Delving into the Latest Updates on SY-5007 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

RET

Action

inhibitors

Mechanism

RET inhibitors(Tyrosine-protein kinase receptor RET inhibitors)

Therapeutic Areas

NeoplasmsRespiratory DiseasesEndocrinology and Metabolic Disease+ [1]

Active Indication

RET fusion-positive Non-Small Cell Lung CancerAdvanced Malignant Solid NeoplasmRET fusion-positive Adenocarcinoma of Lung+ [1]

Inactive Indication-

Originator Organization

Shouyao Holdings (Beijing) Co. Ltd.

Active Organization

Shouyao Holdings (Beijing) Co. Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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主要研究目的：评价单次口服SY-5007片对健康受试者QT/QTc间期的影响。次要研究目的： 1. 评价单次口服SY-5007片在健康人体内的药代动力学（PK）特征； 2. 评价莫西沙星400 mg单次给药后在健康受试者中的PK特征； 3. 评价单次口服SY-5007片对健康受试者其它ECG参数（HR、PR、QRS间期、T波形态和U波存在）的影响； 4. 以莫西沙星作为阳性对照，评价该项临床研究的灵敏度和可靠性；评价单次口服SY-5007片在健康人体内的安全性和耐受性。

[Translation]

Main study objectives: To evaluate the effect of a single oral administration of SY-5007 tablets on the QT/QTc interval in healthy subjects. Secondary study objectives: 1. To evaluate the pharmacokinetic (PK) characteristics of a single oral administration of SY-5007 tablets in healthy subjects; 2. To evaluate the PK characteristics of moxifloxacin 400 mg in healthy subjects after a single administration; 3. To evaluate the effect of a single oral administration of SY-5007 tablets on other ECG parameters (HR, PR, QRS interval, T wave morphology and U wave presence) in healthy subjects; 4. Using moxifloxacin as a positive control, evaluate the sensitivity and reliability of this clinical study; Evaluate the safety and tolerability of a single oral administration of SY-5007 tablets in healthy subjects.

Start Date25 Feb 2025

Sponsor / Collaborator

Shouyao Holdings (Beijing) Co. Ltd.

CTR20241152

/ Active, not recruitingPhase 1

[14C]SY-5007在中国健康成年男性受试者体内的物质平衡研究

[Translation] Study on the material balance of [14C]SY-5007 in healthy adult male subjects in China

主要目的：1.定量分析健康受试者口服[14C]SY-5007后全血与血浆总放射性、获得血浆中总放射性的PK参数，并考察全血和血浆中的总放射性分配情况。2.定量分析健康受试者口服[14C]SY-5007后排泄物中的总放射性，获得人体放射性回收率数据和主要排泄途径。3.鉴定健康受试者口服[14C]SY-5007后人体血、尿、粪样的代谢物谱和主要代谢产物，确定主要生物转化途径。次要目的：1.采用已验证的液相色谱质谱联用法（LS-MS/MS）方法定量分析血浆中SY-5007及其代谢物（如适用）的浓度，获得SY-5007及其代谢物（如适用）的PK参数。2.观察[14C]SY-5007单次给药后受试者的安全性。

[Translation]

Primary objectives: 1. Quantitatively analyze the total radioactivity in whole blood and plasma after oral administration of [14C]SY-5007 to healthy subjects, obtain the PK parameters of total radioactivity in plasma, and investigate the distribution of total radioactivity in whole blood and plasma. 2. Quantitatively analyze the total radioactivity in excreta after oral administration of [14C]SY-5007 to healthy subjects, obtain the data of human radioactivity recovery rate and the main excretion pathway. 3. Identify the metabolite profile and main metabolites of human blood, urine and feces samples after oral administration of [14C]SY-5007 to healthy subjects, and determine the main biotransformation pathway. Secondary objectives: 1. Quantitatively analyze the concentration of SY-5007 and its metabolites (if applicable) in plasma using a validated liquid chromatography-mass spectrometry (LS-MS/MS) method, and obtain the PK parameters of SY-5007 and its metabolites (if applicable). 2. Observe the safety of subjects after a single dose of [14C]SY-5007.

Start Date01 Jul 2024

Sponsor / Collaborator

Shouyao Holdings (Beijing) Co. Ltd.

NCT06352190

/ Not yet recruitingPhase 1

An Open-Label, Single-Center, Single-Dose, Phase I Study to Assess the Mass Balance of [14C] SY-5007 in Healthy Male Subjects in China

This is a single-center, open-label, non-randomized, single dose study in healthy male subjects designed to assess mass balance recovery, metabolite profile and metabolite identification of radio-labeled SY-5007 administered orally.

Start Date01 May 2024

Sponsor / Collaborator

Shouyao Holdings (Beijing) Co. Ltd.

