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    3ms
    Predict the Drug-Drug Interaction of a Novel PI3Kα/δ Inhibitor, TQ-B3525, and Its Two Metabolites Using Physiologically Based Pharmacokinetic Modeling. (PubMed, J Clin Pharmacol)
    Models involving rifampicin combined with midazolam, itraconazole combined with midazolam or digoxin were utilized to showcase the robustness of evaluating DDI effects. PBPK model simulation results showed that the systemic exposure of TQ-B3525 was significantly affected when co-administered with CYP3A4/P-gp inducers and inhibitors. This indicates that the combination with strong inducers and inhibitors should be carefully avoided or adjust the dosage of TQ-B3525 in clinic.
    PK/PD data • Journal
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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    itraconazole • TQ-B3525 • midazolam hydrochloride • rifampicin
    5ms
    Preclinical evaluation and phase 1 study of the PI3Kα/δ inhibitor TQ-B3525 in Chinese patients with advanced cancers. (PubMed, Cancer)
    TQ-B3525 exhibited rapid absorption and a nearly proportional increase in exposure. Acceptable safety and promising efficacy support further investigation of TQ-B3525 (20 mg once daily) for R/R lymphoma.
    P1 data • Preclinical • Journal • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    TQ-B3525
    6ms
    Recent advances in treatment of follicular lymphoma: efficacy of PI3Kα/δ inhibitor (TQ-B3525). (PubMed, Signal Transduct Target Ther)
    No abstract available
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    TQ-B3525
    7ms
    Phase II study of novel orally PI3Kα/δ inhibitor TQ-B3525 in relapsed and/or refractory follicular lymphoma. (PubMed, Signal Transduct Target Ther)
    Grade 3 or higher treatment-related adverse events were observed in 63 (76.8%) cases, with neutropenia (22.0%), hyperglycemia (19.5%), and diarrhea (13.4%) being common. TQ-B3525 showed favorable efficacy and safety for R/R FL patients after ≥2 lines prior therapies.
    P2 data • Journal
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    TQ-B3525
    12ms
    A Study of TQ-B3525 in Subjects With Relapsed/Refractory Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (clinicaltrials.gov)
    P1/2, N=23, Terminated, Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | N=80 --> 23 | Trial completion date: Feb 2024 --> Nov 2023 | Recruiting --> Terminated | Trial primary completion date: Feb 2023 --> Nov 2023; The sponsor terminated the study due to the R&D strategy change.
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    TQ-B3525
    over3years
    A Study of TQ-B3525 Tablets in Subjects With PIK3CA and/or PIK3R1/2 Gene-altered Recurrent/Metastatic Advanced Gynecologic Tumors (clinicaltrials.gov)
    P2, N=90, Recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Clinical • New P2 trial
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1)
    |
    TQ-B3525
    almost4years
    TQBSP: TQB3525 for Advanced Bone Sarcomas With PI3KA Mutations or PTEN Loss (clinicaltrials.gov)
    P1/2, N=29, Active, not recruiting, Peking University People's Hospital
    Clinical • New P1/2 trial
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    PTEN (Phosphatase and tensin homolog)
    |
    PTEN loss
    |
    TQ-B3525
    over4years
    A Study of TQ-B3525 Tablets Combined With Fulvestrant Injection in Subjects With HR-positive, HER2-negative and PIK3CA Mutation Advanced Breast Cancer (clinicaltrials.gov)
    P1/2, N=42, Not yet recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Clinical • New P1/2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HR positive • HER-2 negative • PIK3CA mutation
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    fulvestrant • TQ-B3525