Pasireotide - DrugBank

ID Pharmacology Interactions References Trials Economics Properties Spectra Taxonomy

Targets (4)

Identification

Name

Pasireotide

Accession Number

DB06663

Type

Small Molecule

Groups

Approved

Description

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, which is used in the treatment of Cushing's disease.

Structure

MOL SDF PDB SMILES InChI

Synonyms

cyclo((4R)-4-(2-aminoethylcarbamoyloxy)-L-prolyl-L-phenylglycyl-D-tryptophyl-L-lysyl-4-O-benzyl-L-tyrosyl-L- phenylalanyl-)

Pasireotida

Pasiréotide

Pasireotidum

External IDs

SOM 230 / SOM-230 / SOM230

Product Ingredients

Ingredient	UNII	CAS	InChI Key	Details
Pasireotide diaspartate	I4P76SY3N4	820232-50-6	NEEFMPSSNFRRNC-HQUONIRXSA-N	Details
Pasireotide pamoate	04F55A7UZ3	396091-79-5	HSXBEUMRBMAVDP-QKXVGOHISA-N	Details

Approved Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Signifor	Injection, solution	0.3 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Solution	0.9 mg	Subcutaneous	Novartis	2013-11-28	Not applicable	Canada
Signifor	Injection, solution	0.9 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, powder, for suspension	20 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection	.3 mg/mL	Subcutaneous	Novartis	2012-12-14	Not applicable	US
Signifor	Injection, solution	0.9 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, powder, for suspension	60 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, solution	0.3 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, solution	0.6 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Solution	0.3 mg	Subcutaneous	Novartis	2013-11-26	Not applicable	Canada
Signifor	Injection	.6 mg/mL	Subcutaneous	Novartis	2012-12-14	Not applicable	US
Signifor	Injection, solution	0.3 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, solution	0.9 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, powder, for suspension	40 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, powder, for suspension	60 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, solution	0.6 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Solution	0.6 mg	Subcutaneous	Novartis	2013-11-26	Not applicable	Canada
Signifor	Injection, solution	0.6 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, powder, for suspension	40 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection	.9 mg/mL	Subcutaneous	Novartis	2012-12-14	Not applicable	US
Signifor	Injection, solution	0.3 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, solution	0.9 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor	Injection, solution	0.6 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable	EU
Signifor LAR	Kit			Novartis	2014-12-15	Not applicable	US
Signifor Lar	Kit; Powder, for suspension	20 mg	Intramuscular	Novartis	2016-01-28	Not applicable	Canada
Signifor Lar	Kit; Powder, for suspension	60 mg	Intramuscular	Novartis	2015-08-04	Not applicable	Canada
Signifor LAR	Kit			Novartis	2014-12-15	Not applicable	US
Signifor Lar	Kit; Powder, for suspension	40 mg	Intramuscular	Novartis	2015-08-04	Not applicable	Canada
Signifor LAR	Kit			Novartis	2014-12-15	Not applicable	US

Approved Generic Prescription Products

Not Available

Approved Over the Counter Products

Not Available

Unapproved/Other Products

Not Available

International Brands

Not Available

Brand mixtures

Not Available

Categories

UNII

98H1T17066

CAS number

396091-73-9

Weight

Average: 1047.2062
Monoisotopic: 1046.50142376

Chemical Formula

C₅₈H₆₆N₁₀O₉

InChI Key

VMZMNAABQBOLAK-DBILLSOUSA-N

InChI

InChI=1S/C58H66N10O9/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72)/t43-,46+,47+,48-,49+,50+,51+/m1/s1

IUPAC Name

(3S,6R,9S,12S,15S,19R,20aS)-9-(4-aminobutyl)-15-benzyl-12-{[4-(benzyloxy)phenyl]methyl}-6-(1H-indol-3-ylmethyl)-1,4,7,10,13,16-hexaoxo-3-phenyl-icosahydropyrrolo[1,2-a]1,4,7,10,13,16-hexaazacyclooctadecan-19-yl N-(2-aminoethyl)carbamate

