177 Lu-DOTATATE for the treatment of gastroenteropancreatic neuroendocrine tumors

Das, Satya; Al-Toubah, Taymeyah; El-Haddad, Ghassan; Strosberg, Jonathan

doi:10.1080/17474124.2019.1685381

Cited by 135Neuroendocrine Tumor Research AdvancesRadiopharmaceutical Chemistry and ApplicationsPeptidase Inhibition and Analysis

177 Lu-DOTATATE for the treatment of gastroenteropancreatic neuroendocrine tumors

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Das, Satya, Al-Toubah, Taymeyah, El-Haddad, Ghassan, Strosberg, Jonathan·2019·Expert Review of Gastroenterology & Hepatology

DOI 10.1080/17474124.2019.1685381PMC PMC7227421

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Abstract

Introduction: 177Lutetium-[DOTA°,Tyr3]octreotate (177Lu-DOTATATE) is a type of peptide receptor radionuclide therapy that garnered FDA approval in January 2018 for the treatment of somatostatin receptor-positive gastroenteropancreatic (GEP) neuroendocrine tumor (NET) patients. The therapy approval was based on findings from the randomized international phase III NETTER-1 trial as well as outcome data from a large European registry. The mechanism of the drug stems directly from its structure: a somatostatin analog (octreotate) selectively binding to somatostatin receptor expressing cells and being internalized, along with a chelated beta-emitting isotope 177Lu.Areas Covered: Herein we describe the pharmacology, clinical efficacy and adverse event data from prospective and retrospective studies with 177Lu-DOTATATE. We discuss the role of 177Lu-DOTATATE within the current treatment landscape for GEP NET patients.Expert Opinion: 177Lu-DOTATATE represents a unique addition to the treatment armamentarium for GEP NETs because of its potential to elicit tumor cytoreduction, which is rare among other existing treatment options, and prolonged disease control. Where 177Lu-DOTATATE fits into the treatment sequence for GEP NET patients remains an area of active investigation.

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177Lu-DOTATATE is used to treat neuroendocrine tumors.
“An excellent example is 177Lu-DOTATATE, a radiolabelled somatostatin analogue, used to treat neuroendocrine tumors (NETs) [91].”
From Radiopharmaceuticals: navigating the frontier of precision medicine and therapeutic innovation (2024) · cites this paper as [91]

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PRRT: Defining the Paradigm Shift to Achieve Standardization and Individualization
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Peptide Receptor Radionuclide Therapy (PRRT) in Patients with Progressive Grade 3 Neuroendocrine Neoplasms (NEN)
Zhang, J., Kulkarni, H., Singh, A., Niepsch, K., Müeller, D., & Baum, R. P. (2019) · Journal of Nuclear Medicine · Cited by 2 · see citing works
The failure of clinical factors to predict long-term toxicity after PRRT in >800 patients - Is a genetic screen needed?
Bodei, L., Kidd, M. S., Paganelli, G., Grana, C. M., Drozdov, I. A., Cremonesi, M., & Modlin, I. M. (2014) · Journal of Nuclear Medicine · Cited by 1 · see citing works

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[36]Strosberg J, Wolin E, Chasen B, Health-related quality of life in patients with progressive midgut neuroendocrine tumors treated with (177)Lu-Dotatate in the phase III NETTER-1 trial. J Clin Oncol. 2018; 36(25): 2578– 2584. 29878866 PMC6366953 •• This publication focused on the QOL endpoints examined in the NETTER-1 study. It highlighted the QOL improvements seen with the PRRT arm compared to the high dose octreotide arm across nearly every patient domain tested in the study.

