APN x αvβ3

Ia期： 主要目的：评估中国健康成人受试者接受单次静脉给予68Ga-HX01注射液后的安全性。 次要目的：探索中国健康成人受试者接受单次静脉给予68Ga-HX01注射液后的生物分布（PET显像）、人体的辐射剂量和药代动力学特征。 Ib期： 主要目的：评估恶性实体瘤患者接受单次静脉给予68Ga-HX01注射液后的安全性。 次要目的：探索恶性实体瘤患者接受单次静脉给予68Ga-HX01注射液后的生物分布（PET显像）。 探索性目的：探索在恶性实体瘤患者中单次静脉给予68Ga-HX01注射液后的肿瘤显像特点。

This is a single-center, open Phase I clinical study, consisting of two parts: a Phase Ia study in healthy adult subjects and a Phase Ib study in patients with malignant solid tumors.

Angiogenesis is essential in tumor growth, proliferation, progression, and metastasis. Overexpression of aminopeptidase N (APN/CD13) and/or integrin αvβ3 in endothelial and tumor cells is an essential marker of tumor-associated angiogenesis. It is highly expressed in malignant tissues such as ovarian and pancreatic cancer but less expressed in normal tissues. Therefore, CD13 and αvβ3 are important targets for diagnosis and efficacy assessment in ovarian and pancreatic cancer. Single receptor targeting probes have many disadvantages, such as relatively low binding affinity, short tumor retention time, and low tumor uptake. RGD (Arg-Gly-Asp) and NGR (Asp-Gly-Arg) are recognized peptide sequences targeting CD13 or αvβ3. PET imaging with 68Ga-HX01, a radionuclide 68Ga labeled peptide isomer formed from RGD and NGR, can be helpful for targeted diagnosis and efficacy assessment of malignant tumors.
This project proposes to use 68Ga-HX01 PET imaging in the diagnosis and staging of malignant tumors, i.e., ovarian and pancreatic cancer, and to compare the diagnostic efficacy of 68Ga-HX01 with the pathology gold standard. And this study was conducted to compensate for the lack of value of 18F-FDG PET imaging for the diagnosis and staging of malignant tumors by comparing 68Ga-HX01 with the commonly used 18F-FDG PET imaging.