Delving into the Latest Updates on BEBT-908 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

双利司他

+ [2]

Target

HDACs x PI3K family

Mechanism

HDAC inhibitors(Histone deacetylase inhibitors), Phosphatidylinositol 3-kinase family inhibitors

Therapeutic Areas

NeoplasmsImmune System DiseasesHemic and Lymphatic Diseases+ [4]

Active Indication

Diffuse large B-cell lymphoma recurrentDiffuse large B-cell lymphoma refractoryPeripheral T-Cell Lymphoma+ [8]

Inactive Indication

Multiple MyelomaRecurrent LymphomaRefractory Lymphoma

Originator Organization

BeBetter Med, Inc.

Active Organization

Zhongshan Union Weihua Pharmaceutical Co. Ltd.

BeBetter Med, Inc.

Inactive Organization-

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (CN), Priority Review (CN), Breakthrough Therapy (CN)

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Structure

Molecular FormulaC23H28Cl3N9O3S

InChIKeyXQJBSJNJWWXTFM-UHFFFAOYSA-N

CAS Registry1646906-27-5

View All Structures (2)

This is a multicenter, open Phase Ib clinical study to evaluate the safety,efficacy and pharmacokinetics of BEBT-908 combined with Rituximab (R) or combined with Rituximab-Gemcitabine-Oxaliplatin (R-GemOx) or combined with Rituximab-Ifosfamide-Carboplatin-Etoposide (R-ICE) in the treatment of Relapsed/Refractory Diffuse Large B-Cell Lymphoma (R/R DLBCL).

Start Date01 Dec 2023

Sponsor / Collaborator

BeBetter Med, Inc.

CTR20213331 / RecruitingPhase 1/2

评价BEBT-908与BEBT-109单药或联合治疗晚期非小细胞肺癌的多中心、开放性、三阶段Ib/II期临床试验

[Translation] A multicenter, open-label, three-stage Phase Ib/II clinical trial evaluating BEBT-908 and BEBT-109 as monotherapy or in combination for the treatment of advanced non-small cell lung cancer

主要目的： 1.评价BEBT-908与BEBT-109单药或联合治疗晚期非小细胞肺癌的有效性； 2.评价BEBT-908与BEBT-109单药或联合治疗晚期非小细胞肺癌的安全性和耐受性。次要目的： 1.评价BEBT-908与BEBT-109单药或联合治疗晚期非小细胞肺癌的生物标志物药效学意义； 2.评价BEBT-908与BEBT-109单药或联合治疗晚期非小细胞肺癌的药代动力学特征。

[Translation]

Main objectives: 1. To evaluate the efficacy of BEBT-908 and BEBT-109 as monotherapy or in combination in the treatment of advanced non-small cell lung cancer; 2. To evaluate the safety and tolerability of BEBT-908 and BEBT-109 as monotherapy or in combination in the treatment of advanced non-small cell lung cancer. Secondary objectives: 1. To evaluate the pharmacodynamic significance of biomarkers in the treatment of advanced non-small cell lung cancer with BEBT-908 and BEBT-109 as monotherapy or in combination; 2. To evaluate the pharmacokinetic characteristics of BEBT-908 and BEBT-109 as monotherapy or in combination in the treatment of advanced non-small cell lung cancer.

Start Date28 Mar 2022

Sponsor / Collaborator

BeBetter Med, Inc.

100 Clinical Results associated with BEBT-908

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100 Translational Medicine associated with BEBT-908

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100 Patents (Medical) associated with BEBT-908

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4

Literatures (Medical) associated with BEBT-908

01 Nov 2023·Targeted Oncology

Dual PI3K/HDAC Inhibitor BEBT-908 Exhibits Potent Efficacy as Monotherapy for Primary Central Nervous System Lymphoma

Article

Author: Zhou, Minhua ; Ye, Xiaolan ; Mo, Zhenxian ; Liu, Xinjian ; Xiong, Yan ; Pan, Lu ; Li, Wenyu ; Chen, Feili ; Fan, Fushun ; Qian, Changgeng ; Cai, Xiong ; Wang, Ning

