Identification
- Summary
Edotreotide gallium Ga-68 is a radioactive diagnostic agent used in PET scans for somatostatin receptor positive neuroendocrine tumors in adult and pediatric patients.
- Generic Name
- Edotreotide gallium Ga-68
- DrugBank Accession Number
- DB15494
- Background
Edotreotide gallium Ga-68 is an 8 amino acid peptide bound to the chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA).8 Edotreotide gallium Ga-68 is indicated for localizing somatostatin receptor positive neuroendocrine tumors by positron emission tomography.7 Dotatate gallium Ga-68 is used for a similar indication.2 Dotatate gallium Ga-68 has lower tumor uptake but this data is highly variable between patients.2
Edotreotide gallium Ga-68 was granted FDA approval on 21 August 2019.7
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Edotreotide gallium Ga-68 (DB15494)
- Weight
- Average: 1486.55
Monoisotopic: 1485.520052927 - Chemical Formula
- C65H89GaN14O18S2
- Synonyms
- Edotreotide Gallium Ga-68
- Gallium (68Ga) edotreotide
- Gallium edotreotide Ga-68
- Gallium Ga 68-dotatoc
- Gallium Ga 68-edotreotide
- Gallium Ga-68 edotreotide
Pharmacology
- Indication
Edotreotide gallium Ga-68 is a radioactive diagnostic compound used in positron emission tomography (PET) for diagnose somatostatin receptor positive neuroendocrine tumors in pediatrics and adults.7
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- Contraindications & Blackbox Warnings
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Edotreotide gallium Ga-68 binds to somatostatin receptors where it emits beta particle radiation for detection by positron emission tomography.7 The duration of action is short as it has short radioactive and biological half lives.4,8 Patients should hydrate before and after the administration of this medication to encourage frequent urination and rapid clearance.7
- Mechanism of action
Edotreotide gallium Ga-68 binds to somatostatin receptors, with higher affinity for somatostatin receptor type 2, where it emits beta particle radiation for detection by positron emission tomography (PET).7
Target Actions Organism ASomatostatin receptor type 2 ligandHumans ASomatostatin receptor type 5 ligandHumans ASomatostatin receptor type 3 ligandHumans ASomatostatin receptor type 1 ligandHumans - Absorption
Edotreotide gallium Ga-68 reaches 80% activity in tumors within 30 minutes,4 and reaches its highest activity in tumors 70±20min post injection.8 Edotreotide is mostly taken up into the spleen, followed by kidneys, liver, pituitary, thyroid, and adrenal gland.3,4,8 Accumulation in non-tumor tissue reaches a maximum within 40 minutes.4
- Volume of distribution
Data regarding the volume of distribution of this medication is not readily available.7
- Protein binding
Data suggests edotreotide gallium-Ga 68 may bind to proteins in serum.6 The extent of serum protein binding and which proteins it binds to are not described in the literature.
- Metabolism
Edotreotide gallium Ga-68 is largely unmetabolized.8 4 hours post injection there are no metabolites or degradation products detectable in serum.4
- Route of elimination
16% of a Edotreotide gallium Ga-68 dose is eliminated in the urine within 2h.1,7 It is expected that Edotreotide gallium Ga-68 is exclusively eliminated in the urine.1,7 In animal studies, edotreotide Y-90 was >80% eliminated in the urine within 24h, with 95.6±3.4% being unmetabolized.3,8 <1% of a dose is detected in the feces.5
- Half-life
Edotreotide gallium Ga-68 has a radioactive half life of 68 minutes.4,8 Edotreotide gallium Ga-68 has two half lives, 2.0±0.3min and 48±7min for its removal from blood.4,8
- Clearance
Data regarding the clearance of this medication is not readily available.7
- Adverse Effects
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The LD50 of this medication is not readily available.7
In the event of an overdose, give patients plenty of fluids and diuretics if necessary to encourage frequent urination.7 If possible, an estimation of radioactive dose should be performed.7
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareLanreotide Lanreotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent. Octreotide Octreotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent. Pasireotide Pasireotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent. Somatostatin Somatostatin may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ga-68-DOTATOC Injection, solution 4 mCi/1mL Intravenous UIHC – P E T Imaging Center 2019-09-01 Not applicable US 
Somakit Toc Kit 40 mcg Intravenous Advanced Accelerator Applications 2020-12-22 Not applicable EU 
Categories
- ATC Codes
- V09IX09 — Gallium (68ga) edotreotide
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Y68179SY2L
- CAS number
- 2101630-92-4
- InChI Key
- PZBPHYLKIMOZPR-FIYGWYQWSA-K
- InChI
