Delving into the Latest Updates on Rezivertinib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Rezivertinib, 瑞泽替尼, 瑞齐替尼

+ [4]

Target

EGFR T790M

Mechanism

EGFR T790M inhibitors(EGFR T790M inhibitors)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

EGFR-mutated non-small Cell Lung CancerEGFR T790M Mutation Positive Non-Small Cell Lung Carcinomametastatic non-small cell lung cancer

Inactive Indication-

Originator Organization

Beta Pharma (Shanghai) Co., Ltd.

Active Organization

Beta Pharma (Shanghai) Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

CN (15 May 2024),

EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC27H30N6O3

InChIKeyBPMZUKYFIDPLEA-UHFFFAOYSA-N

CAS Registry1835667-12-3

考察非小细胞肺癌患者单次口服[14C]BPI-7711后全血和血浆中的总放射性强度及分配情况；分析口服[14C]BPI-7711后排泄物中的总放射性强度，获得人体物质平衡数据和主要排泄途径；获得[14C]BPI-7711在非小细胞肺癌患者体内放射性代谢物谱；分析药代动力学参数；测定血浆中主要代谢产物的浓度；观察给药后患者的安全性；

[Translation]

To investigate the total radioactivity intensity and distribution in whole blood and plasma of patients with non-small cell lung cancer after a single oral administration of [14C]BPI-7711; to analyze the total radioactivity intensity in excreta after oral administration of [14C]BPI-7711, to obtain the material balance data and the main excretion pathways in the human body; to obtain the radioactive metabolite spectrum of [14C]BPI-7711 in patients with non-small cell lung cancer; to analyze the pharmacokinetic parameters; to determine the concentration of the main metabolites in plasma; and to observe the safety of patients after administration;

Start Date24 Jun 2020

Sponsor / Collaborator

Beta Pharma (Shanghai) Co., Ltd.

NCT04135820 / CompletedPhase 1

An Open-label, Randomised, Single Dose, Cross-over Phase I Study to Determine the Effect of Food on the Pharmacokinetic Profile of BPI-7711

This is an open-label, randomised, single-dose, cross-over phase I study to evaluate the effect of food on the pharmacokinetic profile of BPI-7711 in Chinese healthy male subjects.

Start Date17 Dec 2019

Sponsor / Collaborator

Beta Pharma (Shanghai) Co., Ltd.

100 Clinical Results associated with Rezivertinib

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100 Translational Medicine associated with Rezivertinib

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100 Patents (Medical) associated with Rezivertinib

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6

Literatures (Medical) associated with Rezivertinib

31 Oct 2023·Zhonghua yi xue za zhi

[China clinical practice guideline for epidermal growth factor receptor tyrosine kinase inhibitors in stage Ⅳ non-small cell lung cancer (version 2023)].

Article

The incidence and mortality of lung cancer rank first among malignant tumors in China. Among them, non-small cell lung cancer (NSCLC) is the most important pathological type, accounting for 80%-85% of lung cancer patients, including adenocarcinoma, squamous cell carcinoma and other pathological subtypes. In recent years, with the discovery of epidermal growth factor receptor (EGFR) gene and the successful development of tyrosine kinase inhibitors (TKIs), the treatment efficacy of stage Ⅳ NSCLC patients with EGFR gene sensitive mutation has been greatly improved. As of August 23, 2023, the first generation EGFR-TKIs, gefitinib, icotinib, and erlotinib; the second generation EGFR-TKIs, afatinib and dacomitinib; and the third generation EGFR-TKIs, osimertinib, almonertinib, furmonertinib and befotertinib were all approved for marketing by China National Medical Products Administration (NMPA). In addition, multiple domestic third-generation EGFR-TKIs are undergoing clinical trials, such as rezivertinib (BPI-7711), limertinib (ASK120067), and oritinib (SH-1028). Meanwhile, mobocertinib and sunvozertinib, which targets EGFR 20ins mutations, were also approved by NMPA. With the increasing variety of EGFR-TKIs approved for marketing subsequently, it brings confusion to clinicians when choosing specific medications, and there is an urgent need to develop relevant treatment guidelines. Hence, the Medical Oncology Branch of China International Exchange and Promotive Association for Medical and Health Care and the Chinese Association for Clinical Oncologists convened experts to integrate the research results of various EGFR-TKIs, and proposed the "China clinical practice guideline for epidermal growth factor receptor tyrosine kinase inhibitors in stage Ⅳ non-small cell lung cancer (version 2023)", to provide reference for better clinical practice.

