177Lu-TATE-RGD in Patients With SSTR2 and Integrin αVβ3 Positive Tumors

Therapeutic Efficiency and Response to 177Lu-TATE-RGD in Patients With SSTR2 and Integrin αVβ3 Positive Tumors

Researchers has conducted extensive research on the treatment of neuroendocrine tumors with 177Lu-EB-TATE and the treatment of FAP-expressing tumors with 177Lu-EB-FAPI, and some researches have revealed 68Ga-TATE-RGD in imaging studies of neuroendocrine tumors to find that the dual-targeted tracer showed an increasing TBR, suggesting the tracer kinetic advantage of TATE-RGD; compared to the single-target tracer DOTATATE, the dual-target TATE-RGD probe has a clear advantage in detecting liver metastases of NETs, and it can be explored for potential therapeutic uses of TATE-RGD in future studies and used for related companion diagnostics in targeted radioisotope therapy (RLT).

Integrin αvβ3 is highly expressed in certain tumor cells and newly formed blood vessels, making it an ideal target for diagnosis and treatment of integrin αVβ3 positive tumors. 177Lu-TATE-RGD is a novel drug developed independently in China, providing an effective target for the treatment of integrin αVβ3 positive tumors. All patients underwent whole-body 68Ga-TATE-RGD PET/CT screening within one week and received a single intravenous injection of 1.48-3.33 GBq (40-100 mCi) 177Lu-TATE-RGD within one week. Blood samples were collected from the vein in 1-2 mL volumes at 5 minutes, 3 hours, 24 hours, 72 hours, and 168 hours after injection to measure radioactivity. Then, whole-body planar and SPECT/CT imaging was performed at 3, 24, 48, 72, 96, 120, and 168 hours after the injection of 177Lu-TATE-RGD. The in vivo radiation dose of 177Lu-TATE-RGD was analyzed and calculated, and the therapeutic effect and response were evaluated.

Inclusion Criteria:

• patients with clear pathological diagnosis and ineffective or progressing clinical conventional treatment;
• tumor lesions with high SSTR2 and RGD untake confirmed on 68Ga-TATE-RGD PET/CT within one week before the injection of 177Lu-TATE-RGD;
• signed written consent.

Exclusion Criteria:

• the exclusion criteria were a serum creatinine level of more than 150 μmol per liter, a hemoglobin level of less than 10.0 g/dl, a white-cell count of less than 4.0× 109/L, a platelet count of less than 100 × 109/L, a total bilirubin level of more than 3 times the upper limit of the normal range and a serum albumin level of more than 3.0 g per deciliter, cardiac insufficiency including carcinoid heart valve disease, a severe allergy or hypersensitivity to radiographic contrast material, claustrophobia;
• any medical condition that in the opinion of the investigator may significantly interfere with study compliance.