lutetium (177Lu) oxodotreotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5275 437608-50-9

Description:

MoleculeDescription

Synonyms:

  • lutetium (177Lu) oxodotreotide
  • lutetium Lu 177 dotatate
  • lutathera
Lutetium Lu 177 dotatate binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSTR2). Upon binding to somatostatin receptor expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized. The beta emission from Lu 177 induces cellular damage by formation of free radicals in somatostatin receptor-positive cells and in neighboring cells.
  • Molecular weight: 1612.58
  • Formula: C65H90LuN14O19S2
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 484.50
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 26, 2017 EMA Advanced Accelerator Applications
Jan. 26, 2018 FDA AAA USA INC
June 23, 2021 PMDA FUJIFILM TOYAMA CHEMICAL Co., Ltd.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 64.31 41.57 26 605 68098 50536395

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Metastases to liver 97.68 33.15 29 914 11827 29561757
Malignant neoplasm progression 51.70 33.15 31 912 73828 29499756
Disease progression 43.80 33.15 29 914 81887 29491697
Metastases to bone 39.51 33.15 14 929 9884 29563700

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Metastases to liver 88.16 31.85 27 1023 23914 64473768
Malignant neoplasm progression 56.00 31.85 30 1020 112841 64384841
Hepatic lesion 51.15 31.85 13 1037 5811 64491871
Metastases to bone 38.78 31.85 14 1036 20421 64477261

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V10XX04 VARIOUS
THERAPEUTIC RADIOPHARMACEUTICALS
OTHER THERAPEUTIC RADIOPHARMACEUTICALS
Various therapeutic radiopharmaceuticals
MeSH PA D064907 Diagnostic Uses of Chemicals
MeSH PA D007202 Indicators and Reagents
MeSH PA D019275 Radiopharmaceuticals

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Neuroendocrine tumor indication 255046005 DOID:169




🐶 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
10mCi/ML LUTATHERA AAA USA INC N208700 Jan. 26, 2018 RX SOLUTION INTRAVENOUS Jan. 26, 2023 NEW CHEMICAL ENTITY
10mCi/ML LUTATHERA AAA USA INC N208700 Jan. 26, 2018 RX SOLUTION INTRAVENOUS Jan. 26, 2025 TREATMENT OF SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS) INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS IN ADULTS

Bioactivity Summary:

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

External reference:

IDSource
C3272344 UMLSCUI
CHEMBL3989924 ChEMBL_ID
132274234 PUBCHEM_CID
D11033 KEGG_DRUG
C447941 MESH_SUPPLEMENTAL_RECORD_UI
DB13985 DRUGBANK_ID
1999335 RXNORM
269294 MMSL
33651 MMSL
d08729 MMSL
4041266 VANDF
4041268 VANDF
017456 NDDF

Pharmaceutical products:

None