Sorted by citations

177Lu-Dotatate plus long-acting octreotide versus high‑dose long-acting octreotide in patients with midgut neuroendocrine tumours (NETTER-1): final overall survival and long-term safety results from an open-label, randomised, controlled, phase 3 trial
Strosberg, J. R., Caplin, M. E., Kunz, P. L., Ruszniewski, P. B., Bodei, L., Hendifar, A., Mittra, E., Wolin, E. M., Yao, J. C., Pavel, M. E., et al. (2021) · The Lancet Oncology · doi:10.1016/s1470-2045(21)00572-6 · Cited by 605 · see citing works
Self-citation
Targeted α -Emitter Therapy with 212 Pb-DOTAMTATE for the Treatment of Metastatic SSTR-Expressing Neuroendocrine Tumors: First-in-Humans Dose-Escalation Clinical Trial
Delpassand, E. S., Tworowska, I., Esfandiari, R., Torgue, J., Hurt, J., Shafie, A., & Núñez, R. (2022) · Journal of Nuclear Medicine · doi:10.2967/jnumed.121.263230 · Cited by 199 · see citing works
“Food and Drug Administration for patients with SSTR-expressing gastroenteropancreatic NETs (5).”
Background
Targeted alpha therapy: progress in radionuclide production, radiochemistry, and applications.
Nelson, B. J. B., Andersson, J. D., & Wuest, F. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics13010049 · Cited by 194 · see citing works
“Clinical success has been demonstrated with the β− emitters 90Y and 131I conjugated with anti-CD20 monoclonal antibodies in follicular B-cell non-Hodgkin lymphoma [6], 177Lu-labeled prostate-specific membrane antigen (PSMA) peptides in metastatic, castrationresistant prostate cancer (CRPC) and 177Lu-DOTATATE for neuro…”
Background
Peptide–drug conjugate-based novel molecular drug delivery system in cancer
Zhu, Y., Tang, K., & Lv, J. (2021) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2021.07.001 · Cited by 157 · see citing works
Radiopharmaceuticals: navigating the frontier of precision medicine and therapeutic innovation
Dhoundiyal, S., Srivastava, S., Kumar, S., Singh, G., Ashique, S., Pal, R., Mishra, N., & Taghizadeh-Hesary, F. (2024) · European Journal of Medical Research · doi:10.1186/s40001-023-01627-0 · Cited by 144 · see citing works
“An excellent example is 177 Lu-DOTATATE, a radiolabelled somatostatin analogue, used to treat neuroendocrine tumors (NETs) [91].”
Background
Drug conjugate-based anticancer therapy - Current status and perspectives
Yang, Y., Wang, S., Ma, P., Jiang, Y., Cheng, K., Yu, Y., Jiang, N., Miao, H., Tang, Q., Liu, F., et al. (2022) · Cancer Letters · doi:10.1016/j.canlet.2022.215969 · Cited by 101 · see citing works
Peptide-Drug Conjugates: A New Hope for Cancer Management
Chavda, V. P., Solanki, H. K., Davidson, M., Apostolopoulos, V., & Bojarska, J. (2022) · Molecules · doi:10.3390/molecules27217232 · Cited by 100 · see citing works
Peptide Drug Conjugates and Their Role in Cancer Therapy
Heh, E., Allen, J. C., Ramirez, F., Lovasz, D., Fernandez, L., Hogg, T., Riva, H. R., Holland, N. A., & Chacon, J. A. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24010829 · Cited by 97 · see citing works
“DOTA-TATE is used to treat somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEPNETs) [16].”
Background
Peptide-drug conjugates: A new paradigm for targeted cancer therapy
Wang, M., Liu, J., Xia, M., Yin, L., Zhang, L., Liu, X., & Yu, C. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116119 · Cited by 88 · see citing works
Strategies to improve the physicochemical properties of peptide-based drugs
Lee, M. F., & Poh, C. L. (2023) · Pharmaceutical Research · doi:10.1007/s11095-023-03486-0 · Cited by 87 · see citing works
