Delving into the Latest Updates on FHND9041 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

FHND-9041

Target

EGFR T790M

Action

inhibitors

Mechanism

EGFR T790M inhibitors(Epidermal Growth Factor Receptor T790M inhibitors)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

metastatic non-small cell lung cancer

Inactive Indication

EGFR-mutated non-small Cell Lung Cancer

Originator Organization

Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.

Active Organization

Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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主要研究目的：1）考察男性健康受试者单次口服[14C]FHND9041后，全血和血浆中的分配情况和血浆总放射性的药代动力学；2）定量分析男性健康受试者口服[14C]FHND9041后，排泄物中的总放射性量，获得人体放射性的累计排泄率和主要排泄途径；3）采用已验证的液相色谱-串联质谱法（LC-MS/MS）定量分析血浆中的FHND9041及其主要代谢产物（如适用）的浓度，获得FHND9041及其主要代谢产物（如适用）的药动学参数；4）鉴定男性健康受试者口服[14C]FHND9041后人体内的主要代谢产物，确定主要生物转化途径和主要代谢产物（接近或大于10%总放射性AUC）。次要研究目的：评价[14C]FHND9041单次给药后健康受试者的安全性。

[Translation]

The main study objectives are: 1) to investigate the distribution of [14C]FHND9041 in whole blood and plasma and the pharmacokinetics of total radioactivity in plasma after a single oral administration of [14C]FHND9041 to male healthy subjects; 2) to quantitatively analyze the total radioactivity in excreta after oral administration of [14C]FHND9041 to male healthy subjects, and obtain the cumulative excretion rate and main excretion pathway of radioactivity in the human body; 3) to quantitatively analyze the concentration of FHND9041 and its main metabolites (if applicable) in plasma using a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method, and obtain the pharmacokinetic parameters of FHND9041 and its main metabolites (if applicable); 4) to identify the main metabolites in the human body after oral administration of [14C]FHND9041 to male healthy subjects, and to determine the main biotransformation pathways and main metabolites (close to or greater than 10% of the total radioactivity AUC). Secondary study objectives: to evaluate the safety of [14C]FHND9041 in healthy subjects after a single dose.

Start Date18 Aug 2023

Sponsor / Collaborator

Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.

CTR20230931

/ Active, not recruitingPhase 1

一项在中国健康男性受试者中评价多次服用伊曲康哗或利福平对单次服用FHND9041 胶囊的药代动力学特征影响的I期、开放、固定序列研究

[Translation] A Phase I, open-label, fixed-sequence study to evaluate the effects of multiple doses of itraconazole or rifampicin on the pharmacokinetic profile of a single dose of FHND9041 capsules in healthy Chinese male subjects

主要目的：在中国健康男性受试者中评价多次口服伊曲康对单次口服FHND9041 胶囊后的药代动力学 (PK)特征的影响。在中国健康男性受试者中评价多次口服利福平对单次口服 FHND9041胶囊后的 PK 特征的影响。次要目的：在中国健康男性受试者中评价多次口服伊曲康的同时单次口服FHND9041 胶囊后的安全性和耐受性。在中国健康男性受试者中评价多次口服利福平的同时单次口服FHND9041 胶囊后的安全性和耐受性

[Translation]

Primary objective: To evaluate the effect of multiple oral doses of itracon on the pharmacokinetic (PK) profile of FHND9041 capsules after a single oral dose in Chinese healthy male subjects. To evaluate the effect of multiple oral doses of rifampicin on the PK profile of FHND9041 capsules after a single oral dose in Chinese healthy male subjects. Secondary objective: To evaluate the safety and tolerability of multiple oral doses of itracon combined with a single oral dose of FHND9041 capsules in Chinese healthy male subjects. To evaluate the safety and tolerability of multiple oral doses of rifampicin combined with a single oral dose of FHND9041 capsules in Chinese healthy male subjects.

Start Date04 May 2023

Sponsor / Collaborator

Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.

CTR20230896

/ Active, not recruitingPhase 1

一项在中国健康男性受试者中评价食物对单次口服FHND9041 胶囊的药代动力学特征影响的开放、随机、单剂量、两周期交叉的 I期临床研究

[Translation] An open, randomized, single-dose, two-period crossover phase I clinical study to evaluate the effect of food on the pharmacokinetic characteristics of a single oral dose of FHND9041 capsules in healthy Chinese male subjects

主要目的：在中国健康男性受试者中评价高脂餐对单次口服 80 mg FHND9041的药代动力学(PK)特征的影响。次要目的：在空腹和高脂餐后状态下，在中国健康男性受试者中评价单次口服 80mg FHND9041后的安全性和耐受性。

[Translation]

Primary objective: To evaluate the effect of a high-fat meal on the pharmacokinetic (PK) profile of a single oral dose of 80 mg FHND9041 in healthy Chinese male subjects. Secondary objective: To evaluate the safety and tolerability of a single oral dose of 80 mg FHND9041 in healthy Chinese male subjects in the fasting and high-fat meal states.

