Scroll

lanreotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
peptides and glycopeptides	1546	108736-35-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lanreotide angiopeptin ipstyl lanreotide autogel somatulin-autogel somatuline lanreotide acetate	synthetic octapeptide analog of somatostatin; inhibits accelerated transplant atherosclerosis in rabbit heart arteries Molecular weight: 1096.33 Formula: C54H69N11O10S2 CLOGP: 3.42 LIPINSKI: 3 HAC: 21 HDO: 13 TPSA: 355.08 ALOGS: -5.34 ROTB: 17 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lanreotide
angiopeptin
ipstyl
lanreotide autogel
somatulin-autogel
somatuline
lanreotide acetate

synthetic octapeptide analog of somatostatin; inhibits accelerated transplant atherosclerosis in rabbit heart arteries

Molecular weight: 1096.33
Formula: C54H69N11O10S2
CLOGP: 3.42
LIPINSKI: 3
HAC: 21
HDO: 13
TPSA: 355.08
ALOGS: -5.34
ROTB: 17

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
3	mg	P

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	0.20 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.03 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Aug. 30, 2007	FDA	IPSEN PHARMA
Dec. 12, 2020	PMDA	TEIJIN PHARMA LIMITED

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
Inappropriate schedule of product administration	303.28	19.56	173	8224	71658	50525069
Injection site mass	193.60	19.56	79	8318	15601	50581126
Insulin-like growth factor increased	193.37	19.56	41	8356	777	50595950
Diarrhoea	156.85	19.56	317	8080	588159	50008568
Injection site pain	120.16	19.56	118	8279	110906	50485821
Cholelithiasis	102.68	19.56	69	8328	37904	50558823
Abdominal pain	89.89	19.56	149	8248	236079	50360648
Blood growth hormone increased	86.89	19.56	19	8378	418	50596309
Flatulence	83.17	19.56	55	8342	29403	50567324
Abdominal distension	79.73	19.56	78	8319	72825	50523902
Neoplasm progression	74.09	19.56	51	8346	29106	50567621
Off label use	55.10	19.56	188	8209	474238	50122489
Disease progression	52.81	19.56	72	8325	95794	50500933
Injection site nodule	52.25	19.56	20	8377	3328	50593399
Carcinoid tumour pulmonary	44.68	19.56	11	8386	412	50596315
Carcinoid crisis	40.17	19.56	9	8388	222	50596505
Intestinal obstruction	40.12	19.56	34	8363	26349	50570378
Blood glucose increased	39.91	19.56	54	8343	71270	50525457
Abdominal pain upper	38.59	19.56	83	8314	159226	50437501
Product dose omission issue	38.09	19.56	90	8307	183748	50412979
Terminal state	38.00	19.56	14	8383	2096	50594631
Weight decreased	36.16	19.56	99	8298	221146	50375581
Hypoglycaemia	35.33	19.56	44	8353	53537	50543190
Blood glucose decreased	35.19	19.56	27	8370	18184	50578543
Nausea	34.61	19.56	217	8180	705181	49891546
Needle issue	34.59	19.56	19	8378	7256	50589471
Insulinoma	30.77	19.56	6	8391	73	50596654
Asthenia	30.59	19.56	119	8278	318923	50277804
Incorrect route of product administration	30.34	19.56	25	8372	18641	50578086
Steatorrhoea	30.33	19.56	8	8389	396	50596331
Product administered at inappropriate site	29.07	19.56	12	8385	2431	50594296
Carcinoid syndrome	28.68	19.56	6	8391	106	50596621
Menopausal symptoms	27.62	19.56	11	8386	2032	50594695
Bronchiolitis	25.99	19.56	11	8386	2370	50594357
Pituitary tumour removal	24.59	19.56	4	8393	15	50596712
Drug hypersensitivity	24.10	19.56	6	8391	251004	50345723
Vomiting	23.90	19.56	144	8253	460614	50136113
Blood chromogranin A increased	23.82	19.56	6	8391	247	50596480
Flushing	23.67	19.56	41	8356	66974	50529753
Faeces pale	23.60	19.56	9	8388	1482	50595245
Injection site haemorrhage	23.59	19.56	23	8374	21323	50575404
Constipation	23.55	19.56	76	8321	185632	50411095
Postoperative adhesion	23.37	19.56	6	8391	267	50596460
Injection site pruritus	23.20	19.56	31	8366	40380	50556347
Malaise	22.86	19.56	113	8284	335419	50261308
Gastroenteropancreatic neuroendocrine tumour disease	22.63	19.56	4	8393	27	50596700
Toxicity to various agents	22.61	19.56	4	8393	212495	50384232
Thyroid neoplasm	21.92	19.56	11	8386	3496	50593231
Malignant neoplasm progression	21.90	19.56	40	8357	68084	50528643
Muscle neoplasm	21.61	19.56	4	8393	36	50596691
Neoplasm	21.55	19.56	13	8384	5915	50590812
Injection site hypoaesthesia	21.37	19.56	6	8391	376	50596351
Gallbladder neoplasm	21.32	19.56	4	8393	39	50596688
Lymphatic system neoplasm	21.23	19.56	4	8393	40	50596687
Biliary dilatation	21.17	19.56	9	8388	1960	50594767
Metastases to liver	20.99	19.56	21	8376	20083	50576644
Spleen disorder	20.69	19.56	7	8390	817	50595910
Decreased appetite	20.07	19.56	76	8321	200847	50395880
Body height increased	19.93	19.56	4	8393	57	50596670