Progress and Future Directions with Peptide-Drug Conjugates for Targeted Cancer Therapy
Lindberg, J., Nilvebrant, J., Nygren, P., & Lehmann, F. (2021) · Molecules · doi:10.3390/molecules26196042 · Cited by 72 · see citing works
“PDCs targeting peptide hormone receptors that are overexpressed on tumor cells are another mechanism for delivering a cytotoxic payload into the tumor [3].”
BackgroundInfluential
Advances in peptide-based drug delivery systems
Guo, S., Wang, J., Wang, Q., Wang, J., Qin, S., & Li, W. (2024) · Heliyon · doi:10.1016/j.heliyon.2024.e26009 · Cited by 65 · see citing works
Therapeutic proteins: developments, progress, challenges, and future perspectives
Kumar, V., Barwal, A., Sharma, N., Mir, D. S., Kumar, P., & Kumar, V. (2024) · 3 Biotech · doi:10.1007/s13205-024-03958-z · Cited by 62 · see citing works
Learn from antibody–drug conjugates: consideration in the future construction of peptide-drug conjugates for cancer therapy
Wu, M., Huang, W., Yang, N., & Liu, Y. (2022) · Experimental Hematology and Oncology · doi:10.1186/s40164-022-00347-1 · Cited by 59 · see citing works
“a chelating molecule (DOTA), and a beta-emitting radioisotope (177Lu), which is the first therapeutic PDC developed by Novartis [61].”
Background
Risk of Bowel Obstruction in Patients with Mesenteric or Peritoneal Disease Receiving Peptide Receptor Radionuclide Therapy
Strosberg, J., Al‐Toubah, T., Pellè, E., Smith, J. J., Haider, M., Hutchinson, T., Fleming, J. B., & El-Haddad, G. E. (2020) · Journal of Nuclear Medicine · doi:10.2967/jnumed.120.242875 · Cited by 58 · see citing works
“Radiolabeled somatostatin analogs have developed into an important treatment option for patients with progressive, well-differentiated neuroendocrine tumors (NETs) (1).”
BackgroundSelf-citation
Peptide-Drug Conjugates: Design, Chemistry, and Drug Delivery System as a Novel Cancer Theranostic
Rizvi, S. F. A., Zhang, L., Zhang, H., & Fang, Q. (2024) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.3c00269 · Cited by 57 · see citing works
A phase I/II study of the safety and efficacy of [177Lu]Lu-satoreotide tetraxetan in advanced somatostatin receptor-positive neuroendocrine tumours
Wild, D., Grønbæk, H., Navalkissoor, S., Haug, A. R., Nicolas, G. P., Pais, B., Ansquer, C., Beauregard, J., McEwan, A. J. B., Laßmann, M., et al. (2023) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-023-06383-1 · Cited by 54 · see citing works
Lutetium-177 PSMA for the treatment of metastatic castrate resistant prostate cancer: a systematic review
Patell, K., Kurian, M., Garcia, J. A., Mendiratta, P., Barata, P. C., Jia, A. Y., Spratt, D. E., & Brown, J. R. (2023) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2023.2213892 · Cited by 54 · see citing works
β-radiating radionuclides in cancer treatment, novel insight into promising approach
Asadian, S., Mirzaei, H., Kalantari, B. A., Davarpanah, M. R., Mohamadi, M., Shpichka, A. I., Nasehi, L., Es, H. A., Timashev, P. S., Najimi, M., et al. (2020) · Pharmacological Research · doi:10.1016/j.phrs.2020.105070 · Cited by 47 · see citing works
Safety and Therapeutic Optimization of Lutetium-177 Based Radiopharmaceuticals
Ladrière, T., Faudemer, J., Levigoureux, E., Peyronnet, D., Desmonts, C., & Vigne, J. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15041240 · Cited by 46 · see citing works
“This infusion is started about 30 min before the Lutathera®infusion and continues for 4 h [45,57,60,61] (Figure 3).”
Background