SMILES

NCCCC[[email protected]@H]1NC(=O)[[email protected]@H](CC2=CNC3=C2C=CC=C3)NC(=O)[[email protected]@H](NC(=O)[[email protected]@H]2C[[email protected]](CN2C(=O)[[email protected]](CC2=CC=CC=C2)NC(=O)[[email protected]](CC2=CC=C(OCC3=CC=CC=C3)C=C2)NC1=O)OC(=O)NCCN)C1=CC=CC=C1

Pharmacology

Indication

For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.

Structured Indications

Pharmacodynamics

Signifor® is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.

Mechanism of action

Pasireotide activates a broad spectrum of somatostatin receptors, exhbiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in Cushing's disease patients. Also this agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin.

Target	Kind	Pharmacological action	Actions	Organism	UniProt ID
Somatostatin receptor type 1	Protein	unknown	Not Available	Human	P30872	details
Somatostatin receptor type 2	Protein	unknown	Not Available	Human	P30874	details
Somatostatin receptor type 3	Protein	unknown	Not Available	Human	P32745	details
Somatostatin receptor type 5	Protein	unknown	Not Available	Human	P35346	details

Absorption

The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC.

Volume of distribution

Pasireotide is widely distributed and has a volume of distribution of >100L.

Protein binding

Plasma protein binding is 88%.

Metabolism

Metabolism is minimal.

Route of elimination

Pasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).

Half life

The half-life is 12 hours.

Clearance

The clearance in healthy patient is ~7.6 L/h and in Cushing’s disease patients is ~3.8 L/h.

