DOTA-TATE를 이용한 SSTR 표적 테라노스틱스: 분자 수준의 이해와 향후 전망

초록

Neuroendocrine tumors (NETs) are heterogeneous malignancies with an increasing incidence,while early diagnosis and standardized staging remain challenging. Somatostatin receptors (SSTRs) are typicallyoverexpressed in well-differentiated NETs. However, SSTR expression often varies significantly across patients andeven within individual tumors, challenging patient stratification and the prediction of treatment response. To addressthis limitation, theranostic strategies combine molecular imaging with peptide receptor radionuclide therapy (PRRT),enabling non-invasive evaluation of SSTR expression and personalized treatment planning. Among various SSTRtargetingligands, [DOTA0, Tyr3]-octreotate (DOTA-TATE) has established itself in clinical practice, due to its highaffinity for SSTR2 and its compatibility with both diagnostic and therapeutic radioisotopes. This review describes themolecular characteristics of DOTA-TATE, the structural mechanisms underlying its SSTR selectivity, followed byrepresentative diagnostic (68Ga, 64Cu, and 44Sc) and therapeutic (177Lu, 90Y, 225Ac, and 212Pb) radionuclides applied toDOTA-TATE, along with their physical characteristics and clinical evidence. It also discusses the current limitationsof DOTA-TATE and highlights recent strategies to overcome them for developing next-generation SSTR-targetingligands for improved theranostics applications.

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