Current treatments and future potential of surufatinib in neuroendocrine tumors (NETs)
Xu, J. (2021) · Therapeutic Advances in Medical Oncology · doi:10.1177/17588359211042689 · Cited by 42 · see citing works
Gastroenteropancreatic neuroendocrine neoplasms: current development, challenges, and clinical perspectives
Zhang, X., Fan, Y., Jing, R., Getu, M. A., Chen, W.-Y., Zhang, W., Dong, H., Dakal, T. C., Hayat, A., Cai, H.-J., et al. (2024) · Military Medical Research · doi:10.1186/s40779-024-00535-6 · Cited by 35 · see citing works
Targeted drug conjugates in cancer therapy: Challenges and opportunities
Jia, G., Jiang, Y., & Li, X. (2024) · Pharmaceutical Science Advances · doi:10.1016/j.pscia.2024.100048 · Cited by 35 · see citing works
“Structures of payloads used within the peptide-drug conjugate ﬁ eld. via the high-af ﬁ nity binding agent 1,4,7,10-tetraazacyclododecane-N,N 0 , N,N 0 -tetraacetic acid (DOTA) [158].”
Engineering peptide drug therapeutics through chemical conjugation and implication in clinics
Rizvi, S. F. A., Zhang, H., & Fang, Q. (2024) · Medicinal Research Reviews · doi:10.1002/med.22046 · Cited by 30 · see citing works
Update in the management of gastroenteropancreatic neuroendocrine tumors
Sedlack, A. J. H., Varghese, D. G., Naimian, A., Anari, P. Y., Bodei, L., Hallet, J. I., Riechelmann, R. P., Halfdanarson, T., Capdevilla, J., & Rivero, J. D. (2024) · Cancer · doi:10.1002/cncr.35463 · Cited by 25 · see citing works
A multidisciplinary approach to the work up and management of pulmonary carcinoid tumors and DIPNECH: a narrative review
Ramirez, R. A., Cass, A. S., Das, S., Low, S., Mehrad, M., Rickman, O. B., Scherer, P. M., Thomas, K. E. H., & Gillaspie, E. A. (2022) · Translational Lung Cancer Research · doi:10.21037/tlcr-22-415 · Cited by 25 · see citing works
“The Ki-67 index, a marker of cell proliferation, can aid in differentiating low-grade PCs from high-grade NETs, such as LCNEC and SCLC, especially in a small biopsy with crush artifact.”
InfluentialSelf-citation
Recent Advances in Augmenting the Therapeutic Efficacy of Peptide–Drug Conjugates
Ma, J., Wang, X., Hu, Y., Ma, J., Ma, Y., Chen, H., & Han, Z. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00007 · Cited by 23 · see citing works
Treatment with Radiopharmaceuticals and Radionuclides in Breast Cancer: Current Options
Altıparmak, B., & Yurt, F. (2021) · European Journal of Breast Health · doi:10.4274/ejbh.galenos.2021.2021-3-4 · Cited by 22 · see citing works
Surufatinib for the treatment of advanced extrapancreatic neuroendocrine tumors
Lu, X., Yan, S., Koral, K., & Chen, Z. (2021) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2021.1944110 · Cited by 22 · see citing works
Current clinical application of lutetium‑177 in solid tumors (Review)
Niu, T., Mi, F., Lin, B., Gao, F., Tan, B., & Du, X. (2024) · Experimental and Therapeutic Medicine · doi:10.3892/etm.2024.12514 · Cited by 21 · see citing works
The neuroscience of cancer: Focus on neuropeptidergic systems
Dong, Z.-K., Wang, Y., & Jin, W. (2025) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2025.03.025 · Cited by 22 · see citing works
Application of Cleavable Linkers to Improve Therapeutic Index of Radioligand Therapies
Lau, J., Lee, H., Rousseau, J., Bénard, F., & Lin, K. (2022) · Molecules · doi:10.3390/molecules27154959 · Cited by 21 · see citing works
“4 GBq every 8 weeks for 4 total doses in the presence of a renal protection regimen [10].”
Background
Emerging innovations in theranostics for pancreatic neuroendocrine tumors