Toxicity

The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction	Drug group
2,4-thiazolidinedione	The therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Pasireotide.	Investigational
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline	7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Pasireotide.	Experimental
Acarbose	The therapeutic efficacy of Acarbose can be decreased when used in combination with Pasireotide.	Approved, Investigational
Acebutolol	Acebutolol may increase the bradycardic activities of Pasireotide.	Approved
Acetohexamide	The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Pasireotide.	Withdrawn
Acetylsalicylic acid	Acetylsalicylic acid may increase the hypoglycemic activities of Pasireotide.	Approved, Vet Approved
AICA ribonucleotide	The therapeutic efficacy of Aicar can be decreased when used in combination with Pasireotide.	Experimental
Alogliptin	The therapeutic efficacy of Alogliptin can be decreased when used in combination with Pasireotide.	Approved
Aminosalicylic Acid	Aminosalicylic Acid may increase the hypoglycemic activities of Pasireotide.	Approved
Amiodarone	Pasireotide may increase the QTc-prolonging activities of Amiodarone.	Approved, Investigational
Anagrelide	Pasireotide may increase the QTc-prolonging activities of Anagrelide.	Approved
Arsenic trioxide	Pasireotide may increase the QTc-prolonging activities of Arsenic trioxide.	Approved, Investigational
Artemether	Pasireotide may increase the QTc-prolonging activities of Artemether.	Approved
Asenapine	Pasireotide may increase the QTc-prolonging activities of Asenapine.	Approved
Atenolol	Atenolol may increase the bradycardic activities of Pasireotide.	Approved
Azithromycin	Pasireotide may increase the QTc-prolonging activities of Azithromycin.	Approved
Balaglitazone	The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Pasireotide.	Investigational
Balsalazide	Balsalazide may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Bedaquiline	Pasireotide may increase the QTc-prolonging activities of Bedaquiline.	Approved
Bendroflumethiazide	Bendroflumethiazide may increase the bradycardic activities of Pasireotide.	Approved
Benmoxin	Benmoxin may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Beractant	Pasireotide may increase the bradycardic activities of Beractant.	Approved
Betaxolol	Betaxolol may increase the bradycardic activities of Pasireotide.	Approved
Bisoprolol	Bisoprolol may increase the bradycardic activities of Pasireotide.	Approved
Bretylium	Bretylium may increase the bradycardic activities of Pasireotide.	Approved
Bromocriptine	The serum concentration of Bromocriptine can be increased when it is combined with Pasireotide.	Approved, Investigational
Buformin	The therapeutic efficacy of Buformin can be decreased when used in combination with Pasireotide.	Withdrawn
Calfactant	Calfactant may increase the bradycardic activities of Pasireotide.	Approved
Canagliflozin	The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Pasireotide.	Approved
Caroxazone	Caroxazone may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Carteolol	Carteolol may increase the bradycardic activities of Pasireotide.	Approved
Carvedilol	Carvedilol may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Castanospermine	The therapeutic efficacy of Castanospermine can be decreased when used in combination with Pasireotide.	Experimental
Ceritinib	Pasireotide may increase the bradycardic activities of Ceritinib.	Approved
Chloroquine	Pasireotide may increase the QTc-prolonging activities of Chloroquine.	Approved, Vet Approved
Chlorpromazine	Pasireotide may increase the QTc-prolonging activities of Chlorpromazine.	Approved, Vet Approved
Chlorpropamide	Chlorpropamide may increase the hypoglycemic activities of Pasireotide.	Approved
Ciglitazone	The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Pasireotide.	Experimental
Cinoxacin	Cinoxacin may increase the hypoglycemic activities of Pasireotide.	Approved, Withdrawn
Ciprofloxacin	Pasireotide may increase the QTc-prolonging activities of Ciprofloxacin.	Approved, Investigational
Cisapride	Pasireotide may increase the QTc-prolonging activities of Cisapride.	Approved, Investigational, Withdrawn
Citalopram	Pasireotide may increase the QTc-prolonging activities of Citalopram.	Approved
Clarithromycin	Pasireotide may increase the QTc-prolonging activities of Clarithromycin.	Approved
Clonidine	Clonidine may increase the bradycardic activities of Pasireotide.	Approved
