistance mechanisms. The compelling antitumor activity in combination with trastuzumab in HER2 + trastuzumab-resistant, PIK3CA mutated breast cancer models is at the basis of the ongoing B-Precise clinical trial (NCT03767335).
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Herceptin (trastuzumab) • Piqray (alpelisib) • taselisib (GDC-0032) • izorlisib (MEN1611)
    over2years
    MEN1611 With Cetuximab in Metastatic Colorectal Cancer (C-PRECISE-01) (clinicaltrials.gov)
    P1/2, N=42, Active, not recruiting, Menarini Group | Recruiting --> Active, not recruiting | Trial completion date: Jul 2023 --> Oct 2023 | Trial primary completion date: Jul 2023 --> Oct 2023
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • RAS (Rat Sarcoma Virus)
    |
    BRAF mutation • PIK3CA mutation • BRAF wild-type
    |
    Erbitux (cetuximab) • 5-fluorouracil • oxaliplatin • irinotecan • izorlisib (MEN1611)
    over2years
    SABINA: PIK3CA/PTEN-altered Advanced Breast Cancer Treated With MEN1611 Monotherapy or in Combination With Eribulin (clinicaltrials.gov)
    P2, N=28, Not yet recruiting, MedSIR
    New P2 trial • Combination therapy • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    PIK3CA mutation
    |
    Halaven (eribulin mesylate) • izorlisib (MEN1611)