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.

NCT06332053 / Not yet recruitingPhase 1

A Randomized, Open-label, Two-period, Self-controlled Study to Evaluate the Effect of Oral Rifampicin or Itraconazole on the Pharmacokinetics of SY-5007 Tablets in Healthy Subjects

This study is a single-center, open-lable and fixed sequence test conducted in healthy subjects to evaluate the pharmacokinetic effects of Itraconazole and Rifampicin on a single dose of SY-5007 Oral administration. It is planned to enroll 28 healthy subjects and assign them to two parallel test groups, Group A (SY-5007 combined with Itraconazole) and Group B (SY-5007 combined with Rifampicin).

Start Date01 Apr 2024

Sponsor / Collaborator

Shouyao Holdings (Beijing) Co. Ltd.

100 Clinical Results associated with SY-5007

100 Translational Medicine associated with SY-5007

100 Patents (Medical) associated with SY-5007

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 ; Li, Wei ; Xu, Chunwei ; Gao, Ge ; 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

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	CN	Shouyao Holdings (Beijing) Co. Ltd.	20 Jun 2023
Advanced Malignant Solid Neoplasm	Phase 2	CN	Shouyao Holdings (Beijing) Co. Ltd.	23 Apr 2021
Thyroid Cancer, Medullary	Phase 2	CN	Shouyao Holdings (Beijing) Co. Ltd.	23 Apr 2021

Clinical Result

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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	(qopdegmdwj) = uyuqltwimh qvapfwdrej (jfqfxnkcvy ) View more	Positive	04 Nov 2024
				SY-5007 (treatment-naïve)	(qopdegmdwj) = wbqmewnxpe qvapfwdrej (jfqfxnkcvy )
NCT05278364 (ASCO2024)	Phase 2	Advanced Malignant Solid Neoplasm \| Non-Small Cell Lung Cancer \| Thyroid Cancer, Medullary RET-fusion positive	105	SY-5007 160 mg twice daily	(ffmmjzktuo) = whwmggbtzd fftglkfghf (kbvvpjvgpq, 67.9 - 84.8) View more	Positive	24 May 2024
NCT05278364 (ASCO2023) Manual	Phase 1	RET fusion-positive Solid Tumors RET positive	60	SY-5007	(nqlnhgjtuh) = lkhopufbba lxtdntkkgu (mnvyoywrpe, 72.7 - 97.8) View more	Positive	31 May 2023
				SY-5007 (NSCLC+MTC)	(nqlnhgjtuh) = rlcahersxs lxtdntkkgu (mnvyoywrpe, 73.0 - 99.0) View more

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