Delving into the Latest Updates on Mefatinib with Synapse

主要研究目的： 1.定量分析健康男性受试者口服[14C]迈华替尼后排泄物中的总放射性，获得人体放射性排泄率数据和主要排泄途径； 2.定量分析健康男性受试者单次口服[14C]迈华替尼后全血和血浆中的总放射性，获得血浆中总放射性的药代动力学参数，并考察全血和血浆中总放射性的分配情况； 3.考察男性受试者口服[14C]迈华替尼后人血浆、尿液和粪便的放射性物谱，鉴定主要代谢产物（≥10%总放射性AUC或≥10%给药量），确定主要生物转化途径及消除途径；次要研究目的 1.采用已验证的HPLC-MS/MS方法定量分析血浆中迈华替尼及其代谢产物（如适用）的浓度，获得血浆中迈华替尼及其代谢产物（如适用）的药代动力学参数； 2.观察[14C]迈华替尼单次给药后健康男性受试者的安全性。

[Translation]

Main study objectives: 1. Quantitatively analyze the total radioactivity in the excreta of healthy male subjects after oral administration of [14C] Maihuatinib, and obtain the data on human radioactive excretion rate and main excretion pathways; 2. Quantitatively analyze the total radioactivity in whole blood and plasma of healthy male subjects after a single oral administration of [14C] Maihuatinib, obtain the pharmacokinetic parameters of total radioactivity in plasma, and investigate the distribution of total radioactivity in whole blood and plasma; 3. Investigate the radioactivity spectrum of human plasma, urine and feces after oral administration of [14C] Maihuatinib to identify the main metabolites (≥10% total radioactivity AUC or ≥10% dose), and determine the main biotransformation pathways and elimination pathways; Secondary study objectives 1. Quantitatively analyze the concentration of Maihuatinib and its metabolites (if applicable) in plasma using a validated HPLC-MS/MS method, and obtain the pharmacokinetic parameters of Maihuatinib and its metabolites (if applicable) in plasma; 2. Observe the safety of healthy male subjects after a single dose of [14C] Maihuatinib.

Start Date21 Nov 2022

Sponsor / Collaborator

Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.

[+1]

CTR20200280

/ CompletedPhase 1

食物对迈华替尼片在健康受试者中单中心、随机、开放、单制剂、两周期、双交叉、单次给药药代动力学影响研究

[Translation] A single-center, randomized, open-label, single-dose, two-period, double-crossover, single-dose pharmacokinetics study of food on mavartinib tablets in healthy subjects

主要研究目的：评价食物对迈华替尼片（60mg/片，1片/次）在健康受试者体内的药代动力学特征的影响。次要研究目的：评价迈华替尼片（60mg/片，1片/次）在健康受试者中的安全性和耐受性。

[Translation]

Primary study objective: To evaluate the effect of food on the pharmacokinetic characteristics of Maihuatinib tablets (60 mg/tablet, 1 tablet/time) in healthy subjects. Secondary study objective: To evaluate the safety and tolerability of Maihuatinib tablets (60 mg/tablet, 1 tablet/time) in healthy subjects.

Start Date07 May 2020

Sponsor / Collaborator

Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.

[+1]

CTR20192297

/ CompletedPhase 3

迈华替尼对比吉非替尼一线治疗EGFR敏感突变的晚期非鳞非小细胞肺癌的随机、平行、双盲双模拟、多中心的Ⅲ期临床

[Translation] A randomized, parallel, double-blind, double-dummy, multicenter phase III clinical trial of mahuatinib versus gefitinib as first-line treatment for advanced non-squamous non-small cell lung cancer with EGFR sensitive mutations

主要目的：评估迈华替尼对比吉非替尼一线治疗EGFR敏感突变的晚期非鳞非小细胞肺癌的有效性。次要目的：评估迈华替尼对比吉非替尼一线治疗EGFR敏感突变的晚期非鳞非小细胞肺癌的安全性。

[Translation]

Primary objective: To evaluate the efficacy of mehuatinib compared with gefitinib as first-line treatment for advanced non-squamous non-small cell lung cancer with EGFR sensitive mutations. Secondary objective: To evaluate the safety of mehuatinib compared with gefitinib as first-line treatment for advanced non-squamous non-small cell lung cancer with EGFR sensitive mutations.

Start Date26 Mar 2020

Sponsor / Collaborator

Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.

[+1]

100 Clinical Results associated with Mefatinib

Login to view more data

100 Translational Medicine associated with Mefatinib

Login to view more data

100 Patents (Medical) associated with Mefatinib

Login to view more data

2

Literatures (Medical) associated with Mefatinib

01 Sep 2023·Cancer communications (London, England)

A phase II study on Mefatinib as first-line treatment of patients with advanced non-small-cell lung cancer harboring uncommon EGFR mutations.