Clozapine	Pasireotide may increase the QTc-prolonging activities of Clozapine.	Approved
Codeine	The metabolism of Codeine can be decreased when combined with Pasireotide.	Approved, Illicit
Crizotinib	Pasireotide may increase the QTc-prolonging activities of Crizotinib.	Approved
Cyclosporine	The serum concentration of Cyclosporine can be decreased when it is combined with Pasireotide.	Approved, Investigational, Vet Approved
Dapoxetine	Dapoxetine may increase the hypoglycemic activities of Pasireotide.	Investigational
Deoxyspergualin	The therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Pasireotide.	Investigational
dersalazine	dersalazine may increase the hypoglycemic activities of Pasireotide.	Investigational
Desvenlafaxine	Desvenlafaxine may increase the hypoglycemic activities of Pasireotide.	Approved
Dexmedetomidine	Dexmedetomidine may increase the bradycardic activities of Pasireotide.	Approved, Vet Approved
Diflunisal	Diflunisal may increase the hypoglycemic activities of Pasireotide.	Approved
Digoxin	Digoxin may increase the bradycardic activities of Pasireotide.	Approved
Dihydrotestosterone	Dihydrotestosterone may increase the hypoglycemic activities of Pasireotide.	Illicit
Diltiazem	Diltiazem may increase the bradycardic activities of Pasireotide.	Approved
Disopyramide	Pasireotide may increase the QTc-prolonging activities of Disopyramide.	Approved
Dofetilide	Pasireotide may increase the QTc-prolonging activities of Dofetilide.	Approved
Dolasetron	Pasireotide may increase the QTc-prolonging activities of Dolasetron.	Approved
Domperidone	Pasireotide may increase the QTc-prolonging activities of Domperidone.	Approved, Investigational, Vet Approved
Donepezil	Donepezil may increase the bradycardic activities of Pasireotide.	Approved
Dronedarone	Pasireotide may increase the QTc-prolonging activities of Dronedarone.	Approved
Droperidol	Pasireotide may increase the QTc-prolonging activities of Droperidol.	Approved, Vet Approved
Dulaglutide	The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Pasireotide.	Approved
Duloxetine	Duloxetine may increase the hypoglycemic activities of Pasireotide.	Approved
Eliglustat	Pasireotide may increase the QTc-prolonging activities of Eliglustat.	Approved
Empagliflozin	The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Pasireotide.	Approved
Enoxacin	Enoxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Erythromycin	Pasireotide may increase the QTc-prolonging activities of Erythromycin.	Approved, Vet Approved
Escitalopram	Pasireotide may increase the QTc-prolonging activities of Escitalopram.	Approved, Investigational
Esmolol	Esmolol may increase the bradycardic activities of Pasireotide.	Approved
Etoperidone	Etoperidone may increase the hypoglycemic activities of Pasireotide.	Approved
Exenatide	The therapeutic efficacy of Exenatide can be decreased when used in combination with Pasireotide.	Approved, Investigational
Fingolimod	Pasireotide may increase the bradycardic activities of Fingolimod.	Approved, Investigational
Flecainide	Pasireotide may increase the QTc-prolonging activities of Flecainide.	Approved, Withdrawn
Fleroxacin	Fleroxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Flumequine	Flumequine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Fluoxetine	Pasireotide may increase the QTc-prolonging activities of Fluoxetine.	Approved, Vet Approved
Fluoxymesterone	Fluoxymesterone may increase the hypoglycemic activities of Pasireotide.	Approved, Illicit
Flupentixol	Pasireotide may increase the QTc-prolonging activities of Flupentixol.	Approved, Withdrawn
Fluvoxamine	Fluvoxamine may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Furazolidone	Furazolidone may increase the hypoglycemic activities of Pasireotide.	Approved, Vet Approved
Gadobenic acid	Pasireotide may increase the QTc-prolonging activities of Gadobenic acid.	Approved
Galantamine	Galantamine may increase the bradycardic activities of Pasireotide.	Approved
Garenoxacin	Garenoxacin may increase the hypoglycemic activities of Pasireotide.	Investigational
Gatifloxacin	Gatifloxacin may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Gemifloxacin	Pasireotide may increase the QTc-prolonging activities of Gemifloxacin.	Approved, Investigational
Glibornuride	The therapeutic efficacy of Glibornuride can be decreased when used in combination with Pasireotide.	Withdrawn
Gliclazide	Gliclazide may increase the hypoglycemic activities of Pasireotide.	Approved
Glimepiride	Glimepiride may increase the hypoglycemic activities of Pasireotide.	Approved