Karimi, A., Bogdani, C., O'Dwyer, E., & Siolas, D. (2025) · npj Precision Oncology · doi:10.1038/s41698-025-00938-1 · Cited by 19 · see citing works
The Management of Phaeochromocytomas and Paragangliomas in the Era of Precision Medicine: Where Are We Now? Evidence-Based Systemic Treatment Options and Future Cluster Oriented Perspectives
Bracigliano, A., Marretta, A. L., Guerrera, L. P., Simioli, R., Clemente, O., Granata, V., Minopoli, A., Scarpati, G. D. V., Picozzi, F., Cannella, L., et al. (2024) · Pharmaceuticals · doi:10.3390/ph17030354 · Cited by 19 · see citing works
“PRRT was firstly approved by FDA for the treatment of GEP-NETs that are somato-statin receptor-positive [105].”
Method
Dosimetry and pharmacokinetics of [177Lu]Lu-satoreotide tetraxetan in patients with progressive neuroendocrine tumours
Beykan, S., Eberlein, U., Ansquer, C., Beauregard, J., Durand‐Gasselin, L., Grønbæk, H., Haug, A. R., Hicks, R. J., Lenzo, N. P., Navalkissoor, S., et al. (2024) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-024-06682-1 · Cited by 18 · see citing works
“[ 177 Lu]Lu-DOTA-TATE has, however, been associated with a mean terminal blood half-life of 72 h [39, 40], which is lower than the 127-hour median (110-hour mean) terminal half-life reported with [ 177 Lu]Lu-satoreotide tetraxetan at treatment cycle 1 in our study.”
Result
Clinical advances in TNC delivery vectors and their conjugate agents
Chen, W., Wu, Y., Wang, J., Yu, W., Shen, X., Zhao, K., Liang, B., Hu, X., Wang, S., Jiang, H., et al. (2023) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2023.108577 · Cited by 18 · see citing works
Tumor Targeting with Peptide-Drug Conjugates: Showcasing Key Progress and Hurdles
Parang, K., Do, T., Dinh, C., Davani-Davari, D., Foroughi, M., Khong, T., Moazen, M., & Shirazi, A. N. (2026) · Drug Design Development and Therapy · doi:10.2147/dddt.s562135 · Cited by 17 · see citing works
Radioligand therapy in the therapeutic strategy for patients with gastro-entero-pancreatic neuroendocrine tumors: a consensus statement from the Italian Association for Neuroendocrine Tumors (Itanet), Italian Association of Nuclear Medicine (AIMN), Italian Society of Endocrinology (SIE), Italian Association of Medical Oncology (AIOM).
Panzuto, F., Albertelli, M., Rimini, M. L. D., Rizzo, F. M., Grana, C. M., Cives, M., Faggiano, A., Versari, A., Tafuto, S., Fazio, N., et al. (2024) · Journal of Endocrinological Investigation · doi:10.1007/s40618-024-02448-6 · Cited by 16 · see citing works
“Furthermore, shrink - age following RLT can be a delayed occurrence [ 64 – 66 ].”
Correlations between [68Ga]Ga-DOTA-TOC Uptake and Absorbed Dose from [177Lu]Lu-DOTA-TATE
Bruvoll, R., Blakkisrud, J., Mikalsen, L. T. G., Connelly, J. P., & Stokke, C. (2023) · Cancers · doi:10.3390/cancers15041134 · Cited by 15 · see citing works
Advancements in the development of radiopharmaceuticals for nuclear medicine applications in the treatment of bone metastases
Dyer, M. R., Jing, Z., Duncan, K., Godbe, J. M., & Shokeen, M. (2024) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2024.108879 · Cited by 15 · see citing works
G Protein‐Coupled Receptor Signaling: Implications and Therapeutic Development Advances in Cancers
Khan, I. R., Khurshid, S., Almawash, S., Kumar, R., Akil, A. A., Bhat, A. A., & Macha, M. A. (2025) · MedComm · doi:10.1002/mco2.70375 · Cited by 14 · see citing works
Recent advances and applications of peptide–agent conjugates for targeting tumor cells
