Edotreotide
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IUPAC name 2-[4-[2-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-[[(2R,3R)-1,3-dihydroxybutan-2-yl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid | |
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Chemical formula | C65H92N14O18S2 |
Molar mass | 1421.65 g·mol−1 |
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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). ![]() ![]() ![]() Infobox references |
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Trade names | SomaKit TOC |
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Edotreotide (USAN, also known as (DOTA0-Phe1-Tyr3) octreotide, DOTA-TOC, DOTATOC) is a substance which, when bound to various radionuclides, is used in the treatment and diagnosis of certain types of cancer.[3] When used therapeutically it is an example of peptide receptor radionuclide therapy.
Yttrium-90
A phase I clinical trial of yttrium-90 labelled edotreotide concluded in 2011,[4] aiming to investigated effects in young cancer patients (up to 25 years of age). Specific cancers being included in the trial include neuroblastoma, childhood brain tumours and gastrointestinal cancer.[5]
A phase II trial for the use of 90Y DOTA-TOC for patients with metastatic carcinoid, where octreotide treatment was no longer effective, also reported results in 2010.[6]
Yttrium-90 labeled edotreotide
Lutetium-177
Lutetium-177 labelled edotreotide (177Lu-DOTA-TOC), with the trade name Solucin, is the subject of a phase 3 clinical trial for treatment of GEP-NETs.[7][8] It was granted orphan drug designation by the European Medicines Agency in 2014.[9]
See also
- DOTA-TATE, a similar compound
References
- ^ "SomaKit TOC 40 micrograms kit for radiopharmaceutical preparation - Summary of Product Characteristics (SmPC)". (emc). 2 July 2021. Retrieved 9 July 2021.
- ^ "SomaKit TOC EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 20 October 2020.
- ^ Martindale, The Extra Pharmacopoeia, 30th ed, p1161.
- ^ S, O'Dorisio (17 June 2016). "Radiolabeled Octreotide in Treating Children With Advanced or Refractory Solid Tumors". ClinicalTrials.gov. US National Library of Medicine. Retrieved 7 November 2020.
- ^ Menda Y, O'Dorisio MS, Kao S, Khanna G, Michael S, Connolly M, et al. (October 2010). "Phase I trial of 90Y-DOTATOC therapy in children and young adults with refractory solid tumors that express somatostatin receptors". Journal of Nuclear Medicine. 51 (10): 1524–31. doi:10.2967/jnumed.110.075226. PMC 3753801. PMID 20847174.
- ^ Bushnell DL, O'Dorisio TM, O'Dorisio MS, Menda Y, Hicks RJ, Van Cutsem E, et al. (April 2010). "90Y-edotreotide for metastatic carcinoid refractory to octreotide". Journal of Clinical Oncology. 28 (10): 1652–9. doi:10.1200/JCO.2009.22.8585. PMC 4872330. PMID 20194865.
- ^ "The therapeutic n.c.a. 177Lu-Edotreotide (Solucin)". ITM Isotopen Technologien München AG. Retrieved 7 November 2020.
- ^ "A prospective, randomised, Controlled, Open-label, Multicentre phase III study to evaluate efficacy and safety of Peptide Receptor Radionuclide Therapy (PRRT) with Lutetium 177-Edotreotide compared to targeted molecular therapy with Everolimus in patients with inoperable, progressive, somatostatin receptor-positive (SSTR+), neuroendocrine tumours of gastroenteric or pancreatic origin (GEP-NET)". EU Clinical Trials Register. Retrieved 7 November 2020.
- ^ "EU/03/14/1269". European Medicines Agency. 17 September 2018. Retrieved 7 November 2020.
- v
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(somatotropin)
- Agonists: Albusomatropin
- Bovine somatotropin
- Efpegsomatropin
- Eftansomatropin alfa
- Growth hormone
- Human placental lactogen
- Lonapegsomatropin
- Placental growth hormone (growth hormone variant)
- Somagrebove
- Somapacitan
- Somatosalm
- Somatotropin
- Somatropin pegol
- Somatrem
- Sometribove
- Somatrogon (MOD-4023; hGH-CTP)
- Somavaratan
- Somavubove
- Somidobove
- Antagonists: G120K-hGH
- Pegvisomant
- Antisense oligonucleotides: Atesidorsen
- Binding proteins: GHBPTooltip Growth hormone-binding protein
(somatostatin)
- Agonists: BIM-23052
- CH-275
- Cortistatin-14
- Depreotide
- Edotreotide
- Ilatreotide
- L-803,087
- L-817,818
- Lanreotide
- NNC 26-9100
- Octreotate
- Octreotide
- Pasireotide
- Pentetreotide
- RC-160
- Seglitide
- Somatostatin (GHIH)
- Somatostatin (1-28)
- SRIF-14
- SRIF-28
- TT-232
- Vapreotide
- Veldoreotide
- Antagonists: BIM-23056
- Cyclosomatostatin
- CYN-154806
- Satoreotide
(somatocrinin)
- Agonists: Peptide: ALRN-5281
- CJC-1295
- Dumorelin
- GHRH
- Modified GRF (1-29)
- Rismorelin
- Sermorelin
- Somatorelin
- Tesamorelin
- Antagonists: MZ-5-156
(ghrelin)
- Agonists: Peptide: Alexamorelin
- Cortistatin-14
- EP-51216
- Examorelin (hexarelin)
- Ghrelin
- GHRP-1
- GHRP-3
- GHRP-4
- GHRP-5
- GHRP-6
- Ipamorelin
- Lenomorelin
- Livoletide
- LY-444711
- Pralmorelin (GHRP-2)
- Relamorelin
- Tabimorelin
- Ulimorelin; Non-peptide: Adenosine
- Anamorelin
- Capromorelin
- CP-464709
- Ibutamoren (MK-677)
- L-692,585
- Macimorelin
- SM-130686; Unsorted: LY-426410
- LY-444711
- Antagonists: A-778193
- Cortistatin-8
- (D-Lys³)-GHRP-6
- JMV2959
- YIL-781
(somatomedin)
- See here instead.
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