DOTATATE

Product Name: DOTATATE

Cas No:177943-88-3

Molar Mass: 1435.62

Chemical Formula: C65H90N14O19S2

Synonyms: Oxodotreotide

IUPAC Name: (2S,3R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-19-[[(2R)-3-phenyl-2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]propanoyl]amino]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-hydroxybutanoic acid

SMILES: C[C@H]([C@H]1C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)[C@@H](CC5=CC=CC=C5)NC(=O)CN6CCN(CCN(CCN(CC6)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)O

InChIKey: QVFLVLMYXXNJDT-CSBVGUNJSA-N

InChI: InChI=1S/C65H90N14O19S2/c1-38(80)56-64(96)73-51(63(95)75-57(39(2)81)65(97)98)37-100-99-36-50(72-59(91)47(28-40-10-4-3-5-11-40)68-52(83)32-76-20-22-77(33-53(84)85)24-26-79(35-55(88)89)27-25-78(23-21-76)34-54(86)87)62(94)70-48(29-41-15-17-43(82)18-16-41)60(92)71-49(30-42-31-67-45-13-7-6-12-44(42)45)61(93)69-46(58(90)74-56)14-8-9-19-66/h3-7,10-13,15-18,31,38-39,46-51,56-57,67,80-82H,8-9,14,19-30,32-37,66H2,1-2H3,(H,68,83)(H,69,93)(H,70,94)(H,71,92)(H,72,91)(H,73,96)(H,74,90)(H,75,95)(H,84,85)(H,86,87)(H,88,89)(H,97,98)/t38-,39-,46+,47-,48+,49-,50+,51+,56+,57+/m1/s1

Storage: Sealed storage, away from moisture

Sequence: {DOTA}-{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Thr-Cys-Thr (Disulfide bridge:Cys2-Cys7)

Purity: 99%

Application:

DOTATATE is a DOTA-conjugated somatostatin analog widely used in radionuclide-based biomedical research. By incorporating the macrocyclic chelator DOTA, DOTATATE can form stable complexes with selected diagnostic or therapeutic radionuclides, making it suitable for positron emission tomography (PET) imaging studies and peptide receptor radionuclide research. Its strong relevance to somatostatin receptor–targeted systems supports applications in receptor-binding evaluation, radiolabeling method development, biodistribution studies, and targeted molecular imaging research. DOTATATE is also an important peptide scaffold for the design and investigation of Radionuclide-Drug Conjugates (RDCs), where peptide-mediated receptor recognition is combined with radionuclide payload delivery. In pharmaceutical and translational research, DOTATATE provides a valuable platform for studying targeted radiopharmaceutical design, peptide chelation chemistry, receptor-selective delivery strategies, and imaging-guided therapeutic concepts. Its well-defined peptide-chelator structure makes it a useful reference compound for developing and optimizing somatostatin receptor–directed radionuclide conjugates.

Current Research:

Current research on DOTATATE is strongly connected to the rapid development of somatostatin receptor–targeted imaging, peptide receptor radionuclide research, and radionuclide-drug conjugate design. As a DOTA-conjugated somatostatin analog, DOTATATE is valued because the DOTA chelator can coordinate medically relevant radionuclides, while the peptide portion supports selective interaction with somatostatin receptor–expressing biological systems, especially SSTR2-positive models. This dual structure makes DOTATATE a representative scaffold in modern radiopharmaceutical and theranostic research.

One major research direction is PET imaging using radiolabeled DOTATATE, particularly gallium-68-labeled DOTATATE. In molecular imaging studies, radiolabeled DOTATATE is used to evaluate somatostatin receptor expression, tumor heterogeneity, lesion detectability, and tracer biodistribution. Current work increasingly emphasizes quantitative imaging parameters, receptor-density assessment, and the use of PET/CT or PET/MRI data to support patient stratification and treatment-planning research. Reviews of neuroendocrine tumor theranostics continue to describe somatostatin receptor PET as a central tool for identifying receptor-positive lesions and guiding radionuclide-based strategies.

Another important area is peptide receptor radionuclide research using lutetium-177-labeled DOTATATE. In this context, DOTATATE functions as a receptor-targeting peptide carrier that can deliver beta-emitting radionuclides to SSTR-positive tissues. Research is not limited to conventional neuroendocrine tumor models; recent studies have explored DOTATATE-based PRRT concepts in additional somatostatin receptor–expressing tumors, including radioiodine-refractory differentiated thyroid carcinoma and medullary thyroid carcinoma. These studies reflect a broader trend: researchers are investigating whether SSTR-targeted radionuclide platforms may be extended beyond traditional indications when receptor expression is biologically relevant.

A growing research topic is alpha-particle therapy based on DOTATATE analogs, including actinium-225-labeled DOTATATE. Compared with beta-emitting systems, alpha-emitting radionuclides have high linear energy transfer and short tissue penetration ranges, which may support more localized radiation effects in receptor-positive tumor models. Recent systematic and translational research has examined the potential efficacy and toxicity profile of 225Ac-DOTATATE in metastatic neuroendocrine tumor settings, highlighting the increasing interest in next-generation radionuclide payloads for peptide-targeted delivery.

DOTATATE is also relevant to radionuclide-drug conjugate research. RDCs combine a targeting vector, a linker or chelator system, and a radionuclide payload. DOTATATE represents a peptide-based targeting module in this design logic. Current RDC research focuses on improving target selectivity, radionuclide-chelator stability, pharmacokinetics, tumor retention, clearance behavior, and dosimetry. Recent reviews describe RDCs as an expanding precision-medicine modality, with active investigation into target selection, payload choice, safety optimization, and translational development challenges.

At the molecular level, computational and structural studies are helping researchers understand how somatostatin analog radiopharmaceuticals interact with SSTR2. Molecular dynamics work has examined receptor-ligand interactions involving somatostatin analog biovectors and chelator-radionuclide components, supporting a more detailed understanding of binding behavior, receptor recognition, and structure-function relationships. This type of research may help guide the rational design of improved DOTATATE-related ligands with optimized affinity, stability, and biological distribution.

Current research also emphasizes personalization and image-guided optimization. Emerging studies are applying advanced imaging analysis, dosimetry, artificial intelligence, and multimodal data integration to predict treatment response and improve follow-up strategies in radionuclide therapy. These approaches may help researchers connect DOTATATE-based imaging signals with biological behavior, therapeutic response, and disease progression. Overall, DOTATATE remains an important reference compound and design platform in radiopharmaceutical science, supporting studies in PET imaging, PRRT, RDC development, alpha-emitter research, receptor biology, and theranostic workflow optimization."