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
Inappropriate schedule of product administration	194.51	21.79	113	5245	44359	29524810
Diarrhoea	153.56	21.79	239	5119	332459	29236710
Injection site pain	137.89	21.79	81	5277	32365	29536804
Insulin-like growth factor increased	135.59	21.79	33	5325	1078	29568091
Neoplasm progression	116.40	21.79	60	5298	18552	29550617
Injection site mass	105.46	21.79	39	5319	5416	29563753
Abdominal pain	84.90	21.79	113	5245	135244	29433925
Flatulence	74.58	21.79	44	5314	17665	29551504
Injection site haemorrhage	70.20	21.79	33	5325	8353	29560816
Disease progression	68.32	21.79	79	5279	81837	29487332
Off label use	67.88	21.79	160	5198	300640	29268529
Cholelithiasis	67.32	21.79	42	5316	18630	29550539
Carcinoid heart disease	60.93	21.79	9	5349	12	29569157
Incorrect route of product administration	48.53	21.79	28	5330	10773	29558396
Pituitary tumour removal	38.08	21.79	5	5353	0	29569169
Injection site nodule	33.98	21.79	12	5346	1458	29567711
Terminal state	33.13	21.79	15	5343	3479	29565690
Injection site abscess	29.38	21.79	9	5349	700	29568469
Abdominal pain upper	29.35	21.79	45	5313	60948	29508221
Pancreatic neuroendocrine tumour metastatic	29.21	21.79	6	5352	88	29569081
Pituitary tumour benign	28.47	21.79	9	5349	777	29568392
Hepatic neoplasm	27.83	21.79	11	5347	1825	29567344
Metastases to liver	26.80	21.79	20	5338	11836	29557333
Insulin-like growth factor abnormal	26.80	21.79	4	5354	6	29569163
Abdominal distension	26.62	21.79	37	5321	45874	29523295
Steatorrhoea	25.36	21.79	8	5350	686	29568483
Keratitis	24.65	21.79	9	5349	1203	29567966
Hepatic pain	24.55	21.79	9	5349	1216	29567953
Product dose omission issue	24.55	21.79	54	5304	96329	29472840
Growth hormone deficiency	23.86	21.79	6	5352	224	29568945
Carcinoid crisis	23.69	21.79	6	5352	231	29568938
Asthenia	22.84	21.79	88	5270	215162	29354007
Nausea	22.07	21.79	107	5251	289148	29280021

