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    5ms
    Preclinical pharmacokinetic characterization of amdizalisib, a novel PI3Kδ inhibitor for the treatment of hematological malignancies. (PubMed, Front Pharmacol)
    It exhibited induction potential on CYP1A2, CYP2B6, CYP3A4, and CYP2C9. The preclinical data from these ADME studies demonstrate a favorable pharmacokinetic profile for amdizalisib, which is expected to support the future clinical development of amdizalisib as a promising anti-cancer agent.
    PK/PD data • Preclinical • Journal
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    PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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    amdizalisib (HMPL-689)
    9ms
    Trial to Evaluate the Safety and Pharmacokinetics of HMPL-689 in Patients With Lymphomas (clinicaltrials.gov)
    P1, N=53, Active, not recruiting, Hutchmed | Trial completion date: Aug 2023 --> Dec 2024 | Trial primary completion date: Aug 2023 --> Jul 2024
    Trial completion date • Trial primary completion date
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    amdizalisib (HMPL-689)
    over1year
    UPDATED RESULTS FROM A PHASE 1B STUDY OF AMDIZALISIB, A NOVEL INHIBITOR OF PHOSPHOINOSITIDE 3-KINASE-DELTA (PI3Kδ), IN PATIENTS WITH RELAPSED OR REFRACTORY LYMPHOMA (ICML 2023)
    Amdizalisib showed an acceptable safety profile and promising anti-tumor activity in R/R lymphoma, providing evidence for future investigations. Clinical trial information: NCT03128164.
    Clinical • P1 data
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    PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta)
    |
    amdizalisib (HMPL-689)
    over2years
    Amdizalisib (HMPL-689), a highly selective PI3Kδ inhibitor, exhibits potent anti-tumor activity in pre-clinical B-cell lymphoma models (AACR 2022)
    Human B cell lymphoma cell line derived xenograft models were used to determine the anti-tumor activity of Amdiz in combination with other agents such as rituximab, BTK inhibitor, and venetoclax. Amdiz is a highly selective inhibitor of PI3Kδ, showing more than 250-fold selectivity over other PI3K isoforms and no significant inhibition over other 319 protein kinases at the concentration of 1 µM. Amdiz is a highly potent and selective PI3Kδ inhibitor with strong activity against B-cell lymphoma in pre-clinical studies, supporting clinical evaluation as either a single agent or in combination with other therapeutic agents for the treatment of B-cell malignancies.
    Preclinical
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    PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CD86 (CD86 Molecule)
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    Venclexta (venetoclax) • Rituxan (rituximab) • amdizalisib (HMPL-689)
    over3years
    [VIRTUAL] A phase Ib study result of HMPL-689, a PI3Kδ inhibitor, in Chinese patients with relapsed/refractory lymphoma (ESMO 2021)
    HMPL-689 showed tolerable safety profile and promising single-agent clinical activity in pts with R/R B-cell lymphoma, with high ORR and CR rates noted particularly for FL patients.
    Clinical • P1 data
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    PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta)
    |
    amdizalisib (HMPL-689)