gallium (68Ga) edotreotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
somatostatin receptor agonists/antagonists	5185	459831-08-4

Description:

Molecule	Description
Synonyms: Ga 68 dotatate gallium (68Ga) edotreotide gallium Ga 68-edotreotide Ga-68 DOTA0-Tyr3-octreotide gallium dotatoc Ga 68 gallium dotatoc GA-68	A radioconjugate consisting of the octreotide derivative edotreotide labeled with gallium 68 (Ga-68) with potential application in somatostatin receptor (SSTR) imaging in conjunction with positron emission tomography (PET). Similar to octreotide, gallium Ga 68-edotreotide binds to SSTRs, especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells and their metastases, thereby allowing for imaging of SSTR-expressing cells upon PET. Gallium Ga 68-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide (Tyr3-octreotide or TOC) and chelating the substituted octreotide to Ga-68 via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA). Molecular weight: 1486.55 Formula: C65H89GaN14O18S2 CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: 434.43 ALOGS: ROTB: None

Molecule

Description

Synonyms:

Ga 68 dotatate
gallium (68Ga) edotreotide
gallium Ga 68-edotreotide
Ga-68 DOTA0-Tyr3-octreotide
gallium dotatoc Ga 68
gallium dotatoc GA-68

A radioconjugate consisting of the octreotide derivative edotreotide labeled with gallium 68 (Ga-68) with potential application in somatostatin receptor (SSTR) imaging in conjunction with positron emission tomography (PET). Similar to octreotide, gallium Ga 68-edotreotide binds to SSTRs, especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells and their metastases, thereby allowing for imaging of SSTR-expressing cells upon PET. Gallium Ga 68-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide (Tyr3-octreotide or TOC) and chelating the substituted octreotide to Ga-68 via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA).

Molecular weight: 1486.55
Formula: C65H89GaN14O18S2
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA: 434.43
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Dec. 8, 2016	EMA	Advanced Accelerator Applications
Aug. 21, 2019	FDA	UIHC PET IMAGING

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	V09IX09	VARIOUS DIAGNOSTIC RADIOPHARMACEUTICALS TUMOUR DETECTION Other diagnostic radiopharmaceuticals for tumour detection

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Positron emission tomography with computed tomography of whole body using gallium (68-Ga) dotatate	indication	764693004

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Somatostatin receptor type 2	GPCR	P30874	SSR2_HUMAN	ANTAGONIST	Ki	8.60		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
C3640098	UMLSCUI
CHEMBL4297340	ChEMBL_ID
71661158	PUBCHEM_CID
DB15494	DRUGBANK_ID
D11651	KEGG_DRUG
018100	NDDF
2199391	RXNORM

Pharmaceutical products:

None