Glipizide	Glipizide may increase the hypoglycemic activities of Pasireotide.	Approved
Gliquidone	The therapeutic efficacy of Gliquidone can be decreased when used in combination with Pasireotide.	Approved
Glyburide	Glyburide may increase the hypoglycemic activities of Pasireotide.	Approved
Goserelin	Pasireotide may increase the QTc-prolonging activities of Goserelin.	Approved
Granisetron	Pasireotide may increase the QTc-prolonging activities of Granisetron.	Approved, Investigational
Grepafloxacin	Grepafloxacin may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Guanfacine	Guanfacine may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Gusperimus	The therapeutic efficacy of Gusperimus can be decreased when used in combination with Pasireotide.	Investigational
Haloperidol	Pasireotide may increase the QTc-prolonging activities of Haloperidol.	Approved
Hydracarbazine	Hydracarbazine may increase the hypoglycemic activities of Pasireotide.	Experimental
Ibutilide	Pasireotide may increase the QTc-prolonging activities of Ibutilide.	Approved
Iloperidone	Pasireotide may increase the QTc-prolonging activities of Iloperidone.	Approved
Indalpine	Indalpine may increase the hypoglycemic activities of Pasireotide.	Investigational, Withdrawn
Insulin Aspart	Insulin Aspart may increase the hypoglycemic activities of Pasireotide.	Approved
Insulin Detemir	Insulin Detemir may increase the hypoglycemic activities of Pasireotide.	Approved
Insulin Glargine	Insulin Glargine may increase the hypoglycemic activities of Pasireotide.	Approved
Insulin Glulisine	Insulin Glulisine may increase the hypoglycemic activities of Pasireotide.	Approved
Insulin Human	Insulin Human may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Insulin Lispro	Insulin Lispro may increase the hypoglycemic activities of Pasireotide.	Approved
Insulin Pork	The therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pasireotide.	Approved
Iproclozide	Iproclozide may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Iproniazid	Iproniazid may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Isocarboxazid	Isocarboxazid may increase the hypoglycemic activities of Pasireotide.	Approved
Ivabradine	Pasireotide may increase the bradycardic activities of Ivabradine.	Approved
Labetalol	Labetalol may increase the bradycardic activities of Pasireotide.	Approved
Lacosamide	Pasireotide may increase the atrioventricular blocking (AV block) activities of Lacosamide.	Approved
Lanreotide	Pasireotide may increase the hypoglycemic activities of Lanreotide.	Approved
Lenvatinib	Pasireotide may increase the QTc-prolonging activities of Lenvatinib.	Approved
Leuprolide	Pasireotide may increase the QTc-prolonging activities of Leuprolide.	Approved, Investigational
Levobunolol	Levobunolol may increase the bradycardic activities of Pasireotide.	Approved
Levofloxacin	Pasireotide may increase the QTc-prolonging activities of Levofloxacin.	Approved, Investigational
Levomilnacipran	Levomilnacipran may increase the hypoglycemic activities of Pasireotide.	Approved
Linagliptin	The therapeutic efficacy of Linagliptin can be decreased when used in combination with Pasireotide.	Approved
Liraglutide	The therapeutic efficacy of Liraglutide can be decreased when used in combination with Pasireotide.	Approved
Lomefloxacin	Lomefloxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Lopinavir	Pasireotide may increase the QTc-prolonging activities of Lopinavir.	Approved
Lucinactant	Lucinactant may increase the bradycardic activities of Pasireotide.	Approved
Lumefantrine	Pasireotide may increase the QTc-prolonging activities of Lumefantrine.	Approved
Mebanazine	Mebanazine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Mecasermin	Mecasermin may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Mesalazine	Mesalazine may increase the hypoglycemic activities of Pasireotide.	Approved
Metformin	The therapeutic efficacy of Metformin can be decreased when used in combination with Pasireotide.	Approved
Methadone	Pasireotide may increase the QTc-prolonging activities of Methadone.	Approved
Methyldopa	Methyldopa may increase the bradycardic activities of Pasireotide.	Approved
Methylene blue	Methylene blue may increase the hypoglycemic activities of Pasireotide.	Investigational
Methyltestosterone	Methyltestosterone may increase the hypoglycemic activities of Pasireotide.	Approved
Metipranolol	Metipranolol may increase the bradycardic activities of Pasireotide.	Approved