Alamdari-Palangi, V., Jaberi, K. R., Shahverdi, M., Naeimzadeh, Y., Tajbakhsh, A., Khajeh, S., Razban, V., & Fallahi, J. (2023) · Journal of Cancer Research and Clinical Oncology · doi:10.1007/s00432-023-05144-9 · Cited by 14 · see citing works
An Overview of Altered Pathways Associated with Sensitivity to Platinum-Based Chemotherapy in Neuroendocrine Tumors: Strengths and Prospects
Stefàno, E., Castro, F. D., Ciccarese, A., Muscella, A., Marsigliante, S., Benedetti, M., & Fanizzi, F. P. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25168568 · Cited by 15 · see citing works
Recent Progress in Peptide-Based Fluorescent Probes Biomedical Applications: A Review
Zhong, X., Xie, Y., Chen, Y., Lu, Y., & Hou, M. (2025) · International Journal of Nanomedicine · doi:10.2147/ijn.s529323 · Cited by 13 · see citing works
An insight into the pharmacology of cysteine/methionine containing peptide drugs
Sharma, A., & Singh, L. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116456 · Cited by 13 · see citing works
Advances in peptide-drug conjugate-based supramolecular hydrogel systems for local drug delivery
Shang, Q., Su, Y., Leslie, F., Sun, M., & Wang, F. (2022) · Medicine in Drug Discovery · doi:10.1016/j.medidd.2022.100125 · Cited by 12 · see citing works
Efficacy and safety of 177Lu-DOTATATE targeted therapy in advanced/metastatic pulmonary neuroendocrine tumors: A systematic review and meta-analysis
Ma, J., Hu, X., Li, L., Rao, Z., & Zhang, C. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.993182 · Cited by 12 · see citing works
“The FDA has approved (177)Lu-DOTATATE mediated PRRT for gastroenteropancreatic neuroendocrine tumors (6).”
Background
Case Report: Hypoglycemia Due to Metastatic Insulinoma in Insulin-Dependent Type 2 Diabetes Successfully Treated With 177 Lu-DOTATATE
Kumar, S., Melek, M., & Rohl, P. (2022) · Frontiers in Endocrinology · doi:10.3389/fendo.2022.906012 · Cited by 12 · see citing works
“Compared to earlier radionuclides, 177-Lutetium emits diagnostic ƴ-radiation, allowing better dosimetry, emits therapeutic b-radiation that has a shorter tissue penetration range (2mm), limiting exposure to neighboring normal tissue, and has nine-fold higher affinity for SST2, and lower hematological/renal toxicity (1…”
Background
Predictive Factors for Resistant Disease with Medical/Radiologic/Liver-Directed Anti-Tumor Treatments in Patients with Advanced Pancreatic Neuroendocrine Neoplasms: Recent Advances and Controversies
Lee, L., Ramos-Álvarez, I., & Jensen, R. T. (2022) · Cancers · doi:10.3390/cancers14051250 · Cited by 12 · see citing works
Addressing the need for more therapeutic options in neuroendocrine prostate cancer
Kemble, J. P., Kwon, E. D., & Karnes, R. J. (2023) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2023.2173174 · Cited by 11 · see citing works
Multi-functional engineered polypeptide-based drug delivery systems for improved cancer therapy
Li, X., Liu, J., Chen, H., Chen, Y., Wang, Y., Zhang, C. Y., & Xing, X. (2022) · Green Chemical Engineering · doi:10.1016/j.gce.2022.07.010 · Cited by 11 · see citing works
Does the proteasome inhibitor bortezomib sensitize to DNA-damaging therapy in gastroenteropancreatic neuroendocrine neoplasms? – A preclinical assessment in vitro and in vivo
Briest, F., Koziolek, E. J., Albrecht, J., Schmidt, F., Bernsen, M. R., Haeck, J. C., Kühl, A. A., Sedding, D., Hartung, T., Exner, S., et al. (2020) · Neoplasia · doi:10.1016/j.neo.2020.11.004 · Cited by 11 · see citing works
