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

Stem definition	Drug id	CAS RN
peptides and glycopeptides	4329	396091-73-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pasireotide pasireotide disapartate SOM 230 SOM230 signifor pasireotide diaspartate pasireotide embonate pasireotide pamoate	a somatostatin analog with pharmacologic properties mimicking those of the natural hormone somatostatin binds and activates the SSTRs resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion Molecular weight: 1047.23 Formula: C58H66N10O9 CLOGP: 6.74 LIPINSKI: 4 HAC: 19 HDO: 9 TPSA: 281.20 ALOGS: -5.71 ROTB: 18 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pasireotide
pasireotide disapartate
SOM 230
SOM230
signifor
pasireotide diaspartate
pasireotide embonate
pasireotide pamoate

a somatostatin analog with pharmacologic properties mimicking those of the natural hormone somatostatin binds and activates the SSTRs resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion

Molecular weight: 1047.23
Formula: C58H66N10O9
CLOGP: 6.74
LIPINSKI: 4
HAC: 19
HDO: 9
TPSA: 281.20
ALOGS: -5.71
ROTB: 18

Status: ONP

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

Drug dosage:

Dose	Unit	Route
1.20	mg	P

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Hosey CM, Chan R, Benet LZ
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 14, 2012	FDA	NOVARTIS

FDA Adverse Event Reporting System (Female)

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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
Hyperglycaemia	385.19	32.90	117	2401	41750	63444754
Diabetes mellitus	364.17	32.90	120	2398	55690	63430814
Glycosylated haemoglobin increased	89.89	32.90	29	2489	12369	63474135
Blood glucose increased	73.34	32.90	44	2474	83712	63402792
Cholelithiasis	66.00	32.90	33	2485	43892	63442612
Adrenal insufficiency	64.84	32.90	25	2493	17890	63468614
Hypoglycaemia	56.31	32.90	33	2485	60032	63426472
Insulin-like growth factor increased	46.20	32.90	10	2508	909	63485595
Polyuria	42.24	32.90	15	2503	8527	63477977
Insulin-like growth factor decreased	41.89	32.90	8	2510	388	63486116

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FDA Adverse Event Reporting System (Male)

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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
Hyperglycaemia	164.24	38.99	53	765	39427	34916686
Diabetes mellitus	132.02	38.99	47	771	46826	34909287

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FDA Adverse Event Reporting System (Geriatric)

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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
Hyperglycaemia	427.75	29.58	143	2980	70192	79671073
Diabetes mellitus	420.33	29.58	145	2978	78245	79663020
Glycosylated haemoglobin increased	96.42	29.58	34	3089	19226	79722039
Adrenal insufficiency	90.38	29.58	36	3087	28451	79712814
Cholelithiasis	80.89	29.58	40	3083	52624	79688641
Polyuria	69.43	29.58	25	3098	14989	79726276
Hypoglycaemia	68.41	29.58	45	3078	101549	79639716
Diabetes mellitus inadequate control	64.43	29.58	27	3096	24237	79717028
Blood glucose increased	63.36	29.58	45	3078	114930	79626335
Cortisol increased	57.74	29.58	11	3112	534	79740731

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	H01CB05	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Somatostatin and analogues
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50266	Prodrugs
FDA EPC	N0000175904	Somatostatin Analog
FDA MoA	N0000000194	Somatostatin Receptor Agonists
MeSH PA	D006728	Hormones

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

Disease	Relation	SNOMED_ID	DOID
Hypercortisolism	indication	47270006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.8	acidic
pKa2	13.26	acidic
pKa3	13.4	acidic
pKa4	13.93	acidic
pKa5	10.31	Basic
pKa6	8.91	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 20MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	Dec. 15, 2014	RX	FOR SUSPENSION	INTRAMUSCULAR	8822637	Aug. 6, 2023	METHOD OF TREATING ACROMEGALY
EQ 40MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	Dec. 15, 2014	RX	FOR SUSPENSION	INTRAMUSCULAR	8822637	Aug. 6, 2023	METHOD OF TREATING ACROMEGALY
EQ 60MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	Dec. 15, 2014	RX	FOR SUSPENSION	INTRAMUSCULAR	8822637	Aug. 6, 2023	METHOD OF TREATING ACROMEGALY

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	June 29, 2018	RX	FOR SUSPENSION	INTRAMUSCULAR	June 29, 2025	INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 20MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	Dec. 15, 2014	RX	FOR SUSPENSION	INTRAMUSCULAR	June 29, 2025	INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 30MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	June 29, 2018	RX	FOR SUSPENSION	INTRAMUSCULAR	June 29, 2025	INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 40MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	Dec. 15, 2014	RX	FOR SUSPENSION	INTRAMUSCULAR	June 29, 2025	INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 60MG BASE/VIAL	SIGNIFOR LAR KIT	RECORDATI RARE	N203255	Dec. 15, 2014	RX	FOR SUSPENSION	INTRAMUSCULAR	June 29, 2025	INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Somatostatin receptor type 2	GPCR	P30874	SSR2_HUMAN	AGONIST	IC50	9	IUPHAR	CHEMBL
Somatostatin receptor type 3	GPCR	P32745	SSR3_HUMAN	AGONIST	IC50	8.80	IUPHAR	CHEMBL
Somatostatin receptor type 5	GPCR	P35346	SSR5_HUMAN	AGONIST	IC50	9.80	IUPHAR	CHEMBL
Somatostatin receptor type 1	GPCR	P30872	SSR1_HUMAN	AGONIST	IC50	8	IUPHAR	CHEMBL
Somatostatin receptor type 2	GPCR		SSR2_RAT	AGONIST	EC50	9.07	IUPHAR

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External reference:

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ID	Source
014802	NDDF
014803	NDDF
015818	NDDF
1364104	RXNORM
192917	MMSL
2018	IUPHAR_LIGAND_ID
28816	MMSL
29021	MMSL
30767	MMSL
396091-79-5	SECONDARY_CAS_RN

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0633	INJECTION	0.30 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0634	INJECTION	0.60 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0635	INJECTION	0.90 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	55292-131	INJECTION	0.30 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	55292-131	INJECTION	0.30 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	55292-132	INJECTION	0.60 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	55292-132	INJECTION	0.60 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	55292-133	INJECTION	0.90 mg	SUBCUTANEOUS	NDA	31 sections
Signifor	HUMAN PRESCRIPTION DRUG LABEL	1	55292-133	INJECTION	0.90 mg	SUBCUTANEOUS	NDA	31 sections

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