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

Action

inhibitors

Mechanism

EGFR T790M inhibitors(Epidermal Growth Factor Receptor T790M inhibitors)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

EGFR-mutated non-small Cell Lung CancerEGFR T790M Mutation Positive Non-Small Cell Lung CarcinomaAdvanced Lung Non-Small Cell Carcinoma+ [1]

Inactive Indication-

Originator Organization

Beta Pharma (Shanghai) Co., Ltd.

Active Organization

Beta Pharma (Shanghai) Co., Ltd.

Inactive Organization-

License Organization

Beta Pharma (Shanghai) Co., Ltd.Shiyao (Shanghai) Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

China (15 May 2024),

EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma

RegulationSpecial Review Project (China)

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Structure/Sequence

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.

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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14

Literatures (Medical) associated with Rezivertinib

01 Jun 2025·BIOORGANIC & MEDICINAL CHEMISTRY

A clinical review on third and fourth generation EGFR tyrosine kinase inhibitors for the treatment of non-small cell lung cancer

Review

Author: Patel, Harun M ; Patil, Chandragouda R ; Gawli, Chandrakant S

"Epidermal growth factor receptor (EGFR)" mutations are pivotal in the pathogenesis of "Non-Small Cell Lung Cancer (NSCLC)," which is associated with high morbidity and mortality rates. The advent of third and fourth-generation EGFR tyrosine kinase inhibitors (TKIs) has significantly advanced the therapeutic landscape for EGFR-mutant NSCLC, particularly in overcoming resistance mutations such as T790M and C797S. This review delves into the current clinical status, efficacy, safety profiles, and regulatory approvals of third-generation EGFR TKIs, including Osimertinib, Lazertinib, Furmonertinib, Aumolertinib, Rezivertinib, Befotertinib, Sunvozertinib. Furthermore, it explores emerging fourth-generation EGFR TKIs designed to address resistance mechanisms beyond those targeted by their predecessors. Notable fourth-generation candidates such as TQB3804, BPI-361175, BDTX-1535, WJ13404, QLH11811, H002, HS-10375, BBT-207, JIN-A02, and HS-10504 are highlighted for their potential to overcome the C797S mutation. The review emphasizes the importance of these advanced inhibitors in enhancing "progression-free survival and overall survival rates". By evaluating the therapeutic potential and limitations of these EGFR TKIs, this review aims to guide future research in the management of EGFR-mutant NSCLC. This acts as guiding beacon for the strategic design and development of third and fourth generation EGFR-TK inhibitors to overcome the drug resistance hurdles in the development of EGFR-TK inhibitors.

01 Apr 2025·Lancet Respiratory Medicine

Rezivertinib versus gefitinib as first-line therapy for patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer (REZOR): a multicentre, double-blind, randomised, phase 3 study

Article

Author: Lu, Hong ; Qin, Jianwen ; Guo, Yanzhen ; Yi, Shanyong ; Zhou, Anqi ; Li, Xingya ; Shi, Huaqiu ; Zhang, Don ; Yang, Minglei ; Peng, Jirong ; Wang, Lijun ; Bi, Minghong ; Cang, Shundong ; Li, Manxiang ; Zhao, Wenhua ; Zhao, Yanqiu ; Sun, Shenghua ; Pan, Yueyin ; Hu, Sheng ; Chen, Zhaohong ; Shu, Yongqian ; Guo, Shuliang ; Zhong, DianSheng ; He, Zhiyong ; Wang, Ke ; Han, Zhigang ; Yu, Zhuang ; Zhou, Rui ; Gao, Feng ; Gao, Jinghua ; Liu, Zheng ; Shi, Jianhua ; Shi, Yuankai ; Lin, Yingcheng ; Zhang, Liangming ; Ye, Feng ; Ji, Hongbo ; Cui, Jiuwei ; Zhang, Hua ; Zhu, Bo ; Zhou, Xiangdong ; Sun, Meili ; Li, Wen ; Fan, Yun ; Yang, Sheng ; Wang, Tingting ; Jiang, Mingyan ; Wu, Lin ; Ma, Rui ; Yao, Wenxiu ; Wen, Meiling ; Yi, Tienan ; Zhang, Yan ; Yu, Huiqing ; Shen, Haijiao ; Fang, Jian ; Wang, Haitao

BACKGROUND:

This study aimed to compare the efficacy and safety of rezivertinib (BPI-7711) and gefitinib as first-line therapies in patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer (NSCLC).