Metoprolol	Metoprolol may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Mifepristone	Mifepristone may increase the QTc-prolonging activities of Pasireotide.	Approved, Investigational
Miglitol	The therapeutic efficacy of Miglitol can be decreased when used in combination with Pasireotide.	Approved
Miglustat	The therapeutic efficacy of Miglustat can be decreased when used in combination with Pasireotide.	Approved
Milnacipran	Milnacipran may increase the hypoglycemic activities of Pasireotide.	Approved
Minaprine	Minaprine may increase the hypoglycemic activities of Pasireotide.	Approved
Mitiglinide	The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Pasireotide.	Approved, Investigational
Moclobemide	Moclobemide may increase the hypoglycemic activities of Pasireotide.	Approved
Moxifloxacin	Pasireotide may increase the QTc-prolonging activities of Moxifloxacin.	Approved, Investigational
Nadolol	Nadolol may increase the bradycardic activities of Pasireotide.	Approved
Nalidixic Acid	Nalidixic Acid may increase the hypoglycemic activities of Pasireotide.	Approved
Nateglinide	Nateglinide may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Nebivolol	Nebivolol may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Nefazodone	Nefazodone may increase the hypoglycemic activities of Pasireotide.	Approved, Withdrawn
Nemonoxacin	Nemonoxacin may increase the hypoglycemic activities of Pasireotide.	Investigational
Nialamide	Nialamide may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Nilotinib	Pasireotide may increase the QTc-prolonging activities of Nilotinib.	Approved, Investigational
Nitroaspirin	Nitroaspirin may increase the hypoglycemic activities of Pasireotide.	Investigational
Norfloxacin	Norfloxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Octamoxin	Octamoxin may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Octreotide	Octreotide may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Ofloxacin	Pasireotide may increase the QTc-prolonging activities of Ofloxacin.	Approved
Olsalazine	Olsalazine may increase the hypoglycemic activities of Pasireotide.	Approved
Ondansetron	Pasireotide may increase the QTc-prolonging activities of Ondansetron.	Approved
Oxandrolone	Oxandrolone may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Oxymetholone	Oxymetholone may increase the hypoglycemic activities of Pasireotide.	Approved, Illicit
Paliperidone	Pasireotide may increase the QTc-prolonging activities of Paliperidone.	Approved
Panobinostat	Pasireotide may increase the QTc-prolonging activities of Panobinostat.	Approved, Investigational
Pargyline	Pargyline may increase the hypoglycemic activities of Pasireotide.	Approved
Paroxetine	Paroxetine may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Pazopanib	Pasireotide may increase the QTc-prolonging activities of Pazopanib.	Approved
Pazufloxacin	Pazufloxacin may increase the hypoglycemic activities of Pasireotide.	Investigational
Pefloxacin	Pefloxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Pegvisomant	The risk or severity of adverse effects can be increased when Pasireotide is combined with Pegvisomant.	Approved
Penbutolol	Penbutolol may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Pentamidine	Pasireotide may increase the QTc-prolonging activities of Pentamidine.	Approved
Perflutren	Pasireotide may increase the QTc-prolonging activities of Perflutren.	Approved
Phenelzine	Phenelzine may increase the hypoglycemic activities of Pasireotide.	Approved
Phenformin	The therapeutic efficacy of Phenformin can be decreased when used in combination with Pasireotide.	Approved, Withdrawn
Pheniprazine	Pheniprazine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Phenoxypropazine	Phenoxypropazine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Pimozide	Pasireotide may increase the QTc-prolonging activities of Pimozide.	Approved
Pindolol	Pindolol may increase the bradycardic activities of Pasireotide.	Approved
Pioglitazone	The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Pasireotide.	Approved, Investigational
Pirlindole	Pirlindole may increase the hypoglycemic activities of Pasireotide.	Approved
Pivhydrazine	Pivhydrazine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Poractant alfa	Pasireotide may increase the bradycardic activities of Poractant alfa.	Approved
Pramlintide	The therapeutic efficacy of Pramlintide can be decreased when used in combination with Pasireotide.	Approved, Investigational
Primaquine	Pasireotide may increase the QTc-prolonging activities of Primaquine.	Approved