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
Inappropriate schedule of product administration	308.14	18.42	197	11418	92089	64395028
Insulin-like growth factor increased	232.51	18.42	55	11560	1597	64485520
Diarrhoea	230.34	18.42	440	11175	722264	63764853
Injection site mass	173.45	18.42	77	11538	17193	64469924
Injection site pain	172.56	18.42	150	11465	111258	64375859
Abdominal pain	157.19	18.42	234	11381	312141	64174976
Flatulence	143.82	18.42	86	11529	35580	64451537
Neoplasm progression	137.81	18.42	88	11527	40876	64446241
Cholelithiasis	129.37	18.42	88	11527	45418	64441699
Abdominal distension	91.35	18.42	99	11516	95895	64391222
Off label use	81.46	18.42	274	11341	632532	63854585
Disease progression	78.03	18.42	111	11504	141569	64345548
Injection site nodule	65.88	18.42	24	11591	3206	64483911
Blood growth hormone increased	58.58	18.42	15	11600	607	64486510
Terminal state	58.44	18.42	24	11591	4420	64482697
Injection site haemorrhage	57.46	18.42	42	11573	24236	64462881
Weight decreased	54.98	18.42	143	11472	285596	64201521
Pituitary tumour removal	51.25	18.42	8	11607	19	64487098
Intestinal obstruction	50.37	18.42	46	11569	36240	64450877
Nausea	50.00	18.42	275	11340	785525	63701592
Abdominal pain upper	49.52	18.42	102	11513	174928	64312189
Asthenia	49.34	18.42	179	11436	427865	64059252
Incorrect route of product administration	47.79	18.42	37	11578	23261	64463856
Product dose omission issue	47.65	18.42	107	11508	194640	64292477
Blood glucose increased	46.97	18.42	72	11543	98001	64389116
Carcinoid tumour pulmonary	46.40	18.42	11	11604	322	64486795
Carcinoid heart disease	45.71	18.42	8	11607	46	64487071
Metastases to liver	42.65	18.42	35	11580	23906	64463211
Injection site abscess	42.52	18.42	14	11601	1384	64485733
Steatorrhoea	41.43	18.42	12	11603	774	64486343
Malignant neoplasm progression	40.78	18.42	73	11542	112798	64374319
Blood chromogranin A increased	39.79	18.42	10	11605	375	64486742
Hepatic neoplasm	38.37	18.42	16	11599	3061	64484056
Carcinoid crisis	38.15	18.42	10	11605	444	64486673
Vomiting	37.73	18.42	197	11418	550920	63936197
Blood glucose decreased	37.45	18.42	32	11583	23091	64464026
Insulin-like growth factor abnormal	36.29	18.42	6	11609	23	64487094
Insulinoma	34.83	18.42	7	11608	92	64487025
Hypoglycaemia	33.57	18.42	59	11556	89833	64397284
Drug interaction	33.02	18.42	12	11603	362071	64125046
Constipation	31.68	18.42	102	11513	229235	64257882
Flushing	31.17	18.42	53	11562	78595	64408522
Menopausal symptoms	29.43	18.42	11	11604	1579	64485538
Drug hypersensitivity	29.41	18.42	4	11611	237811	64249306
Pituitary tumour	29.37	18.42	10	11605	1096	64486021
Needle issue	28.89	18.42	19	11596	9253	64477864
Pituitary tumour benign	28.85	18.42	12	11603	2281	64484836
Metastases to bone	28.54	18.42	26	11589	20409	64466708
Faeces pale	27.53	18.42	12	11603	2559	64484558
Thyroid neoplasm	27.15	18.42	12	11603	2645	64484472
Carcinoid syndrome	26.06	18.42	6	11609	154	64486963
Growth hormone deficiency	26.02	18.42	7	11608	344	64486773
Biliary obstruction	25.76	18.42	13	11602	3851	64483266
Tumour necrosis	25.12	18.42	10	11605	1699	64485418
Injection site hypoaesthesia	24.89	18.42	7	11608	406	64486711
Gallbladder neoplasm	24.45	18.42	5	11610	72	64487045
Acromegaly	24.02	18.42	5	11610	79	64487038
Hepatic pain	23.97	18.42	12	11603	3496	64483621
Pneumonia	23.05	18.42	41	11574	559535	63927582
Hepatic embolisation	22.71	18.42	4	11611	24	64487093
Injection site induration	22.37	18.42	16	11599	8916	64478201
Gastroenteropancreatic neuroendocrine tumour disease	21.94	18.42	4	11611	30	64487087
Keratitis	21.90	18.42	11	11604	3226	64483891
Postoperative adhesion	21.79	18.42	6	11609	322	64486795
Hepatobiliary disease	21.71	18.42	7	11608	647	64486470
Hormone level abnormal	21.65	18.42	9	11606	1708	64485409
Rash	21.32	18.42	31	11584	458518	64028599
Biliary colic	21.26	18.42	11	11604	3433	64483684
Headache	21.05	18.42	165	11450	529302	63957815
Neoplasm	20.92	18.42	14	11601	7017	64480100
Decreased appetite	20.87	18.42	103	11512	281186	64205931
Bronchiolitis	20.68	18.42	11	11604	3630	64483487
Lymphatic system neoplasm	20.56	18.42	4	11611	44	64487073
Bile duct stone	20.03	18.42	12	11603	4966	64482151
Cholecystitis	19.96	18.42	21	11594	19615	64467502
Muscle neoplasm	19.94	18.42	4	11611	52	64487065
Injection site pruritus	19.84	18.42	29	11586	37797	64449320
Fatigue	19.50	18.42	213	11402	748517	63738600
Malaise	19.49	18.42	130	11485	396117	64091000
Product administered at inappropriate site	19.39	18.42	10	11605	3100	64484017
Biliary dilatation	19.25	18.42	9	11606	2259	64484858

