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

Stem definitionDrug idCAS RN
somatostatin receptor agonists/antagonists 5185 459831-08-4

Description:

MoleculeDescription

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Aug. 21, 2019 FDA UIHC PET IMAGING
Dec. 8, 2016 EMA Advanced Accelerator Applications

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:

SourceCodeDescription
ATC V09IX09 VARIOUS
DIAGNOSTIC RADIOPHARMACEUTICALS
TUMOUR DETECTION
Other diagnostic radiopharmaceuticals for tumour detection

Related Drugs by ATC class:

V09IX Other diagnostic radiopharmaceuticals for tumour detection 10 drugs
fluciclovine (18F)fludeoxyglucose (18F)fluorodopa (18F)fluoroestradiol F 18fluoroethylcholine (18F)gallium (68Ga) gozetotideiobenguane (123I)iobenguane (131I)methioninesodium fluoride F-18

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

DiseaseRelationSNOMED_IDDOID
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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.5-4mCi/ML GALLIUM GA 68 EDOTREOTIDE UIHC PET IMAGING N210828 Aug. 21, 2019 RX SOLUTION INTRAVENOUS Aug. 21, 2026 EXCLUSIVITY ON THIS APPLICATION EXPIRING ON THIS DATE HAS BEEN WAIVED BY SPONSOR - SEE SECTION 1.8 OF ORANGE BOOK PREFACE WAIVED EXCLUSIVITY
0.5-4mCi/ML GALLIUM GA 68 EDOTREOTIDE UIHC PET IMAGING N210828 Aug. 21, 2019 RX SOLUTION INTRAVENOUS Aug. 21, 2026 FOR USE WITH POSITRON EMISSION TOMOGRAPHY (PET) FOR THE LOCALIZATION OF KNOWN SOMATOSTATIN RECEPTOR POSITIVE NEUROENDOCRINE TUMORS (NETS) IN ADULT AND PEDIATRIC PATIENTS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Somatostatin receptor type 2 GPCR ANTAGONIST Ki 8.60 DRUG LABEL DRUG LABEL

External reference:

IDSource
C3640098 UMLSCUI
CHEBI:756835 CHEBI
CHEMBL4297340 ChEMBL_ID
71661158 PUBCHEM_CID
DB15494 DRUGBANK_ID
D11651 KEGG_DRUG
1371422008 SNOMEDCT_US
018100 NDDF
2199391 RXNORM

Pharmaceutical products:

None