METHODS:

This multicentre, double-blind, randomised, phase 3 study (REZOR) included eligible patients from 50 hospitals across China. Those who had been histologically or cytologically confirmed as having NSCLC with EGFR exon 19 deletion or exon 21 Leu858Arg mutation by central laboratory were randomly assigned (1:1) to receive once daily either rezivertinib 180 mg or gefitinib 250 mg, until unacceptable toxicity occurred, disease progression, or other treatment discontinuation criteria were met. Each cycle lasted for 21 days. The primary endpoint was progression-free survival evaluated by masked independent central review (MICR) in the intention-to-treat set. This trial is registered with ClinicalTrials.gov, NCT03866499 and follow-up is ongoing.

FINDINGS:

Between July 15, 2019, and Feb 14, 2022, 695 patients were screened. Among them, 369 eligible patients were randomly assigned to receive either rezivertinib 180 mg/day plus placebo (n=184) or gefitinib 250 mg/day plus placebo (n=185) in a 1:1 ratio; all of eligible participants were included in the intention-to-treat set. Median MICR-assessed progression-free survival was 19·3 months (95% CI 13·8-22·1) in the rezivertinib group and 9·6 months (8·4-11·3) in the gefitinib group (hazard ratio [HR] 0·48, 95% CI 0·36-0·63; p<0·0001) and the prespecified subgroup efficacy analysis showed consistent results. Median duration of exposure was 16·0 months (95% CI 0·0-29·7) in the rezivertinib group and 11·0 months (0·0-28·9) in the gefitinib group. Grade 3 or higher treatment-emergent adverse events (82 [45%] of 184 in the rezivertinib group; 80 [43%] of 185 in the gefitinib group) and treatment-related adverse events (TRAEs; 43 [23%] of 184 in the rezivertinib group; 43 [23%] of 185 in the gefitinib group) were similar in both groups. One patient died from a TRAE in the rezivertinib group, due to pneumonia and interstitial lung disease.

INTERPRETATION:

Our findings suggested that rezivertinib is a potential choice for patients with EGFR-mutated locally advanced or metastatic NSCLC as first-line therapy, owing to the superior overall efficacy and subgroup progression-free survival compared with gefitinib in targeted patients. No new safety signals were identified.

FUNDING:

Beta Pharma (Shanghai) and the China National Science and Technology Major Project for Key New Drug Development.

01 Apr 2024·Translational Lung Cancer Research

Development and validation of a deep learning-based model to predict response and survival of T790M mutant non-small cell lung cancer patients in early clinical phase trials using electronic medical record and pharmacokinetic data

Article

Author: Han, Xiaohong ; Jiang, Ji ; Qiao, Nan ; Wang, Weicong ; Shen, Wei ; Lin, Xinyuan ; Gao, Ruyun ; Wang, Shanbo ; Zheng, Xin ; Wang, Lu ; Lou, Ning ; Xu, Chi ; Cui, Xinge

Background:

Epidermal growth factor receptor (EGFR) T790M mutation is the standard predictive biomarker for third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) treatment. While not all T790M-positive patients respond to third-generation EGFR-TKIs and have a good prognosis, it necessitates novel tools to supplement EGFR genotype detection for predicting efficacy and stratifying EGFR-mutant patients with various prognoses. Mixture-of-experts (MoE) is designed to disassemble a large model into many small models. Meanwhile, it is also a model ensembling method that can better capture multiple patterns of intrinsic subgroups of enrolled patients. Therefore, the combination of MoE and Cox algorithm has the potential to predict efficacy and stratify survival in non-small cell lung cancer (NSCLC) patients with EGFR mutations.

Methods:

We utilized the electronic medical record (EMR) and pharmacokinetic parameters of 326 T790M-mutated NSCLC patients, including 283 patients treated with Abivertinib in phase I (n=177, for training) and II (n=106, for validation) clinical trials and an additional validation cohort 2 comprising 43 patients treated with BPI-7711. Furthermore, 18 patients underwent whole-exome sequencing for biological interpretation of CoxMoE. We evaluated the predictive performance for therapeutic response using the area under the curve (AUC) and the Concordance index (C-index) for progression-free survival (PFS).