Comparison of the Anti-Tumour Activity of the Somatostatin Receptor (SST) Antagonist [177Lu]Lu-Satoreotide Tetraxetan and the Agonist [177Lu]Lu-DOTA-TATE in Mice Bearing AR42J SST2-Positive Tumours
Plas, P., Limana, L., Carré, D., Thiongane, A., Raguin, O., Mansi, R., Meyer-Losic, F., & Lezmi, S. (2022) · Pharmaceuticals · doi:10.3390/ph15091085 · Cited by 10 · see citing works
SSTR2 as an anatomical imaging marker and a safety switch to monitor and manage CAR T cell toxicity
Alcaina, Y., Yang, Y., Vedvyas, Y., McCloskey, J. E., & Jin, M. M. (2022) · Scientific Reports · doi:10.1038/s41598-022-25224-z · Cited by 10 · see citing works
Advances in radiopharmaceuticals for precision medicine: A global and Chinese perspective
Huang, Q., & Huang, G. (2024) · LabMed discovery. · doi:10.1016/j.lmd.2024.100031 · Cited by 10 · see citing works
Peptide therapeutics: current status and future opportunity with focus on nose-to-brain delivery☆
Jülke, E., & Beck‐Sickinger, A. G. (2025) · Peptides · doi:10.1016/j.peptides.2025.171404 · Cited by 13 · see citing works
Applying real-world data from expanded-access (“compassionate use”) patients to drug development
Wasser, J. S., & Greenblatt, D. J. (2023) · Journal of Clinical and Translational Science · doi:10.1017/cts.2023.606 · Cited by 10 · see citing works
Advances in Homing Peptide Targeted Therapies
Xian, X., Ren, Q., Du, H., Qi, Y., & Yan, J. (2025) · International Journal of Peptide Research and Therapeutics · doi:10.1007/s10989-024-10682-y · Cited by 9 · see citing works
“It received FDA approval in January 2018 for the treatment of patients with growth inhibitor receptor-positive gastroenteropancreatic (GEP) neuroendocrine tumors (NET) (Das et al. 2019).”
A dual-targeting peptide–drug conjugate based on CXCR4 and FOLR1 inhibits triple-negative breast cancer
Wang, K., Wang, C., Yang, H., Chen, G., Wang, K., Ji, P., Sun, X., Fan, X., Ma, J., Cui, Z., et al. (2025) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2025.06.012 · Cited by 9 · see citing works
“Since 2018, when the FDA approved the first PDC ( 177 Lu-DOTATATE) for the treatment of gastroenteropancreatic neuroendocrine tumors 20 , more than 100 PDCs have been evaluated for clinical development for tumor treatment and diagnosis.”
Circulating hsa-miR-5096 predicts 18F-FDG PET/CT positivity and modulates somatostatin receptor 2 expression: a novel miR-based assay for pancreatic neuroendocrine tumors
Bocchini, M., Tazzari, M., Ravaioli, S., Piccinini, F., Foca, F., Tebaldi, M., Nicolini, F., Grassi, I., Severi, S., Calogero, R., et al. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2023.1136331 · Cited by 9 · see citing works
“Future optimization of PRRT will depend on improved patient stratification (23, 24).”
Background
Radiopharmaceuticals for Pancreatic Cancer: A Review of Current Approaches and Future Directions
Calistri, S., Ottaviano, G., & Ubaldini, A. (2024) · Pharmaceuticals · doi:10.3390/ph17101314 · Cited by 8 · see citing works
NOTA and NODAGA Radionuclide Complexing Agents: Versatile Approaches for Advancements in Radiochemistry
Chambers, C., Wang, J., Sakr, T. M., Miao, Y., & Smith, C. J. (2025) · Molecules · doi:10.3390/molecules30102095 · Cited by 8 · see citing works
Advanced 64Cu/67Cu-Based Theranostics: Application of the Copper Chelator TE1PA to a Murine Model of HER2-Positive Gastric Cancer
Pineau, J., Ollier, C., Mothes, C., Belderbos, S., Bris, N. L., & Tripier, R. (2025) · Inorganic Chemistry · doi:10.1021/acs.inorgchem.5c01513 · Cited by 7 · see citing works
