TQ-B3525 / Sino Biopharm - LARVOL DELTA

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."

Journal • PK/PD data • Hematological Malignancies • Lymphoma • Oncology • Solid Tumor • CYP3A4 • PIK3CA

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."

Journal • Metastases • P1 data • Preclinical • Diabetes • Hematological Malignancies • Lymphoma • Oncology • Solid Tumor • PIK3CA

A novel and selective oral PI3Kα/δ inhibitor, TQ-B3525, in patients with relapsed and/or refractory follicular lymphoma: A phase II, single-arm, open-label study. (ASCO 2024) - P2 | "TQ-B3525 exhibited favorable efficacy and manageable safety profiles, supporting its potential as a valuable treatment modality for heavily pretreated Chinese R/R/ FL patients."

Clinical • P2 data • Diabetes • Follicular Lymphoma • Hematological Malignancies • Lymphoma • Oncology • PIK3CA

Recent advances in treatment of follicular lymphoma: efficacy of PI3Kα/δ inhibitor (TQ-B3525). (PubMed, Signal Transduct Target Ther) - No abstract available

Journal • Follicular Lymphoma • Hematological Malignancies • Lymphoma • Oncology • PIK3CA

Phase II study of novel orally PI3Kα/δ inhibitor TQ-B3525 in relapsed and/or refractory follicular lymphoma. (PubMed, Signal Transduct Target Ther) - P2 | "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."

Journal • P2 data • Diabetes • Follicular Lymphoma • Hematological Disorders • Hematological Malignancies • Lymphoma • Neutropenia • Oncology • PIK3CA

Phase II study of novel orally PI3Kα/δ inhibitor TQ-B3525 in relapsed and/or refractory follicular lymphoma (Nature, Signal Transduct Target Ther) - P2 | N=80 | NCT04324879 | Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | "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."

P2 data • Follicular Lymphoma

Phase II study of novel orally PI3Kα/δ inhibitor TQ-B3525 in relapsed and/or refractory follicular lymphoma (Nature, Signal Transduct Target Ther) - P2 | N=80 | NCT04324879 | Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | "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."

P2 data • Follicular Lymphoma

A Study of TQ-B3525 in Subjects With Relapsed/Refractory Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (clinicaltrials.gov) - P1/2 | N=23 | Terminated | Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | N=80 ➔ 23 | Trial completion date: Feb 2024 ➔ Nov 2023 | Recruiting ➔ Terminated; The sponsor terminated the study due to the R&D strategy change.

Enrollment change • Trial completion date • Trial termination • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma

Zhongsheng Pharmaceutical: The marketing application for the innovative drug TQ-B3525 tablets for the treatment of lymphoma indications has been accepted [Google translation] (Yahoo Finance) - "Sino Biopharmaceutical...announced that TQ-B3525 Tablets (PI3Kδ/α Dual Inhibitor), an innovative class 1 anti-tumor drug developed by the Group, has submitted a new drug marketing application to the Drug Evaluation Center of the State Drug Administration of China And accepted, the treatment indications are relapsed or refractory follicular lymphoma who have received at least second-line systemic therapy in the past."

Non-US regulatory • Hematological Malignancies • Lymphoma • Oncology

A Study of TQ-B3525 on Tolerance and Pharmacokinetics (clinicaltrials.gov) - P1 | N=60 | Recruiting | Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Unknown status ➔ Recruiting | Trial completion date: Dec 2019 ➔ Aug 2024 | Trial primary completion date: Dec 2019 ➔ Aug 2022

Enrollment open • Trial completion date • Trial primary completion date • Hematological Malignancies • Lymphoma • Oncology • Solid Tumor

[VIRTUAL] Safety and efficacy of TQ-B3525, a novel and selective oral PI3K α/δ inhibitor, in Chinese patients with advanced malignancies: A phase I dose-escalation and expansion trial. (ASCO 2020) - P1 | "Background: TQ-B3525 is a novel and selective oral PI3K α/δ inhibitor with activity 41 and 138 folds higher than Buparlisib against PI3K α and PI3K δ in pre-clinical research. TQ-B3525 is well-tolerated in Chinese patients with advanced malignancies, and demonstrated high promising antitumor activity in R/R lymphoma patients. Recommended phase II dose was established at 20mg qd. A single-arm phase 2 trial of TQ-B3525 in patients with R/R FL is currently underway."

