All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

lutetium (177Lu) oxodotreotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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	292.89	36.40	107	2160	106763	90519417
Metastases to liver	82.78	36.40	30	2237	28777	90597403
Carcinoid crisis	76.65	36.40	12	2255	286	90625894
Abdominal pain	60.41	36.40	61	2206	395660	90230520
Thrombocytopenia	57.50	36.40	45	2222	208680	90417500
Platelet count decreased	57.13	36.40	38	2229	136931	90489249
Carcinoid syndrome	50.20	36.40	8	2259	214	90625966
Lymphocyte count decreased	43.50	36.40	20	2247	35030	90591150
Ill-defined disorder	42.72	36.40	36	2231	184855	90441325
Ascites	40.49	36.40	21	2246	47719	90578461
Myelodysplastic syndrome	39.31	36.40	16	2251	20887	90605293
Neuroendocrine tumour	39.01	36.40	8	2259	893	90625287
General physical health deterioration	37.19	36.40	45	2222	355070	90271110

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
Malignant neoplasm progression	269.54	29.40	131	2475	108269	42510460
Metastases to liver	159.04	29.40	53	2553	16273	42602456
Ill-defined disorder	116.46	29.40	42	2564	16254	42602475
Platelet count decreased	60.58	29.40	57	2549	138524	42480205
Metastases to bone	55.67	29.40	24	2582	14785	42603944
Disease progression	51.43	29.40	53	2553	143603	42475126
Pancreatic neuroendocrine tumour	46.22	29.40	9	2597	311	42618418
Blood chromogranin A increased	45.99	29.40	9	2597	319	42618410
General physical health deterioration	38.94	29.40	47	2559	151199	42467530
Lymphocyte count decreased	36.11	29.40	22	2584	27787	42590942
Carcinoid syndrome	34.30	29.40	6	2600	113	42618616
Hepatic lesion	29.88	29.40	11	2595	4483	42614246

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
Malignant neoplasm progression	394.56	28.60	164	3483	174403	110411249
Metastases to liver	185.99	28.60	62	3585	35324	110550328
Platelet count decreased	95.81	28.60	71	3576	230372	110355280
Carcinoid crisis	92.43	28.60	16	3631	539	110585113
Carcinoid syndrome	73.36	28.60	12	3635	285	110585367
Abdominal pain	68.15	28.60	84	3563	512905	110072747
Metastases to bone	65.48	28.60	28	3619	31344	110554308
Lymphocyte count decreased	60.58	28.60	32	3615	57211	110528441
Hepatic lesion	57.26	28.60	18	3629	8475	110577177
Thrombocytopenia	49.27	28.60	59	3588	348826	110236826
Carcinoid heart disease	39.88	28.60	6	3641	81	110585571
Blood chromogranin A increased	38.45	28.60	8	3639	725	110584927
Decreased appetite	37.80	28.60	61	3586	475785	110109867
Neuroendocrine tumour	37.39	28.60	9	3638	1578	110584074
Nausea	31.93	28.60	101	3546	1235589	109350063
Ill-defined disorder	31.59	28.60	32	3615	156821	110428831
Myelodysplastic syndrome	31.49	28.60	18	3629	37466	110548186
Disease progression	30.73	28.60	39	3608	243995	110341657
Ascites	30.63	28.60	25	3622	92783	110492869
Lymphopenia	30.33	28.60	18	3629	40152	110545500
Anaemia	29.18	28.60	59	3588	547027	110038625

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	D007202	Indicators and Reagents
MeSH PA	D019275	Radiopharmaceuticals
MeSH PA	D064907	Diagnostic Uses of Chemicals

Related Drugs by ATC class:

V10XX Various therapeutic radiopharmaceuticals 4 drugs

ibritumomab tiuxetanlutetium (177Lu) vipivotide tetraxetanradium Ra 223 dichloridesodium phosphate (32P)

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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	12144873	July 25, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	12151003	July 25, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	12161732	July 25, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	12168063	July 25, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	12415003	July 25, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	12491272	July 25, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS

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	April 23, 2027	NEW PATIENT POPULATION
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	Oct. 23, 2027	PEDIATRIC EXCLUSIVITY
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	April 23, 2031	TREATMENT OF PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH SOMATOSTATIN RECEPTOR-POSITIVE GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS (GEP-NETS), INCLUDING FOREGUT, MIDGUT, AND HINDGUT NEUROENDOCRINE TUMORS
10mCi/ML	LUTATHERA	AAA USA INC	N208700	Jan. 26, 2018	RX	SOLUTION	INTRAVENOUS	Oct. 23, 2031	PEDIATRIC EXCLUSIVITY

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
4041266	VANDF
4041268	VANDF
C3272344	UMLSCUI
CHEBI:757020	CHEBI
CHEMBL4297545	ChEMBL_ID
131952892	PUBCHEM_CID
D11033	KEGG_DRUG
C447941	MESH_SUPPLEMENTAL_RECORD_UI
DB13985	DRUGBANK_ID
269294	MMSL
33651	MMSL
d08729	MMSL
017456	NDDF
1999335	RXNORM

Pharmaceutical products:

None