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	H01CB03	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Somatostatin and analogues
FDA MoA	N0000000194	Somatostatin Receptor Agonists
MeSH PA	D000970	Antineoplastic Agents
FDA EPC	N0000175904	Somatostatin Analog

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

Disease	Relation	SNOMED_ID	DOID
Acromegaly	indication	74107003	DOID:2449
Hypersomatotropic gigantism	indication	86073008
Thyroid-stimulating hormone secreting pituitary tumour	indication	127024001	DOID:1785
Hypertensive disorder	contraindication	38341003	DOID:10763
Disorder of gallbladder	contraindication	39621005	DOID:0060262
Hypothyroidism	contraindication	40930008	DOID:1459
Bradycardia	contraindication	48867003
Hyperglycemia	contraindication	80394007	DOID:4195
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409
Hypoglycemic disorder	contraindication	237630007
Calculus in biliary tract	contraindication	266474003

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.65	acidic
pKa2	12.16	acidic
pKa3	12.71	acidic
pKa4	13.18	acidic
pKa5	13.43	acidic
pKa6	13.67	acidic
pKa7	10.31	Basic
pKa8	6.97	Basic

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
EQ 120MG BASE/0.5ML (EQ 120MG BASE/0.5ML)	SOMATULINE DEPOT	IPSEN PHARMA	N022074	Aug. 30, 2007	RX	SOLUTION	SUBCUTANEOUS	Sept. 15, 2024	TREATMENT OF ADULTS WITH CARCINOID SYNDROME; WHEN USED, IT REDUCES THE FREQUENCY OF SHORT-ACTING SOMATOSTATIN ANALOG RESCUE THERAPY
EQ 60MG BASE/0.2ML (EQ 60MG BASE/0.2ML)	SOMATULINE DEPOT	IPSEN PHARMA	N022074	Aug. 30, 2007	RX	SOLUTION	SUBCUTANEOUS	Sept. 15, 2024	TREATMENT OF ADULTS WITH CARCINOID SYNDROME; WHEN USED, IT REDUCES THE FREQUENCY OF SHORT-ACTING SOMATOSTATIN ANALOG RESCUE THERAPY
EQ 90MG BASE/0.3ML (EQ 90MG BASE/0.3ML)	SOMATULINE DEPOT	IPSEN PHARMA	N022074	Aug. 30, 2007	RX	SOLUTION	SUBCUTANEOUS	Sept. 15, 2024	TREATMENT OF ADULTS WITH CARCINOID SYNDROME; WHEN USED, IT REDUCES THE FREQUENCY OF SHORT-ACTING SOMATOSTATIN ANALOG RESCUE THERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Somatostatin receptor type 2	GPCR	P30874	SSR2_HUMAN	AGONIST	Ki	9.60	IUPHAR	CHEMBL
