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

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100 Translational Medicine associated with Mefatinib

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100 Patents (Medical) associated with Mefatinib

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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

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer	NDA/BLA	CN	Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.	11 May 2024
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	CN	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	26 Mar 2020
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	CN	Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd.	26 Mar 2020
Advanced Lung Non-Small Cell Carcinoma	Preclinical	CN	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	30 Mar 2019
Advanced Lung Non-Small Cell Carcinoma	Preclinical	CN	Suzhou Maitai Bio-Technology Co., Ltd.	30 Mar 2019
Metastatic Non-Squamous Non-Small Cell Lung Carcinoma	Preclinical	CN	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	30 Mar 2019
Metastatic Non-Squamous Non-Small Cell Lung Carcinoma	Preclinical	CN	Suzhou Maitai Bio-Technology Co., Ltd.	30 Mar 2019
Non-squamous non-small cell lung cancer	Preclinical	CN	Suzhou Maitai Bio-Technology Co., Ltd.	20 Jun 2018
Advanced Malignant Solid Neoplasm	Preclinical	CN	Suzhou Maitai Bio-Technology Co., Ltd.	09 Oct 2015
Advanced Malignant Solid Neoplasm	Preclinical	CN	Hangzhou Huadong MEDICINE Group Pharmaceutical Research Institute Co., Ltd.	09 Oct 2015

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Clinical Result

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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	(eoggkjaetu) = ikxqcnqkyb vizwfylqab (ocvqnnegeb ) View more	Positive	24 May 2024
				Gefitinib 250 mg	(eoggkjaetu) = wpinjmnehm vizwfylqab (ocvqnnegeb ) View more
CTR20190110 (ASCO2022) Manual	Phase 2	EGFR-mutated non-small Cell Lung Cancer First line EGFR Mutation	21	Mefatinib	(djyxuvharx) = voynyinapy cavgmwfjtl (frswkuctpc, 63.66 - 96.95) View more	Positive	02 Jun 2022
				Mefatinib (mutation in G719X)	(djyxuvharx) = dxgidnwcre cavgmwfjtl (frswkuctpc, 71.31 - 99.85) View more
WCLC2021	Not Applicable	Non-Small Cell Lung Cancer First line	71	Mefatinib 60mg	(zgtbmsbmiz) = coqvclwtph qbwyfwckej (tghdwyccqw ) View more	-	28 Jan 2021