100 Clinical Results associated with SY-5007

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100 Translational Medicine associated with SY-5007

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100 Patents (Medical) associated with SY-5007

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1

Literatures (Medical) associated with SY-5007

Signal Transduction and Targeted Therapy

First-in-human, phase 1 dose-escalation and dose-expansion study of a RET inhibitor SY-5007 in patients with advanced RET-altered solid tumors

Article

Author: Wang, Qiming ; Li, Zhihui ; Ye, Feng ; Liu, Jiaye ; Zhou, Caicun ; Song, Zhengbo ; Zhang, Yiping ; Wang, Yongsheng ; Xiong, Anwen ; Xu, Chunwei ; Gao, Ge ; Li, Wei ; Liu, Xijie ; Sun, Yinghui ; Huang, Dingzhi ; Zhou, Fei

AbstractOncogenic RET alteration is an important, tissue-agnostic therapeutic target across diverse cancers. We conducted a first-in-human phase 1 study on SY-5007, a potent and selective RET inhibitor, in patients with RET-altered solid tumors. Primary endpoints were safety, maximum tolerated dose (MTD), and recommended phase 2 dose (RP2D). Secondary endpoints included pharmacokinetics and preliminary anti-tumor activity. A total of 122 patients were enrolled (17 in dose-escalation phase and 105 in dose-expansion phase), including 91 with non-small cell lung cancer, 23 with medullary thyroid cancer, 7 with papillary thyroid cancer and 1 with gastric cancer. Treatment-related adverse events (TRAEs) were reported in 96.7% of patients, with the most common grade ≥ 3 TRAEs being hypertension (22.1%), diarrhea (16.4%), hypertriglyceridemia (6.6%), and neutropenia (6.6%). The exposure to SY-5007 was dose proportional. Among the 116 efficacy-evaluable patients, the overall objective response rate (ORR) was 57.8%, with 70.0% in treatment-naïve patients and 51.3% in previously treated patients. The median progression-free survival (PFS) was 21.1 months. Efficacy was observed regardless of tumor types and previous therapies. Biomarker analysis of 61 patients with circulating tumor DNA (ctDNA)-detectable RET alterations showed an ORR of 57.4% and median PFS of 13.8 months. Rapid ctDNA clearance of RET alteration correlated with faster responses and improved outcomes. In relapsed patients, off-target induced resistance was observed in 57.1% (12/21), with no on-target RET alterations identified. In conclusion, SY-5007 was well-tolerated and showed promising efficacy in patients with RET-altered solid tumors. Serial ctDNA monitoring may unveil treatment response and potential resistance mechanisms (NCT05278364).

100 Deals associated with SY-5007

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
RET fusion-positive Non-Small Cell Lung Cancer	Phase 3	China	Shouyao Holdings (Beijing) Co. Ltd.	20 Jun 2023
Advanced Malignant Solid Neoplasm	Phase 2	China	Shouyao Holdings (Beijing) Co. Ltd.	23 Apr 2021
RET fusion-positive Adenocarcinoma of Lung	Phase 2	China	Shouyao Holdings (Beijing) Co. Ltd.	23 Apr 2021
RET Mutation-Positive Medullary Thyroid Cancer	Phase 2	China	Shouyao Holdings (Beijing) Co. Ltd.	23 Apr 2021

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05278364 (Pubmed) Manual	Phase 1	RET mutation Solid Tumors	122	SY-5007	(eegdvaynhx) = ufwaxmzyju lmbmlathpt (dmndnoyilx ) View more	Positive	04 Nov 2024
				SY-5007 (treatment-naïve)	(eegdvaynhx) = qekfringcu lmbmlathpt (dmndnoyilx )
NCT05278364 (ASCO2024)	Phase 2	RET fusion-positive Adenocarcinoma of Lung \| Advanced Malignant Solid Neoplasm \| Non-Small Cell Lung Cancer \| RET fusion-positive Non-Small Cell Lung Cancer \| Thyroid Cancer, Medullary \| RET Mutation-Positive Medullary Thyroid Cancer RET-fusion positive	105	SY-5007 160 mg twice daily	(ekhfqhjdpm) = iguqzizkgx adljwkpyyv (zpgujvtaua, 67.9 - 84.8) View more	Positive	24 May 2024
NCT05278364 (ASCO 12023 \| ASCO 22023) Manual	Phase 1	RET fusion-positive Solid Tumors RET positive	60	SY-5007	(pmpramycyy) = qxfnsgkeql ubtipprvfd (nldrwlpqhu, 72.7 - 97.8) View more	Positive	31 May 2023
				SY-5007 (NSCLC+MTC)	(pmpramycyy) = lxglsvqbyk ubtipprvfd (nldrwlpqhu, 73.0 - 99.0) View more