Delving into the Latest Updates on Sutetinib Maleate with Synapse

This trial is a single-center, open-label, single-dose clinical pharmacokinetic study. It aims to evaluate the in vivo absorption, material balance and biotransformation pathways of a single oral dose of 80 mg/100 μCi [14C] sutetinib maleate suspension in healthy Chinese male subjects, so as to reveal the overall pharmacokinetics and safety of sutetinib maleate in humans and provide a reference for the rational use of the drug in clinical practice.

Start Date01 Aug 2023

Sponsor / Collaborator

Jiangsu Maidu Pharmaceutical Research and Development Co., Ltd.

[+1]

CTR20223110 / Active, not recruitingPhase 2

一项评价马来酸苏特替尼胶囊治疗EGFR突变阳性的局部晚期或转移性非小细胞肺癌患者的有效性和安全性多中心、单臂、Ⅱ期临床研究

[Translation] A multicenter, single-arm, phase II clinical study to evaluate the efficacy and safety of sutetinib maleate capsules in the treatment of patients with locally advanced or metastatic non-small cell lung cancer with EGFR mutation-positive

主要目的：评价马来酸苏特替尼胶囊治疗EGFR突变阳性的局部晚期或转移性NSCLC患者的有效性。次要目的：评价马来酸苏特替尼胶囊治疗EGFR突变阳性的局部晚期或转移性NSCLC患者的安全性。

[Translation]

Primary objective: To evaluate the efficacy of sutetinib maleate capsules in the treatment of patients with locally advanced or metastatic NSCLC who are EGFR mutation-positive. Secondary objective: To evaluate the safety of sutetinib maleate capsules in the treatment of patients with locally advanced or metastatic NSCLC who are EGFR mutation-positive.

Start Date30 Mar 2023

Sponsor / Collaborator

Jiangsu Maidu Pharmaceutical Research and Development Co., Ltd.

[+1]

100 Clinical Results associated with Sutetinib Maleate

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100 Translational Medicine associated with Sutetinib Maleate

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100 Patents (Medical) associated with Sutetinib Maleate

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2

Literatures (Medical) associated with Sutetinib Maleate

01 Jun 2024·Investigational New Drugs

The effect of food on the pharmacokinetics of Sutetinib maleate capsule, an irreversible EGFR tyrosine kinase inhibitor, in healthy Chinese subjects

Article

Author: Lin, Hui ; Yang, Yuanxun ; Cao, Bei ; Zhang, Yuqiang ; Huang, Lei ; Cao, Sumin ; Li, Juan ; Zhao, Yu ; Jiang, Huanhuan ; Ma, Tingting ; Geng, Yan

Sutetinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and showed favorable efficacy and safety in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harbouring nondrug-resistant rare EGFR mutations. To evaluate the potential food effect, eighteen healthy Chinese subjects were enrolled in a single-centre, randomized, open-label, two-sequence, two-period crossover study. Sutetinib was administered as a single oral 100 mg under fasting or fed conditions, and pharmacokinetic sampling was performed following each dose and analysed by a validated liquid chromatography/mass spectrometry method. Safety and tolerability were also evaluated. Food intake slightly decreased maximum plasma concentration (C_max) and area under the plasma concentration-time curve from time 0 to infinity (AUC_0 - inf) of sutetinib (geometric least-squares mean [GLSM] ratio, 80.94% and 86.11%; 90% confidence interval [CI], 68.43-95.72 and 75.88-97.73) and its active metabolite sutetinib N-Oxide (GLSM ratio, 75.58% and 84.00%; 90% CI, 65.69-86.95 and 75.42-93.56), respectively. In addition, the time to maximum plasma concentration (T_max) of both sutetinib and its metabolite has been prolonged by 2 h under fed conditions. A total of 31 adverse events (AEs) occurred during the study, with no serious adverse events (SAE) reported, and no obvious difference was observed between the fasting and fed groups. Our results demonstrated that a high-fat and high-calorie diet caused a significant delay in drug absorption and a marginal reduction in drug exposure. Sutetinib was generally well tolerated in healthy Chinese subjects. (This trial was registered at http://www.chinadrugtrials.org.cn . The registration No. is CTR20201933, and the date of registration is 2020-10-16).

01 Oct 2020·Biomedical ChromatographyQ4 · MEDICINE

Simultaneous determination of sutetinib and its active metabolite sutetinib N‐oxide in human plasma by liquid chromatography–tandem mass spectrometry: Evaluation of plasma stability

Q4 · MEDICINE

Article

Author: Chen, Xiaoyan ; Li, Ranran ; Tang, Chongzhuang ; Zhang, Yuqiang ; Cao, Sumin ; Qiu, Yanan

AbstractFrom the point of view of drug efficacy and safety, pharmacokinetic profiles of both In this work, a sensitive and reliable liquid chromatographic–tandem mass spectrometric method was established for simultaneous determination of sutetinib and N‐oxide metabolite (SNO) in human plasma and further applied to a pharmacokinetic study. Analytes were extracted from plasma samples (100 μl) via acetonitrile‐induced protein precipitation and separated on a C18 column using ammonium acetate with ammonium hydroxide and acetonitrile as the mobile phase. Positive electrospray ionization was carried out through multiple reaction monitoring with transitions of m/z 440.2 → 367.1 and 446.2 → 367.1 for sutetinib and SNO, respectively. The method was linear within the concentration range of 0.5–100 ng/ml for both analytes. The precision, accuracy, selectivity, recovery and matrix effect of this method all met the requirements of bioanalytical guidance. In addition, a plasma stability assessment demonstrated unexpected results. Sutetinib was prone to form covalent conjugates with plasma albumin in vitro. The degree of covalent binding increased with increasing temperature, resulting in a significant decrease in its plasma concentrations. However, SNO could not easily bind with albumin owing to steric hindrance or electronegativity. Furthermore, sutetinib and SNO remained stable when blood and plasma samples were kept on wet ice. The validated method was successfully employed for the pharmacokinetic evaluation of sutetinib in patients with advanced malignant solid tumors.

100 Deals associated with Sutetinib Maleate

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
EGFR-mutated non-small Cell Lung Cancer	Phase 2	CN	SZYY Group Pharmaceutical Ltd.	30 Mar 2023
EGFR-mutated non-small Cell Lung Cancer	Phase 2	CN	Jiangsu Maidu Pharmaceutical Research and Development Co., Ltd.	30 Mar 2023
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	US	Suzhou Teligene Ltd.	01 Sep 2022
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	CN	Suzhou Teligene Ltd.	01 Sep 2022
EGFR positive non-small cell lung cancer	Phase 2	CN	Jiangsu Maidu Pharmaceutical Research and Development Co., Ltd.	15 Jul 2019
EGFR positive non-small cell lung cancer	Phase 2	CN	SZYY Group Pharmaceutical Ltd.	15 Jul 2019
Advanced Malignant Solid Neoplasm	Preclinical	CN	SZYY Group Pharmaceutical Ltd.	06 Jan 2017
Advanced Malignant Solid Neoplasm	Preclinical	CN	Jiangsu Maidu Pharmaceutical Research and Development Co., Ltd.	06 Jan 2017

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CTR20190681 (ASCO2023) Manual	Phase 2	EGFR-mutated non-small Cell Lung Cancer EGFR Mutation	30	Sutetinib 80 mg/day	(rjxhxcksoh) = dpfqiqtxbb eyqeiodduq (nanlkefnzt ) View more	Positive	26 May 2023
				Sutetinib 64 mg/day	(rjxhxcksoh) = yhvldfxaix eyqeiodduq (nanlkefnzt ) View more