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Edotreotide

From Wikipedia, the free encyclopedia
Edotreotide
Names
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
Other names
SomaKit TOC
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
DrugBank
UNII
  • InChI=1S/C65H92N14O18S2/c1-39(81)51(36-80)72-64(96)53-38-99-98-37-52(73-60(92)48(28-41-10-4-3-5-11-41)68-54(84)32-76-20-22-77(33-55(85)86)24-26-79(35-57(89)90)27-25-78(23-21-76)34-56(87)88)63(95)70-49(29-42-15-17-44(83)18-16-42)61(93)71-50(30-43-31-67-46-13-7-6-12-45(43)46)62(94)69-47(14-8-9-19-66)59(91)75-58(40(2)82)65(97)74-53/h3-7,10-13,15-18,31,39-40,47-53,58,67,80-83H,8-9,14,19-30,32-38,66H2,1-2H3,(H,68,84)(H,69,94)(H,70,95)(H,71,93)(H,72,96)(H,73,92)(H,74,97)(H,75,91)(H,85,86)(H,87,88)(H,89,90)/t39-,40-,47+,48-,49+,50-,51-,52+,53+,58+/m1/s1 ☒N
    Key: RZHKDBRREKOZEW-AAXZNHDCSA-N ☒N
  • InChI=1/C65H92N14O18S2/c1-39(81)51(36-80)72-64(96)53-38-99-98-37-52(73-60(92)48(28-41-10-4-3-5-11-41)68-54(84)32-76-20-22-77(33-55(85)86)24-26-79(35-57(89)90)27-25-78(23-21-76)34-56(87)88)63(95)70-49(29-42-15-17-44(83)18-16-42)61(93)71-50(30-43-31-67-46-13-7-6-12-45(43)46)62(94)69-47(14-8-9-19-66)59(91)75-58(40(2)82)65(97)74-53/h3-7,10-13,15-18,31,39-40,47-53,58,67,80-83H,8-9,14,19-30,32-38,66H2,1-2H3,(H,68,84)(H,69,94)(H,70,95)(H,71,93)(H,72,96)(H,73,92)(H,74,97)(H,75,91)(H,85,86)(H,87,88)(H,89,90)/t39-,40-,47+,48-,49+,50-,51-,52+,53+,58+/m1/s1
    Key: RZHKDBRREKOZEW-AAXZNHDCBX
  • 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)Cc2c[nH]c3c2cccc3)Cc4ccc(cc4)O)NC(=O)[C@@H](Cc5ccccc5)NC(=O)CN6CCN(CCN(CCN(CC6)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)N[C@H](CO)[C@@H](C)O)O
Properties
C65H92N14O18S2
Molar mass1421.65 g·mol−1
Pharmacology
License data
Legal status
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
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Chemical compound

Edotreotide (USAN, also known as (DOTA0-Phe1-Tyr3)octreotide,DOTA-TOC,DOTATOC) is a substance which, when bound to variousradionuclides, is used in the treatment and diagnosis of certain types of cancer.[3] When used therapeutically it is an example ofpeptide receptor radionuclide therapy.

Yttrium-90

[edit]

Aphase I clinical trial ofyttrium-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 includeneuroblastoma, childhoodbrain tumours andgastrointestinal cancer.[5]

Aphase II trial for the use of90Y DOTA-TOC for patients withmetastaticcarcinoid, whereoctreotide treatment was no longer effective, also reported results in 2010.[6]

Yttrium-90 labeled edotreotide

Lutetium-177

[edit]

Lutetium-177 labelled edotreotide (177Lu-DOTA-TOC), with thetrade name Solucin, is the subject of aphase 3 clinical trial for treatment ofGEP-NETs.[7][8] It was grantedorphan drug designation by theEuropean Medicines Agency in 2014.[9]

See also

[edit]

References

[edit]
  1. ^"SomaKit TOC 40 micrograms kit for radiopharmaceutical preparation - Summary of Product Characteristics (SmPC)".(emc). 2 July 2021. Retrieved9 July 2021.
  2. ^"SomaKit TOC EPAR".European Medicines Agency (EMA). 17 September 2018. Retrieved20 October 2020.
  3. ^Martindale, The Extra Pharmacopoeia, 30th ed, p1161.
  4. ^S, O'Dorisio (17 June 2016)."Radiolabeled Octreotide in Treating Children With Advanced or Refractory Solid Tumors".ClinicalTrials.gov. US National Library of Medicine. Retrieved7 November 2020.
  5. ^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.
  6. ^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.
  7. ^"The therapeutic n.c.a. 177Lu-Edotreotide (Solucin)". ITM Isotopen Technologien München AG. Retrieved7 November 2020.
  8. ^"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. Retrieved7 November 2020.
  9. ^"EU/03/14/1269".European Medicines Agency. 17 September 2018. Retrieved7 November 2020.
GH
(somatotropin)
GHIH
(somatostatin)
GHRH
(somatocrinin)
GHS
(ghrelin)
IGF-1
(somatomedin)
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