更新于：2024-11-11
TQ-B3525
更新于：2024-11-11
概要
基本信息
药物类型 小分子化药 |
别名 TQ B3525、TQ-B3525、TQB3525 |
作用机制 PI3Kα抑制剂(磷脂酰肌醇3-激酶α抑制剂)、PI3Kδ抑制剂(磷脂酰肌醇-3激酶δ抑制剂) |
非在研适应症 |
原研机构 |
非在研机构 |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评优先审评 (中国)、突破性疗法 (中国)、特殊审批 (中国) |
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关联
20
项与 TQ-B3525 相关的临床试验[14C] TQ-B3525在中国成年男性健康受试者体内的吸收、代谢和排泄临床试验-[14C] TQ-B3525人体物质平衡及生物转化研究
Clinical Trial on Absorption, Metabolism and Excretion of [14C] TQ-B3525 in Chinese Adult Male Healthy Subjects - Research on Material Balance and Biotransformation of [14C] TQ-B3525
A Single-arm, Open-label, Multi-cohort, Multi-center Clinical Study on the Safety and Efficacy of TQ-B3525 Tablets Combined With Osimertinib in Subjects With Advanced Non-small Cell Lung Cancer
100 项与 TQ-B3525 相关的临床结果
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100 项与 TQ-B3525 相关的转化医学
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100 项与 TQ-B3525 相关的专利（医药）
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3
项与 TQ-B3525 相关的文献（医药）Signal transduction and targeted therapy
Phase II study of novel orally PI3Kα/δ inhibitor TQ-B3525 in relapsed and/or refractory follicular lymphoma
Article
作者: Ran, Xuehong ; Wu, Huijing ; Su, Liping ; Wang, Binghua ; Feng, Jifeng ; Fang, Meiyun ; Zhou, Hebing ; Sun, Ping ; Chen, Zhuowen ; Wang, Huaqing ; Yang, Yu ; Li, Zhiming ; Su, Hang ; Zhou, Hui ; Xie, Xiaobao ; Liu, Lihong ; Qian, Zhengzi ; Liang, Aibin ; Hu, Guoyu ; Tao, Shi ; Gao, Da ; Liu, Yanyan ; Huang, Zhenqian
Abstract:
This registration study assessed clinical outcomes of TQ-B3525, the dual phosphatidylinositol-3-kinase (PI3K) α/δ inhibitor, in relapsed and/or refractory follicular lymphoma (R/R FL). This phase II study (ClinicalTrials.gov NCT04324879. Registered March 27, 2020) comprised run-in stage and stage 2. R/R FL patients after ≥2 lines therapies received oral 20 mg TQ-B3525 once daily in a 28-day cycle until intolerable toxicity or disease progression. Primary endpoint was independent review committee (IRC)-assessed objective response rate (ORR). Based on results (ORR, 88.0%; duration of response [DOR], 11.8 months; progression-free survival [PFS], 12.0 months) in 25 patients at run-in stage, second stage study was initiated and included 82 patients for efficacy/safety analysis. Patients received prior-line (median, 3) therapies, with 56.1% refractory to previous last therapies; 73.2% experienced POD24 at baseline. At stage 2, ORR was 86.6% (71/82; 95% CI, 77.3–93.1%), with 28 (34.2%) complete responses. Disease control rate was 95.1% due to 7 (8.5%) stable diseases. Median time to response was 1.8 months. Among 71 responders, median DOR was not reached; 18-month DOR rate was 51.6%. with median follow-up of 13.3 months, median PFS was 18.5 (95% CI, 10.2-not estimable) months. Median overall survival (OS) was not reached by cutoff date; 24-month OS rate was estimated as 86.1%. Response rates and survival data were consistent across all subgroups. 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.
CANCER
Preclinical evaluation and phase 1 study of the PI3Kα/δ inhibitor TQ‐B3525 in Chinese patients with advanced cancers
Article
作者: Li, Xiang ; Jiang, Wenqi ; Wang, Huaqing ; Li, Su ; Li, Zhiming ; Tian, Xin ; Tao, Rong ; Feng, Fan
Abstract:
Background:
Phosphatidylinositol 3‐kinase (PI3K) inhibitors transformed management of various malignancies. This study preclinically characterized TQ‐B3525 (dual PI3Kα/δ inhibitor) and assessed the recommended phase 2 dose (RP2D), safety, efficacy, and pharmacokinetics in relapsed or refractory (R/R) lymphoma or advanced solid tumors (STs).
Methods:
Oral TQ‐B3525 was given at eight dose levels on a 28‐day cycle. Primary end points were dose‐limiting toxicity (DLT), maximum tolerated dose (MTD), and safety.