Somatostatin receptor type 5	GPCR	P35346	SSR5_HUMAN	AGONIST	Ki	9.30	IUPHAR	CHEMBL
Somatostatin receptor type 1	GPCR	P30872	SSR1_HUMAN		Ki	6.30	PDSP
Somatostatin receptor type 4	GPCR	P31391	SSR4_HUMAN		Ki	7.18	PDSP
Somatostatin receptor type 3	GPCR	P32745	SSR3_HUMAN	AGONIST	Ki	8	IUPHAR
Somatostatin receptor type 2	GPCR		SSR2_MOUSE	AGONIST	Ki	9.10	IUPHAR
Somatostatin receptor type 3	GPCR		SSR3_MOUSE	AGONIST	IC50	8.20	IUPHAR
Somatostatin receptor type 5	GPCR		SSR5_RAT	AGONIST	Ki	7.60	IUPHAR
Somatostatin receptor type 2	GPCR		SSR2_RAT	AGONIST	Ki	8.80	IUPHAR
Somatostatin receptor type 3	GPCR		SSR3_RAT	AGONIST	Ki	6.90	IUPHAR

External reference:

ID	Source
4026631	VUID
N0000179366	NUI
D04666	KEGG_DRUG
127984-74-1	SECONDARY_CAS_RN
4026631	VANDF
C0209211	UMLSCUI
CHEBI:135901	CHEBI
CHEMBL1201185	ChEMBL_ID
CHEMBL1201184	ChEMBL_ID
DB06791	DRUGBANK_ID
C060347	MESH_SUPPLEMENTAL_RECORD_UI
2031	IUPHAR_LIGAND_ID
6649	INN_ID
0G3DE8943Y	UNII
6918011	PUBCHEM_CID
236167	RXNORM
18121	MMSL
354365	MMSL
d04961	MMSL
005272	NDDF
005273	NDDF
327379003	SNOMEDCT_US
395765000	SNOMEDCT_US
429611006	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SOMATULINE DEPOT	HUMAN PRESCRIPTION DRUG LABEL	1	15054-1060	INJECTION	60 mg	SUBCUTANEOUS	NDA	29 sections
SOMATULINE DEPOT	HUMAN PRESCRIPTION DRUG LABEL	1	15054-1060	INJECTION	60 mg	SUBCUTANEOUS	NDA	29 sections
SOMATULINE DEPOT	HUMAN PRESCRIPTION DRUG LABEL	1	15054-1090	INJECTION	90 mg	SUBCUTANEOUS	NDA	29 sections
SOMATULINE DEPOT	HUMAN PRESCRIPTION DRUG LABEL	1	15054-1090	INJECTION	90 mg	SUBCUTANEOUS	NDA	29 sections
SOMATULINE DEPOT	HUMAN PRESCRIPTION DRUG LABEL	1	15054-1120	INJECTION	120 mg	SUBCUTANEOUS	NDA	29 sections
SOMATULINE DEPOT	HUMAN PRESCRIPTION DRUG LABEL	1	15054-1120	INJECTION	120 mg	SUBCUTANEOUS	NDA	29 sections
Lanreotide Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	69097-870	INJECTION	120 mg	SUBCUTANEOUS	NDA	26 sections
Lanreotide Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	69097-880	INJECTION	60 mg	SUBCUTANEOUS	NDA	26 sections
Lanreotide Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	69097-890	INJECTION	90 mg	SUBCUTANEOUS	NDA	26 sections