- InChI=1S/C65H92N14O18S2.Ga/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);/q;+3/p-3/t39-,40-,47+,48-,49+,50-,51-,52+,53+,58+;/m1./s1/i;1-2
- IUPAC Name
- (68Ga)gallium(3+) 2-[4-({[(1R)-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-yl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-19-yl]carbamoyl}-2-phenylethyl]carbamoyl}methyl)-7,10-bis(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetate
- SMILES
- [68Ga+3].C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](CC2=CC=CC=C2)NC(=O)CN2CCN(CC([O-])=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC2)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@H](CC2=CNC3=C2C=CC=C3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1
References
- General References
- Hartmann H, Zophel K, Freudenberg R, Oehme L, Andreeff M, Wunderlich G, Eisenhofer G, Kotzerke J: [Radiation exposure of patients during 68Ga-DOTATOC PET/CT examinations]. Nuklearmedizin. 2009;48(5):201-7. doi: 10.3413/nukmed-0214. Epub 2009 Jul 28. [Article]
- Poeppel TD, Binse I, Petersenn S, Lahner H, Schott M, Antoch G, Brandau W, Bockisch A, Boy C: 68Ga-DOTATOC versus 68Ga-DOTATATE PET/CT in functional imaging of neuroendocrine tumors. J Nucl Med. 2011 Dec;52(12):1864-70. doi: 10.2967/jnumed.111.091165. Epub 2011 Nov 9. [Article]
- de Jong M, Bakker WH, Krenning EP, Breeman WA, van der Pluijm ME, Bernard BF, Visser TJ, Jermann E, Behe M, Powell P, Macke HR: Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA0,d-Phe1,Tyr3]octreotide, a promising somatostatin analogue for radionuclide therapy. Eur J Nucl Med. 1997 Apr;24(4):368-71. doi: 10.1007/bf00881807. [Article]
- Hofmann M, Maecke H, Borner R, Weckesser E, Schoffski P, Oei L, Schumacher J, Henze M, Heppeler A, Meyer J, Knapp H: Biokinetics and imaging with the somatostatin receptor PET radioligand (68)Ga-DOTATOC: preliminary data. Eur J Nucl Med. 2001 Dec;28(12):1751-7. doi: 10.1007/s002590100639. Epub 2001 Oct 31. [Article]
- Kwekkeboom DJ, Kooij PP, Bakker WH, Macke HR, Krenning EP: Comparison of 111In-DOTA-Tyr3-octreotide and 111In-DTPA-octreotide in the same patients: biodistribution, kinetics, organ and tumor uptake. J Nucl Med. 1999 May;40(5):762-7. [Article]
- Bangard M, Behe M, Guhlke S, Otte R, Bender H, Maecke HR, Biersack HJ: Detection of somatostatin receptor-positive tumours using the new 99mTc-tricine-HYNIC-D-Phe1-Tyr3-octreotide: first results in patients and comparison with 111In-DTPA-D-Phe1-octreotide. Eur J Nucl Med. 2000 Jun;27(6):628-37. doi: 10.1007/s002590050556. [Article]
- FDA Approved Drug Products: Gallium Dotatoc GA 68 [Link]
- EMA Assessment Report: SomaKit TOC [Link]
- External Links
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Diagnostic Adult Medulloblastoma / Medulloblastoma, Childhood / Neuroblastoma (NB) / Neuroendocrine Tumors / Somatostatinoma 1 2 Recruiting Diagnostic Meningiomas 1 1, 2 Terminated Diagnostic Carcinoid Tumors / Neuroblastoma (NB) / Neuroendocrine Tumors / Paragangliomas 1 0 Terminated Diagnostic Meningiomas / Metastatic Well Differentiated Neuroendocrine Neoplasm / Multiple Endocrine Neoplasia, Type 1 / Neuroendocrine Neoplasms / Somatostatin Positive Neoplastic Cells Present / Von Hippel-Lindau Syndrome 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 4 mCi/1mL Injection, solution Parenteral Injection, powder, lyophilized, for solution Intravenous 40 mcg Kit Intravenous 40 mcg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0646 mg/mL ALOGPS logP 1.66 ALOGPS logP -9.6 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) -0.48 Chemaxon pKa (Strongest Basic) 10.28 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 23 Chemaxon Hydrogen Donor Count 14 Chemaxon Polar Surface Area 488.88 Å2 Chemaxon Rotatable Bond Count 26 Chemaxon Refractivity 397.48 m3·mol-1 Chemaxon Polarizability 143.64 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and ...
- Gene Name
- SSTR2
- Uniprot ID
- P30874
- Uniprot Name
- Somatostatin receptor type 2
- Molecular Weight
- 41332.37 Da
References
- FDA Approved Drug Products: Gallium Dotatoc GA 68 [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Increases cell growth inhibition act...
- Gene Name
- SSTR5
- Uniprot ID
- P35346
- Uniprot Name
- Somatostatin receptor type 5
- Molecular Weight
- 39201.925 Da
References
- EMA Assessment Report: SomaKit TOC [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase.
- Gene Name
- SSTR3
- Uniprot ID
- P32745
- Uniprot Name
- Somatostatin receptor type 3
- Molecular Weight
- 45846.995 Da
References
- EMA Assessment Report: SomaKit TOC [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stim...
- Gene Name
- SSTR1
- Uniprot ID
- P30872
- Uniprot Name
- Somatostatin receptor type 1
- Molecular Weight
- 42685.77 Da
References
- EMA Assessment Report: SomaKit TOC [Link]
Drug created at September 17, 2019 20:38 / Updated at August 06, 2021 21:26