Edotreotide gallium Ga-68

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

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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

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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

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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Food Interactions

No interactions found.

Products

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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
Somakit Toc	Kit		Intravenous	Advanced Accelerator Applications	2020-12-22	Not applicable

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

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

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	Recruiting	Diagnostic	Meningiomas	1
1, 2	Terminated	Diagnostic	Carcinoid Tumors / Neuroblastomas / Neuroendocrine Tumors / Paraganglioma	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
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
Injection, powder, lyophilized, for solution	Intravenous
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

Targets

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Details1. Somatostatin receptor type 2

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

1. FDA Approved Drug Products: Gallium Dotatoc GA 68 [Link]

Details2. Somatostatin receptor type 5

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

1. EMA Assessment Report: SomaKit TOC [Link]

Details3. Somatostatin receptor type 3

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

1. EMA Assessment Report: SomaKit TOC [Link]

Details4. Somatostatin receptor type 1

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

1. EMA Assessment Report: SomaKit TOC [Link]

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Drug created on September 17, 2019 20:38 / Updated on March 04, 2021 09:26