Results:

CoxMoE exhibited AUCs of 0.73-0.83 for predicting efficacy defined by best overall response (BoR) and achieved C-index values of 0.64-0.65 for PFS prediction in training and validating cohorts. The PFS of 198 patients with a low risk [median, 6.0 (range, 1.0-23.3) months in the abivertinib treated cohort; median 16.5 (range, 1.4-27.4) months in BPI-7711 treated cohort] of being non-responder increased by 43% [hazard ratio (HR), 0.56; 95% confidence interval (CI), 0.40-0.78; P=0.0013] and 50% (HR, 0; 95% CI, 0-0; P=0.01) compared to those at high-risk [median, 4.2 (range, 1.0-35) months in the abivertinib treated cohort; median, 11.0 (range, 1.4-25.1) months in BPI-7711 treated cohort]. Additionally, activated partial thromboplastin time (APTT), creatinine clearance (Ccr), monocyte, and steady-state plasma trough concentration utilited to construct model were found significantly associated with drug resistance and aggressive tumor pathways. A robust correlation was observed between APTT and Ccr with PFS (log-rank test; P<0.01) and treatment response (Wilcoxon test; P<0.05), respectively.

Conclusions:

CoxMoE offers a valuable approach for patient selection by forecasting therapeutic response and PFS utilizing laboratory tests and pharmacokinetic parameters in the setting of early-phase clinical trials. Simultaneously, CoxMoE could predict the efficacy of third-generation EGFR-TKI non-invasively for T790M-positive NSCLC patients, thereby complementing existing EGFR genotype detection.

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	China	Beta Pharma (Shanghai) Co., Ltd.	29 Oct 2024
EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	China	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
Advanced Lung Non-Small Cell Carcinoma	Phase 1	China	Beta Pharma (Shanghai) Co., Ltd.	16 Aug 2017
metastatic non-small cell lung cancer	Phase 1	China	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


NCT03866499 (REZOR, Pubmed) Manual	Phase 3	EGFR-mutated non-small Cell Lung Cancer First line EGFR L858R \| EGFR Exon 19 Deletion	369	rezivertinib	efvgtwbcif(xxjiiynepu) = zercjeknro nrsnrnxipv (gixlyavkyf, 13.8 - 22.1) View more	Positive	03 Feb 2025
NCT03866499 (REZOR, Pubmed) Manual	Phase 3		369	gefitinib	efvgtwbcif(xxjiiynepu) = qjuaunodpy nrsnrnxipv (gixlyavkyf, 8.4 - 11.3) View more	Positive	03 Feb 2025
NCT03812809 \| NCT03386955 (Pubmed \| Lung Cancer)	Not Applicable	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	355	Rezivertinib	dbcepvrzot(tdimodrakq) = recycctkxq liyxejjrgr (jzwztanmax, 34.0 - 50.3) View more	Positive	17 Apr 2023
NCT03386955 (ESMO2022) Manual	Phase 2	Non-Small Cell Lung Cancer First line EGFR Mutation	43	rezivertinib	zthehdubyj(xrskxyhogi) = zzhihvnzne kvyjmgsjfk (telxiedwfg, 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)	zthehdubyj(xrskxyhogi) = zmbuodmqyc kvyjmgsjfk (telxiedwfg, 21.1 - 78.9) View more	Positive	10 Sep 2022
NCT03812809 (Pubmed \| J Thorac Oncol)	Phase 2	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	226	Rezivertinib 180mg	njnwwfuhps(doofyuamau) = frpauxgcyh tquomwnnkt (ntqlwlgqwt, 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	ggxfsadmvm(tsxveskazx) = qlknzgzlhv djnobildjr (tvwdfmbbih ) View more	Positive	02 Jun 2022
NCT03812809 (ASCO2022) Manual	Phase 2		226	Rezivertinib 180mg (exon 19 deletion)	ggxfsadmvm(zyxoartlpx) = kzjaxwmiiu thqgsizpyv (mitadvigvw, 64.4 - 79.5) View more	Positive	02 Jun 2022
NCT03386955 (Pubmed \| J Thorac Oncol) Manual	Phase 1	Non-Small Cell Lung Cancer EGFR T790M Mutation	172	Rezivertinib	rthjtwspbr(scicbzklgz) = No dose-limiting toxicity occurred in the dose-escalation phase jramnornxn (vtnmrzqvun ) View more	Positive	15 Feb 2022
NCT03386955 (ASCO2019)	Phase 1	EGFR-mutated non-small Cell Lung Cancer	82	BPI-7711	utmpqwjouj(vjvbxoncmz) = owwjgdsqhd iewcnohtik (mjeqtyudeh ) View more	Positive	26 May 2019