BACKGROUNDThe efficacy of systemic treatment for primary central nervous system lymphoma (PCNSL) is limited because of the blood-brain barrier (BBB) and the ineffectiveness of chemotherapy. The dual PI3K/HDAC inhibitor BEBT-908 has exhibited favorable in vivo distribution and activity in various cancers.OBJECTIVESThe aims of this study were to assess the efficacy of BEBT-908 in brain orthotopic mouse models of hematological malignancies, to investigate its pharmacologic properties, and to elucidate the underlying mechanism of action.METHODSWe evaluated the anticancer activity of BEBT-908 in various hematological malignancies through cell viability assays. The impact of BEBT-908 on c-Myc expression and ferroptosis signaling pathways was assessed using Western blotting, qPCR, ROS detection, GSH/GSSG detection, and IHC. Pharmacokinetic and pharmacodynamic profiles were assessed through LC-MS/MS and Western blotting. The effects of BEBT-908 in vivo were examined using xenografts and brain orthotopic mouse models.RESULTSOur findings demonstrate that BEBT-908 exhibits promising anti-tumor activity in vitro and in vivo across multiple subtypes of hematological malignancies. Furthermore, BEBT-908 exhibits excellent BBB penetration and inhibits tumor growth in a brain orthotopic lymphoma model with prolonged survival of host mice. Mechanistically, BEBT-908 downregulated c-Myc expression, which contributed to ferroptosis, ultimately leading to tumor shrinkage.CONCLUSIONOur study provides robust evidence for the dual PI3K/HDAC inhibitor BEBT-908 as an effective anti-cancer agent for PCNSL.

15 Dec 2021·Cancer ResearchQ1 · MEDICINE

A Dual PI3K/HDAC Inhibitor Induces Immunogenic Ferroptosis to Potentiate Cancer Immune Checkpoint Therapy

Q1 · MEDICINE

Article

Author: Fan, Fushun ; Liu, Haiqi ; Bao, Rudi ; Liu, Pei ; Ma, Yaru ; Mo, Zhenxian ; Zhou, Minhua ; Qian, Changgeng ; Zhou, Yiping ; Chen, Jian ; Liu, Xinjian ; Cai, Xiong

AbstractThe capacity of targeted anticancer agents to exert immunomodulatory effects provides a strong rationale to develop novel agents suitable for combinatorial regimens with immunotherapy to improve clinical outcomes. In this study, we developed a dual-targeting PI3K and HDAC inhibitor BEBT-908 that potently inhibits tumor cell growth and potentiates anti-PD1 therapy in mice by inducing immunogenic ferroptosis in cancer cells. Treatment with BEBT-908 promoted ferroptotic cell death of cancer cells by hyperacetylating p53 and facilitating the expression of ferroptotic signaling. Furthermore, BEBT-908 promoted a proinflammatory tumor microenvironment that activated host antitumor immune responses and potentiated immune checkpoint blockade therapy. Mechanistically, BEBT-908–induced ferroptosis led to upregulation of MHC class I and activation of endogenous IFNγ signaling in cancer cells via the STAT1 signaling pathway. The dual PI3K/HDAC inhibitor BEBT-908 is a promising targeted therapeutic agent against multiple cancer types that promotes immunogenic ferroptosis and enhances the efficacy of immunotherapy.Significance:The dual PI3K/HDAC inhibitor BEBT-908 elicits potent antitumor responses, effectively inducing immunogenic ferroptosis of tumor cells and potentiating cancer immunotherapy.

01 Mar 2018·Biochemical and Biophysical Research CommunicationsQ3 · BIOLOGY

Retraction notice to “BEBT-908: A novel potent PI3K/HDAC inhibitor against diffuse large B-cell lymphoma” [Biochem. Biophys. Res. Commun. 491 (2017) 939-945]

Q3 · BIOLOGY

Article

Author: Li, Kunlun ; Yi, Pingyong ; Li, Jin ; Li, Jiwei ; Qian, Changgeng ; Zhou, Qianqian

This article has been retracted.

100 Deals associated with BEBT-908

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diffuse large B-cell lymphoma recurrent	NDA/BLA	CN	BeBetter Med, Inc.	09 Oct 2023
Diffuse large B-cell lymphoma recurrent	NDA/BLA	CN	Zhongshan Union Weihua Pharmaceutical Co. Ltd.	09 Oct 2023
Diffuse large B-cell lymphoma refractory	NDA/BLA	CN	BeBetter Med, Inc.	09 Oct 2023
Diffuse large B-cell lymphoma refractory	NDA/BLA	CN	Zhongshan Union Weihua Pharmaceutical Co. Ltd.	09 Oct 2023
Peripheral T-Cell Lymphoma	Phase 2	CN	BeBetter Med, Inc.	16 Aug 2021
Chronic Lymphocytic Leukemia	Phase 2	CN	BeBetter Med, Inc.	12 Aug 2021
Follicular Lymphoma	Phase 2	CN	BeBetter Med, Inc.	12 Aug 2021
Marginal Zone B-Cell Lymphoma	Phase 2	CN	BeBetter Med, Inc.	12 Aug 2021
Small Lymphocytic Lymphoma	Phase 2	CN	BeBetter Med, Inc.	12 Aug 2021
Waldenstrom Macroglobulinemia	Phase 2	-	BeBetter Med, Inc.	-