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

Stem definition	Drug id	CAS RN
somatostatin receptor agonists/antagonists	5275	437608-50-9

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	108.87	35.45	43	980	82078	63405921
Abdominal pain	52.94	35.45	41	982	293415	63194584
Metastases to liver	48.09	35.45	17	1006	23622	63464377
Neuroendocrine tumour	43.92	35.45	8	1015	750	63487249

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Metastases to liver	133.30	28.07	40	1342	13623	34941926
Malignant neoplasm progression	82.16	28.07	48	1334	87998	34867551
Disease progression	54.21	28.07	40	1342	108037	34847512
Ill-defined disorder	52.56	28.07	20	1362	13889	34941660
Blood chromogranin A increased	38.15	28.07	7	1375	274	34955275
Metastases to bone	37.39	28.07	15	1367	11955	34943594
Pancreatic neuroendocrine tumour	32.17	28.07	6	1376	257	34955292
Carcinoid syndrome	30.16	28.07	5	1377	107	34955442
Hepatic lesion	28.22	28.07	9	1373	3703	34951846

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Metastases to liver	126.87	29.85	40	1745	28274	79714329
Malignant neoplasm progression	107.99	29.85	55	1730	135935	79606668
Hepatic lesion	58.34	29.85	16	1769	6943	79735660
Abdominal pain	51.92	29.85	53	1732	389516	79353087
Metastases to bone	45.53	29.85	18	1767	24409	79718194
Carcinoid syndrome	36.93	29.85	6	1779	204	79742399
Platelet count decreased	34.38	29.85	31	1754	194633	79547970
Blood chromogranin A increased	31.70	29.85	6	1779	496	79742107
Neuroendocrine tumour	31.19	29.85	7	1778	1337	79741266

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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 | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

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

External reference:

ID	Source
C3272344	UMLSCUI
CHEMBL3989924	ChEMBL_ID
76966897	PUBCHEM_CID
D11033	KEGG_DRUG
C447941	MESH_SUPPLEMENTAL_RECORD_UI
DB13985	DRUGBANK_ID
269294	MMSL
33651	MMSL
d08729	MMSL
017456	NDDF
4041266	VANDF
4041268	VANDF
1999335	RXNORM

Pharmaceutical products:

None