Edotreotide - Wiki slovník

Edotreotide
Clinical data
Trade names	SomaKit TOC
Identifiers
DrugBank	DB15494;
CompTox Dashboard (EPA)	DTXSID701021591 ;

Edotreotide
Names
	IUPAC name 2-2-(2R)-1-(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-(2R,3R)-1,3-dihydroxybutan-2-ylcarbamoyl-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-ylamino-1-oxo-3-phenylpropan-2-ylamino-2-oxoethyl-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-ylacetic acid
Identifiers
CAS Number	204318-14-9 ;
3D model (JSmol)	Interactive image;
ChemSpider	139675 ;
PubChem CID	158782;
UNII	U194AS08HZ ;
CompTox Dashboard (EPA)	DTXSID701021591 ;
	InChI 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 Key: RZHKDBRREKOZEW-AAXZNHDCSA-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;
	SMILES CC@H(C@H1C(=O)NC@@H(CSSCC@@H(C(=O)NC@H(C(=O)NC@@H(C(=O)NC@H(C(=O)N1)CCCCN)Cc2cnHc3c2cccc3)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)NC@H(CO)C@@H(C)O)O;
Properties
Chemical formula	C65H92N14O18S2
Molar mass	1421.65 g·mol−1
Pharmacology
License data	EU EMA: by INN;
Pharmacology
Legal status	UK: POM (Prescription only); EU: Rx-only;
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C 77 °F, 100 kPa). verify (what is ?) Infobox references

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-90edit

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]

Lutetium-177edit

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]

Referencesedit

^ "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.

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[1] "SomaKit TOC 40 micrograms kit for radiopharmaceutical preparation - Summary of Product Characteristics (SmPC)". (emc). 2 July 2021. Retrieved 9 July 2021.

[2] "SomaKit TOC EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 20 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. Retrieved 7 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. Retrieved 7 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. Retrieved 7 November 2020.

[9] "EU/03/14/1269". European Medicines Agency. 17 September 2018. Retrieved 7 November 2020.

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v t e GH/IGF-1 axis signaling modulators
GH (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
GHIH (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
GHRH (somatocrinin)	Agonists: Peptide: ALRN-5281 CJC-1295 Dumorelin GHRH Modified GRF (1-29) Rismorelin Sermorelin Somatorelin Tesamorelin Antagonists: MZ-5-156
GHS (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
IGF-1 (somatomedin)	See here instead.

Yttrium-90edit

Lutetium-177edit

See alsoedit

Referencesedit