Clinical • P1 data • Follicular Lymphoma • Hematological Disorders • Hematological Malignancies • Oncology

Material Balance Study of TQ-B3525 (clinicaltrials.gov) - P1 | N=8 | Not yet recruiting | Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

New P1 trial • Chronic Kidney Disease • Nephrology • Renal Disease

TQ-B3525 Tablets Combined With Osimertinib Mesylate Tablets in the Treatment of Advanced Non-Small Cell Lung Cancer (clinicaltrials.gov) - P1/2 | N=160 | Recruiting | Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

New P1/2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TQ-B3525 in Subjects With Relapse/Refractory Diffuse Large B-cell Lymphoma （DLBCL） (clinicaltrials.gov) - P2; N=93; Recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.; Not yet recruiting ➔ Recruiting

Enrollment open • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Chia Tai Tianqing’s PI3K-targeted drug nails BTD for FL in China (GBI Health) - "The Center for Drug Evaluation (CDE) website indicates that Chia Tai Tianqing Pharmaceutical Group Co. Ltd’s TQ-B3525 has been awarded breakthrough therapy designation (BTD) status for use in recurrent/refractory follicular lymphoma. Specifically, the indication is for use in patients who have failed second-line or later treatment."

Non-US regulatory • Diffuse Large B Cell Lymphoma • Follicular Lymphoma • Hematological Malignancies • Non-Hodgkin’s Lymphoma • Oncology

A Study of TQ-B3525 in Subjects With Relapsed/Refractory Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (clinicaltrials.gov) - P1/2; N=80; Recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma

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; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

New P2 trial • Cervical Cancer • Endometrial Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor • PIK3CA • PIK3R1

A Study of TQ-B3525 in Subjects With Relapsed/Refractory Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (clinicaltrials.gov) - P1/2; N=80; Not yet recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Clinical • New P1/2 trial • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma

TQBSP: TQB3525 for Advanced Bone Sarcomas With PI3KA Mutations or PTEN Loss (clinicaltrials.gov) - P1/2; N=29; Active, not recruiting; Sponsor: Peking University People's Hospital

Clinical • New P1/2 trial • Oncology • Osteosarcoma • Sarcoma • Solid Tumor • PTEN

A Study of TQ-B3525 in Subjects With Relapsed/Refractory Peripheral T-cell Lymphoma（PTCL） (clinicaltrials.gov) - P2; N=78; Not yet recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Clinical • New P2 trial • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Peripheral T-cell Lymphoma • T Cell Non-Hodgkin Lymphoma

A Study of TQ-B3525 in Subjects With Relapse/Refractory Diffuse Large B-cell Lymphoma （DLBCL） (clinicaltrials.gov) - P2; N=93; Not yet recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Clinical • New P2 trial • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

A Study of TQ-B3525 Tablet in the Treatment of Relapsed / Refractory Mantle Cell Lymphoma (MCL) (clinicaltrials.gov) - P2; N=102; Recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma • Oncology

A Study of TQ-B3525 in the Treatment of Relapsed / Refractory Follicular Lymphoma (FL) (clinicaltrials.gov) - P2; N=80; Recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Follicular Lymphoma • Hematological Malignancies • Lymphoma • Oncology

A Study of TQ-B3525 Tablet in the Treatment of Relapsed / Refractory Mantle Cell Lymphoma (MCL) (clinicaltrials.gov) - P2; N=102; Not yet recruiting; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Clinical • New P2 trial • Hematological Disorders • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma • Oncology

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; Sponsor: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Clinical • New P1/2 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2