01 Jun 2023·Lung Cancer

Central nervous system efficacy of rezivertinib (BPI-7711) in advanced NSCLC patients with EGFR T790M mutation: A pooled analysis of two clinical studies

Article

Author: Yi, Tienan ; Lu, Hong ; Chen, Zhendong ; Sun, Meili ; Zheng, Rongsheng ; Yu, Huiqing ; Wu, Gang ; Guo, Zhongliang ; Yi, Shanyong ; Zhong, Diansheng ; Chen, Zhaohong ; Zhou, Anqi ; Wu, Lin ; Guo, Shuliang ; Huang, Jianan ; Xie, Congying ; Zhang, Liangming ; Sun, Shenghua ; Yang, Zhixiong ; Yang, Sheng ; Wang, Tingting ; Bi, Minghong ; Zhao, Guofang ; Greco, Michael ; Li, Jingzhang ; Liu, Chunling ; Chen, Gongyan ; Liu, Jiwei ; Cang, Shundong ; Huang, Meijuan ; Zhang, Longzhen ; Yao, Wenxiu ; Liu, Zhefeng ; Zhu, Bo ; Fan, Yun ; Pan, Yueyin ; Ma, Rui ; Shu, Yongqian ; Zhao, Yanqiu ; Fang, Jian ; Wang, Lijun ; Lin, Yingcheng ; Zhuang, Zhixiang ; Zhou, Jianying ; Wang, Donglin ; Guo, Yanzhen ; Li, Xingya ; Meng, Zili ; Shi, Yuankai ; Liu, Zheng ; Wang, Ke ; Shi, Jianhua ; Hu, Sheng ; Li, Wen ; Han, Zhigang ; Wu, Shiman ; Zhao, Hui

BACKGROUNDRezivertinib (BPI-7711) is a novel third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) which revealed the systematic and central nervous system (CNS) antitumor activities for EGFR T790M-mutated advanced NSCLC in previous clinical studies and is further analyzed here.METHODSEligible patients from the previous phase I and phase IIb studies of rezivertinib were included for pooled analysis. Post-progressive patients who received a prescribed dosage (≥180 mg) of rezivertinib orally once daily were included in full analysis set (FAS), while those with stable, asymptomatic CNS lesions, including measurable and non-measurable ones at baseline were included in CNS full analysis set (cFAS). Patients with measurable CNS lesions were included in CNS evaluable for response set (cEFR). BICR-assessed CNS objective response rate (CNS-ORR), CNS disease control rate (CNS-DCR), CNS duration of response (CNS-DoR), CNS progression-free survival (CNS-PFS), and CNS depth of response (CNS-DepOR) were evaluated.RESULTS355 patients were included in FAS, among whom 150 and 45 patients were included in cFAS and cEFR. This pooled analysis showed the CNS-ORR was 32.0% (48/150; 95% CI: 24.6-40.1%) and the CNS-DCR was 42.0% (63/150; 95% CI: 34.0-50.3%) in cFAS, while that in cEFR were 68.9% (31/45; 95% CI: 53.4-81.8%) and 100% (45/45; 95% CI: 92.1-100.0%). In cEFR, the median CNS-DepOR and the mean of CNS-DepOR were -52.0% (range: -100.0 to 16.1%) and -46.8% (95% CI: -55.5 to -38.1%). In cFAS, the median CNS-DoR and CNS-PFS were 13.8 (95% CI: 9.6-not calculable [NC]) and 16.5 (95% CI: 13.7-NC) months.CONCLUSIONSRezivertinib demonstrated encouraging clinical CNS efficacy among advanced NSCLC patients with EGFR T790M mutation and CNS metastases.

01 Nov 2022·Journal of Thoracic Oncology

Efficacy and Safety of Rezivertinib (BPI-7711) in Patients With Locally Advanced or Metastatic/Recurrent EGFR T790M-Mutated NSCLC: A Phase 2b Study

Article

Author: Chen, Gongyan ; Shi, Jianhua ; Guo, Zhongliang ; Huang, Meijuan ; Liu, Chunling ; Wang, Lijun ; Han, Zhigang ; Li, Wen ; Zhu, Bo ; Wu, Lin ; Shu, Yongqian ; Wang, Ke ; Zhao, Hui ; Sun, Shenghua ; Yi, Shanyong ; Xie, Congying ; Sun, Meili ; Li, Xingya ; Yao, Wenxiu ; Lu, Hong ; Chen, Zhendong ; Shi, Yuankai ; Zhang, Longzhen ; Wu, Shiman ; Fang, Jian ; Hu, Sheng ; Guo, Yanzhen ; Li, Jingzhang ; Bi, Minghong ; Guo, Shuliang ; Cang, Shundong ; Liu, Zheng ; Greco, Michael ; Ma, Rui ; Zhong, Diansheng ; Yi, Tienan ; Wang, Tingting ; Liu, Zhefeng ; Zhao, Yanqiu ; Liu, Jiwei ; Fan, Yun ; Pan, Yueyin ; Yang, Zhixiong ; Meng, Zili ; Zhao, Guofang ; Yu, Huiqing ; Chen, Zhaohong ; Shen, Haijiao ; Lin, Yingcheng

