Edotreotide gallium Ga-68

Identification

Name

Edotreotide gallium Ga-68

Accession Number

DB15494

Description

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

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MOLSDFPDBSMILESInChI

Similar Structures

Structure for Edotreotide gallium Ga-68 (DB15494)

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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

Associated Conditions

• Neuroendocrine Tumors

Contraindications & Blackbox Warnings

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Pharmacodynamics

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	ligand	Humans
ASomatostatin receptor type 5	ligand	Humans
ASomatostatin receptor type 3	ligand	Humans
ASomatostatin receptor type 1	ligand	Humans

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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Toxicity

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

Affected organisms

Not Available

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Lanreotide	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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Severity
Severity
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Food Interactions

No interactions found.

Products

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Unlock Additional Data
Ga-68-DOTATOC	Injection, solution	4 mCi/1mL	Intravenous	UIHC – P E T Imaging Center	2019-09-01	Not applicable
Somakit Toc	Kit		Intravenous	Advanced Accelerator Applications	2016-12-08	Not applicable

Additional Data Available

Application Number
Application Number
Available for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
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Product Code
Product Code
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A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories

ATC Codes

V09IX09 — Gallium (68ga) edotreotide

• V09IX — Other diagnostic radiopharmaceuticals for tumour detection
• V09I — TUMOUR DETECTION
• V09 — DIAGNOSTIC RADIOPHARMACEUTICALS
• V — VARIOUS

Drug Categories

• Diagnostic Radiopharmaceuticals
• Gallium Radioisotopes
• Radiopharmaceuticals
• Tumour Detection

Classification

Not classified

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

1. 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. [PubMed:19639164]
2. 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. [PubMed:22072704]
3. 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. [PubMed:9096086]
4. 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. [PubMed:11734911]
5. 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. [PubMed:10319747]
6. 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. [PubMed:10901448]
7. FDA Approved Drug Products: Gallium Dotatoc GA 68 [Link]
8. EMA Assessment Report: SomaKit TOC [Link]

External Links

ChemSpider

52083916

RxNav

2199391

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
2	Not Yet Recruiting	Diagnostic	Meningiomas	1
1, 2	Terminated	Diagnostic	Carcinoid Tumors / Neuroblastomas / Neuroendocrine Tumors / Paraganglioma	1
0	Active Not Recruiting	Diagnostic	Meningiomas / Metastatic Well Differentiated Neuroendocrine Neoplasm / Multiple Endocrine Neoplasia Type 1 / Neuroendocrine Neoplasms / Somatostatin Positive Neoplastic Cells Present / Von Hippel-Lindau Syndrome	1
Not Available	Not Yet Recruiting	Diagnostic	Myocarditis	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Intravenous	4 mCi/1mL
Injection, solution	Parenteral	20 MBq/ml
Injection, powder, lyophilized, for solution	Intravenous	40 mcg
Kit	Intravenous

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

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Drug created on September 17, 2019 14:38 / Updated on November 02, 2020 18:20