Letter

Author: Yang, Mei ; Ren, Shengxiang ; Yu, Bing ; Zhu, Chaonan ; Fan, Yun ; Tian, Panwen ; Lv, Dongqing ; Miao, Liyun ; Song, Yong ; Cao, Liming ; Wang, Kai ; Zhao, Xin ; Zhou, Chengzhi ; Wang, Pingli ; Xu, June ; Li, Yuping

Signal Transduction and Targeted TherapyQ1 · MEDICINE

Mefatinib as first-line treatment of patients with advanced EGFR-mutant non-small-cell lung cancer: a phase Ib/II efficacy and biomarker study

Q1 · MEDICINE

ArticleOA

Author: Zhou, Jianying ; Li, Yuping ; Wang, Kai ; Lv, Dongqing ; Ding, Liren ; Zhou, Jianya ; Hong, Wei ; Yang, Lingge ; Zhang, Dongqing ; Chen, Youfei ; Wang, Pingli ; He, Susu

AbstractEGFR inhibitors have revolutionized the treatment of advanced non-small-cell lung cancer (NSCLC). Mefatinib is a novel, bioavailable, second-generation, irreversible pan-EGFR inhibitor. This phase Ib/II open-label, single-arm, multi-center study investigated the efficacy, safety, biomarker, and resistance mechanisms of mefatinib in the first-line treatment of patients with advanced EGFR-mutant NSCLC. This study included 106 patients with EGFR-mutant stage IIIB-IV NSCLC who received first-line mefatinib at a daily dose of either 60 mg (n = 51) or 80 mg (n = 55). The primary endpoint was progression-free survival (PFS). Secondary endpoints were overall response rate (ORR), disease control rate (DCR), overall survival (OS), and safety. The cohort achieved an ORR of 84.9% and DCR of 97.2%. The median PFS was 15.4 months and the median OS was 31.6 months. Brain metastasis was detected in 29% of patients (n = 31) at diagnosis and demonstrated an ORR of 87.1%, PFS of 12.8 months, and OS of 25.2 months. Adverse events primarily involved skin and gastrointestinal toxicities, which were well-tolerated and manageable. Analyses of mutation profiles were performed using targeted sequencing of plasma samples at baseline, first follow-up 6 weeks from starting mefatinib therapy (F1), and at progression. Patients with concurrent TP53 mutations had comparable PFS as wild-type TP53 (14.0 vs 15.4 months; p = 0.315). Furthermore, circulating tumor DNA clearance was associated with longer PFS (p = 0.040) and OS (p = 0.002). EGFR T790M was the predominant molecular mechanism of mefatinib resistance (42.1%, 16/38). First-line mefatinib provides durable PFS and an acceptable toxicity profile in patients with advanced EGFR-mutant NSCLC.

100 Deals associated with Mefatinib

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer	NDA/BLA	China	Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.	11 May 2024
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	China	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	26 Mar 2020
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	China	Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.	26 Mar 2020
EGFR positive non-small cell lung cancer	Preclinical	China	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	11 May 2017
Advanced Lung Non-Small Cell Carcinoma	Discovery	China	Suzhou Maitai Bio-Technology Co., Ltd.	30 Mar 2019
Advanced Lung Non-Small Cell Carcinoma	Discovery	China	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	30 Mar 2019
Metastatic Non-Squamous Non-Small Cell Lung Carcinoma	Discovery	China	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	30 Mar 2019
Metastatic Non-Squamous Non-Small Cell Lung Carcinoma	Discovery	China	Suzhou Maitai Bio-Technology Co., Ltd.	30 Mar 2019
Advanced Malignant Solid Neoplasm	Discovery	China	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	09 Oct 2015
Advanced Malignant Solid Neoplasm	Discovery	China	Suzhou Maitai Bio-Technology Co., Ltd.	09 Oct 2015

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CTR20192297 (phase III, ASCO2024)	Phase 3	EGFR positive non-small cell lung cancer First line EGFR sensitizing mutation-positive \| TP53 mutations	336	Mefatinib 60 mg	(vblvruwphj) = watyciqrki edakynuhqw (mrykylmade ) View more	Positive	24 May 2024
				Gefitinib 250 mg	(vblvruwphj) = rydcghqjil edakynuhqw (mrykylmade ) View more
CTR20190110 (ASCO2022) Manual	Phase 2	EGFR-mutated non-small Cell Lung Cancer First line EGFR Mutation	21	Mefatinib	(aezdirdhbg) = aoncjigxqz ephvaxnlmz (iqattiecgh, 63.66 - 96.95) View more	Positive	02 Jun 2022
				Mefatinib (mutation in G719X)	(aezdirdhbg) = nfavsdmzso ephvaxnlmz (iqattiecgh, 71.31 - 99.85) View more
WCLC2021	Not Applicable	Non-Small Cell Lung Cancer First line	71	Mefatinib 60mg	(mxwkvevnnr) = egprgpvzef bhdcpxcqhb (arjqowwffx ) View more	-	28 Jan 2021