Results:
TQ‐B3525 showed high selectivity and suppressed tumor growth. Between June 12, 2018, and November 18, 2020, 80 patients were enrolled (63 in dose‐escalation cohort; 17 in dose‐expansion cohort). Two DLTs occurred in two (two of 63, 3.2%) DLT‐evaluable patients; MTD was not identified. TQ‐B3525 at 20 mg once daily was selected as RP2D. Grade 3 or worse treatment‐related adverse events mainly included hyperglycemia (16.3%), neutrophil count decreased (15.0%), and diarrhea (10.0%). Two (2.5%) treatment‐related deaths were reported. Sixty patients with R/R lymphoma and 11 advanced STs demonstrated objective response rates of 68.3% and 9.1%, disease control rates of 91.7% and 54.6%, median progression‐free survivals of 12.1 and 1.1 months; median overall survivals were not reached.
Conclusion:
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.
JOURNAL OF CLINICAL PHARMACOLOGY
Predict the Drug–Drug Interaction of a Novel PI3Kα/δ Inhibitor, TQ‐B3525, and Its Two Metabolites Using Physiologically Based Pharmacokinetic Modeling
Article
作者: Yu, Ding ; Wang, Xin ; Wang, Xunqiang ; Zhu, Shixing
Abstract:
A novel dual PI3K α/δ inhibitor, TQ‐B3525, has been developed for the targeted treatment of lymphoma and solid tumors. TQ‐B3525 is primarily metabolized by CYP3A4 and FOM3, while also serving as a substrate for the P‐glycoprotein transporter. The aim of this study was to anticipate the drug–drug interaction (DDI) of TQ‐B3525 and its two metabolites with CYP3A4 enzyme potent inducer (rifampicin) and CYP3A4/P‐gp inhibitor (itraconazole) utilizing a physiologically based pharmacokinetic (PBPK) modeling approach. Clinical data from healthy and cancer patient adults were employed to construct and evaluate the PBPK model for TQ‐B3525, M3, and M8‐3. Models involving rifampicin combined with midazolam, itraconazole combined with midazolam or digoxin were utilized to showcase the robustness of evaluating DDI effects. The simulated drug exposure of TQ‐B3525, M3, and M8‐3 in healthy and patient adults were consistent with clinical data, and the mean fold error values were within the acceptable ranges. The simulated results of positive substrates correspond to those reported in the literature. Co‐administration with rifampicin reduces Cmax and AUC of TQ‐B3525 to 76.1% and 46.0%, while increasing the levels of M3 and M8‐3. With itraconazole, Cmax and AUC of TQ‐B3525 rise to 131% and 204%, but decrease substantially for M3 and M8‐3. 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.
100 项与 TQ-B3525 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 复发性滤泡性淋巴瘤 | 申请上市 | 中国 | 2023-05-22 | |
| 难治性滤泡性淋巴瘤 | 申请上市 | 中国 | 2023-05-22 | |
| 晚期非小细胞肺癌 | 临床2期 | 中国 | 2022-03-11 | |
| 复发性慢性淋巴细胞白血病 | 临床2期 | 中国 | 2021-06-05 | |
| 小淋巴细胞淋巴瘤 | 临床2期 | 中国 | 2021-06-05 | |
| 子宫内膜癌 | 临床2期 | 中国 | 2021-04-23 | |
| 卵巢癌 | 临床2期 | 中国 | 2021-04-23 | |
| 宫颈癌 | 临床2期 | 中国 | 2021-04-23 | |
| 弥漫性大B细胞淋巴瘤 | 临床2期 | 中国 | 2021-01-20 | |
| 外周T细胞淋巴瘤 | 临床2期 | 中国 | 2020-12-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | - | 鏇齋廠製構憲醖衊簾築(淵齋鏇網獵鏇鏇鬱膚衊) = 築積觸觸鹹衊蓋鬱鹽網 鹹窪觸鑰構壓鏇觸艱積 (積鏇衊構構構積膚構淵 ) | 积极 | 2024-05-24 | |||
临床2期 | - | 構顧構顧範醖築網遞壓(衊蓋鑰襯淵淵獵製糧齋) = 膚窪糧簾衊鑰鏇範繭醖 夢夢鹹鏇願觸齋鬱遞壓 (鹹蓋廠鹽鏇製願鏇齋獵 ) 更多 | 积极 | 2024-04-17 | |||
临床1期 | 40 | 膚築鏇醖網製簾鑰鑰範(壓糧鹹簾繭願築鏇鹽淵) = 築繭範壓遞蓋願鹹觸鬱 淵鏇醖蓋觸鬱膚製獵鏇 (壓艱蓋築鏇壓築鹹選構 ) 更多 | 积极 | 2020-05-25 |
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