Start Date09 Apr 2023

Sponsor / Collaborator

Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.

100 Clinical Results associated with FHND9041

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100 Translational Medicine associated with FHND9041

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100 Patents (Medical) associated with FHND9041

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Literatures (Medical) associated with FHND9041

BMC Pharmacology & Toxicology

Effect of CYP3A4 inhibitor and induction on the pharmacokinetics and safety of FHND9041, a novel EGFR T790M inhibitor, in healthy Chinese

Article

Author: Zhu, Yongqiang ; Gong, Jian ; Lu, Chang ; Xie, Yunqiu ; Chen, Rongzhen ; Cheng, Dongmei ; Zhou, Huan ; Shang, Minghong

BACKGROUND:

Non-small cell carcinoma is the main pathologic type of lung cancer, and a large number of clinical trials have shown that epidermal growth factor receptor tyrosinase inhibitors exhibit superior clinical efficacy and lower toxicity compared with chemotherapy. FHND9041 is a new irreversible EGFR T790M mutation-selective small molecule kinase inhibitor, a third-generation EGFR inhibitor developed by Nanjing Chuangte Pharmaceutical Technology Co., Ltd. The aim of this study was to evaluate the effects of oral Itraconazole capsules and oral Rifampicin capsules on the pharmacokinetic profile and safety and tolerability of a single oral dose of FHND9041 capsules in healthy Chinese male subjects.

PATIENTS AND METHODS:

This study employed a single-center, open-label, fixed-sequence design, comprising two parallel groups: Group 1 received FHND9041 40 mg in combination with Itraconazole, while Group 2 received Rifampicin in combination with FHND9041 80 mg. Each group enrolled 16 subjects for a two-period study, with the first period involving monotherapy and the second period involving co-administration. All subjects participating in this clinical trial were healthy adult Chinese males.

RESULTS:

In healthy subjects, after a single oral administration of 40 mg FHND9041 capsules, the corrected geometric mean ratios (90% confidence intervals) of FHND9041 C_max, AUC_0 - last, and AUC_0 - inf when co-administered with itraconazole capsules compared to the monotherapy phase were 111.46% (103.26 - 120.30%), 169.53% (156.21 - 183.99%), and 168.25% (156.26 - 181.15%), respectively. The 90% confidence interval for C_max fell within the 80-125% range, while the 90% confidence intervals for both AUC_0 - last and AUC_0 - inf exceeded the 80-125% range. Following a single oral dose of 80 mg FHND9041 capsules, the adjusted geometric mean ratios (90% confidence intervals) of C_max, AUC_0 - last, and AUC_0 - inf for FHND9041 during co-administration with Rifampicin compared to monotherapy were 52.12% (41.95 - 64.74%), 16.47% (13.34 - 20.31%), and 16.51% (13.56 - 20.09%), respectively. The 90% confidence intervals for C_max, AUC_0 - last, and AUC_0 - inf all fell outside the 80 - 125% range. No serious adverse events occurred during the trial.

CONCLUSIONS:

Co-administration with Rifampicin significantly reduced the exposure of FHND9041. Therefore, it is recommended to avoid co-administration of FHND9041 with Rifampicin and other potent CYP3A4 inducers. Conversely, co-administration with Itraconazole significantly increased the total exposure of FHND9041. Caution is advised when FHND9041 is co-administered with Itraconazole or other strong CYP3A4 inhibitors. Close monitoring of tolerability during co-administration is essential, and dose reduction may be necessary if required. FHND9041 capsules demonstrated good safety and tolerability when used alone or in combination with strong CYP3A4 inhibitors or inducers.

TRIAL REGISTRATION:

Registered 03/27/2023 ( http://www.chinadrugtrials.org.cn/index.html , CTR202300931).

100 Deals associated with FHND9041

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 3	China	Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.	01 Aug 2021
EGFR-mutated non-small Cell Lung Cancer	Phase 2	China	Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.	27 Jun 2019

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AACR2023 Manual	Phase 1/2	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma EGFR Mutation	124	FHND9041 80mg (First-line )	ihipnrdghu(ypmnjagqpz) = nhsuvyhfnq onnhqudrht (hauwdiuoyt ) View more	Positive	14 Apr 2023
				FHND9041 40mg (Second/Third-line T790M+ )	ihipnrdghu(ypmnjagqpz) = sfuhrgzkmb onnhqudrht (hauwdiuoyt ) View more