INTRODUCTIONRezivertinib (BPI-7711) is a novel third-generation EGFR tyrosine kinase inhibitor (TKI) targeting both EGFR-sensitizing mutations and EGFR T790M mutation. This study aimed to evaluate the efficacy and safety of rezivertinib in patients with locally advanced or metastatic/recurrent EGFR T790M-mutated NSCLC.METHODSPatients with locally advanced or metastatic/recurrent NSCLC with confirmed EGFR T790M mutation who progressed after first-/second-generation EGFR TKI therapy or primary EGFR T790M mutation were enrolled. Patients received rezivertinib at 180 mg orally once daily until disease progression, unacceptable toxicity, or withdrawal of consent. The primary end point was objective response rate (ORR) assessed by blinded independent central review per Response Evaluation Criteria in Solid Tumors version 1.1. Secondary end points included disease control rate (DCR), duration of response, progression-free survival (PFS), overall survival, and safety. This study is registered with Clinical Trials.gov (NCT03812809).RESULTSA total of 226 patients were enrolled from July 5, 2019, to January 22, 2020. By the data cutoff date on January 24, 2022, the median duration of follow-up was 23.3 months (95% confidence interval [CI]: 22.8-24.0). The ORR by blinded independent central review was 64.6% (95% CI: 58.0%-70.8%), and DCR was 89.8% (95% CI: 85.1%-93.4%). The median duration of response was 12.5 months (95% CI: 10.0-13.9), and median PFS was 12.2 months (95% CI: 9.6-13.9). The median overall survival was 23.9 months (95% CI: 20.0-not calculated [NC]). Among 91 (40.3%) patients with central nervous system (CNS) metastases, the median CNS PFS was 16.6 months (95% CI: 11.1-NC). In 29 patients with more than or equal to one brain target lesion at baseline, the CNS ORR and CNS DCR were 69.0% (95% CI: 49.2%-84.7%) and 100% (95% CI: 88.1%-100%), respectively. Time to progression of CNS was 16.5 months (95% CI: 9.7-NC). Of 226 patients, 188 (83.2%) had at least one treatment-related adverse event, whereas grade more than or equal to 3 occurred in 45 (19.9%) patients. No interstitial lung disease was reported.CONCLUSIONSRezivertinib was found to have promising efficacy and favorable safety profile for patients with locally advanced or metastatic/recurrent NSCLC with EGFR T790M mutation.

100 Deals associated with Rezivertinib

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
EGFR-mutated non-small Cell Lung Cancer	CN	Beta Pharma (Shanghai) Co., Ltd.	29 Oct 2024
EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	CN	Beta Pharma (Shanghai) Co., Ltd.	15 May 2024

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 1	CN	Beta Pharma (Shanghai) Co., Ltd.	16 Aug 2017

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed	Not Applicable	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	355	Rezivertinib	vaqlxvfadj(hrxnucpcwa) = fuianzjvnc ifjzqljxva (gunthgplpd, 34.0 - 50.3) View more	Positive	17 Apr 2023
NCT03386955 (Pubmed)	Phase 1/2	EGFR-mutated non-small Cell Lung Cancer First line	43	Rezivertinib 180 mg	(xxolagkozq) = qrotfzgufj ymnpesvhwy (bpthyoxfgh, 69.3 - 93.2) View more	Positive	08 Jan 2023
NCT03386955 (ESMO2022) Manual	Phase 2	Non-Small Cell Lung Cancer First line EGFR Mutation	43	rezivertinib	(rjhjhsacmz) = svgwcfnpkm heqsusqfuk (rtaobnwdmx, 69.3 - 93.2) View more	Positive	10 Sep 2022
NCT03386955 (ESMO2022) Manual	Phase 2	Non-Small Cell Lung Cancer First line EGFR Mutation	43	rezivertinib (CNS metastases)	(rjhjhsacmz) = xttumucfzh heqsusqfuk (rtaobnwdmx, 21.1 - 78.9) View more	Positive	10 Sep 2022
NCT03812809 (Pubmed)	Phase 2	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	226	Rezivertinib 180mg	lheipbyilk(dgjcggxaxi) = sahhqueszs bnvatpkxyb (wgbemrnnww, 49.2% - 84.7%) View more	Positive	29 Aug 2022
NCT03812809 (ASCO2022) Manual	Phase 2	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma EGFR T790M Mutation	226	Rezivertinib 180mg	(rlrasrrfef) = yciazvrdcb coyuaiyxvo (zvrsyhxkul ) View more	Positive	02 Jun 2022
NCT03812809 (ASCO2022) Manual	Phase 2		226	Rezivertinib 180mg (exon 19 deletion)	(gnsuncgiwy) = sogdbawnva afipvzycyw (nkdhfxbduk, 64.4 - 79.5) View more	Positive	02 Jun 2022
NCT03386955 (Pubmed) Manual	Phase 1	Non-Small Cell Lung Cancer EGFR T790M Mutation	172	Rezivertinib	(qrnkmaoykq) = No dose-limiting toxicity occurred in the dose-escalation phase wtmbvlmeqa (ssibcsrdod ) View more	Positive	15 Feb 2022
NCT03386955 (ASCO2019)	Phase 1	EGFR-mutated non-small Cell Lung Cancer	82	BPI-7711	(ockqphticw) = fqbzembuzx tdsmlcapkp (ntfmlwgzva ) View more	Positive	26 May 2019