Diagnosis and Surgical Treatment of Gastroenteropancreatic Neuroendocrine Neoplasms: A Literature Review
Kohno, S. (2022) · Cancer Diagnosis & Prognosis · doi:10.21873/cdp.10085 · Cited by 7 · see citing works
Clinical Evaluation of Nuclear Imaging Agents in Breast Cancer
Li, Z., Aboian, M., Zhu, X., & Marquez-Nostra, B. V. (2022) · Cancers · doi:10.3390/cancers14092103 · Cited by 7 · see citing works
“Nowadays, several FDA-approved theranostic pairs, such as [68Ga]DOTATATE and [177Lu]DOTATATE for neuroendocrine tumors, are used in clinical nuclear medicine practice [13,14].”
Background
Novel Cyclic Peptide–Drug Conjugate P6-SN38 Toward Targeted Treatment of EGFR Overexpressed Non-Small Cell Lung Cancer
Bazylevich, A., Miller, A., Tkachenko, I. G., Merlani, M., Patsenker, L. D., Gellerman, G., & Lubin, B. C. R. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16121613 · Cited by 6 · see citing works
“…approved for clinical use to treat somatostatin receptors and prostate-specific membrane antigen (PSMA) overexpressing cancers, respectively [22,23]. peptide–radionuclide conjugates, 177Lu-DOTA-TATE and 177Lu-PSMA-617, have been approved for clinical use to treat somatostatin receptors and ﬁ c…”
Recent Advances in the Linkers of Drug Conjugates
Deng, S., Wen, X., & Wang, J. (2024) · Current Medicinal Chemistry · doi:10.2174/0109298673320170240829110110 · Cited by 6 · see citing works
Advances and future directions in radiopharmaceutical delivery for cancer treatment
Ailawadhi, S., Pafundi, D., & Peterson, J. (2025) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2025.2472859 · Cited by 6 · see citing works
177Lu-DOTATATE PRRT for Multiple Unusual Metastatic Sites in Neuroendocrine Tumor
Parghane, R. V., & Basu, S. K. (2022) · Clinical Nuclear Medicine · doi:10.1097/rlu.0000000000004139 · Cited by 6 · see citing works
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Authors: Das, S., Al-Toubah, T., El-Haddad, G., & Strosberg, J.
Affiliations: Vanderbilt University Medical Center (US)
Department of GI Oncology, Moffitt Cancer Center, Tampa, FL, USA
Moffitt Cancer Center (US)
Corresponding author: Das, Satya
ORCID: Das, Satya
El-Haddad, Ghassan
Strosberg, Jonathan
Venue: Expert Review of Gastroenterology & Hepatology
Publisher: Informa UK Limited
Published: 2019-10-30
Volume: 13
Issue: 11
Pages: 1023-1031
ISSN: 1747-4124 (ISSN-L)
1747-4132
DOI: 10.1080/17474124.2019.1685381
PMC: PMC7227421
OpenAlex: W2981499856
Cited by: 135
References: 53
Citations by year: 2026: 23 · 2025: 32 · 2024: 32 · 2023: 15 · 2022: 20 · 2021: 9 · 2020: 4
FWCI: 6.28
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Expert Review of Gastroenterology & Hepatology (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Cancer Institute (K12CA090625)
Topics: Health Sciences › Medicine › Epidemiology › Neuroendocrine Tumor Research Advances
Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
Health Sciences › Medicine › Oncology › Peptidase Inhibition and Analysis
Keywords: 177Lu-DOTATATE, peptide receptor radionuclide therapy, gastroenteropancreatic neuroendocrine tumors, somatostatin receptors, octreotate, NETTER-1 trial, treatment efficacy, adverse events, treatment sequencing
MeSH terms: Animals, Gastrointestinal Neoplasms, Humans, Organometallic Compounds, Pancreatic Neoplasms, Octreotide, Treatment Outcome, Neuroendocrine Tumors, Radiopharmaceuticals

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177 Lu-DOTATATE for the treatment of gastroenteropancreatic neuroendocrine tumors

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