Procainamide	Pasireotide may increase the QTc-prolonging activities of Procainamide.	Approved
Promazine	Pasireotide may increase the QTc-prolonging activities of Promazine.	Approved, Vet Approved
Propafenone	Pasireotide may increase the QTc-prolonging activities of Propafenone.	Approved
Propranolol	Propranolol may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Prulifloxacin	Prulifloxacin may increase the hypoglycemic activities of Pasireotide.	Investigational
Quetiapine	Pasireotide may increase the QTc-prolonging activities of Quetiapine.	Approved
Quinidine	Pasireotide may increase the QTc-prolonging activities of Quinidine.	Approved
Quinine	Pasireotide may increase the QTc-prolonging activities of Quinine.	Approved
Rasagiline	Rasagiline may increase the hypoglycemic activities of Pasireotide.	Approved
Repaglinide	Repaglinide may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Rivastigmine	Rivastigmine may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Rosiglitazone	The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pasireotide.	Approved, Investigational
Rosoxacin	Rosoxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Ruxolitinib	Ruxolitinib may increase the bradycardic activities of Pasireotide.	Approved
Safrazine	Safrazine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Salicylic acid	Salicylic acid may increase the hypoglycemic activities of Pasireotide.	Approved, Vet Approved
Saquinavir	Pasireotide may increase the QTc-prolonging activities of Saquinavir.	Approved, Investigational
Saxagliptin	The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pasireotide.	Approved
Selegiline	Selegiline may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational, Vet Approved
Sertraline	Sertraline may increase the hypoglycemic activities of Pasireotide.	Approved
Sitagliptin	The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide.	Approved, Investigational
Sotalol	Pasireotide may increase the QTc-prolonging activities of Sotalol.	Approved
Sparfloxacin	Sparfloxacin may increase the hypoglycemic activities of Pasireotide.	Approved
Stanozolol	Stanozolol may increase the hypoglycemic activities of Pasireotide.	Approved, Vet Approved
Sufentanil	Sufentanil may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Sulfadiazine	Sulfadiazine may increase the hypoglycemic activities of Pasireotide.	Approved, Vet Approved
Sulfamethoxazole	Sulfamethoxazole may increase the hypoglycemic activities of Pasireotide.	Approved
Sulfisoxazole	Pasireotide may increase the QTc-prolonging activities of Sulfisoxazole.	Approved, Vet Approved
Sulodexide	The therapeutic efficacy of Sulodexide can be decreased when used in combination with Pasireotide.	Approved, Investigational
Sunitinib	Sunitinib may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Telavancin	Pasireotide may increase the QTc-prolonging activities of Telavancin.	Approved
Telithromycin	Pasireotide may increase the QTc-prolonging activities of Telithromycin.	Approved
Temafloxacin	Temafloxacin may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Testosterone	Testosterone may increase the hypoglycemic activities of Pasireotide.	Approved, Investigational
Tetrabenazine	Pasireotide may increase the QTc-prolonging activities of Tetrabenazine.	Approved
Thioridazine	Pasireotide may increase the QTc-prolonging activities of Thioridazine.	Withdrawn
Timolol	Timolol may increase the bradycardic activities of Pasireotide.	Approved
Tizanidine	Tizanidine may increase the bradycardic activities of Pasireotide.	Approved
Tofacitinib	Tofacitinib may increase the bradycardic activities of Pasireotide.	Approved, Investigational
Tolazamide	Tolazamide may increase the hypoglycemic activities of Pasireotide.	Approved
Tolbutamide	Tolbutamide may increase the hypoglycemic activities of Pasireotide.	Approved
Toloxatone	Toloxatone may increase the hypoglycemic activities of Pasireotide.	Approved
Toremifene	Pasireotide may increase the QTc-prolonging activities of Toremifene.	Approved, Investigational
Trans-2-Phenylcyclopropylamine	Trans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Pasireotide.	Experimental
Tranylcypromine	Tranylcypromine may increase the hypoglycemic activities of Pasireotide.	Approved
Troglitazone	The therapeutic efficacy of Troglitazone can be decreased when used in combination with Pasireotide.	Withdrawn
Trovafloxacin	Trovafloxacin may increase the hypoglycemic activities of Pasireotide.	Approved, Withdrawn
Vandetanib	Pasireotide may increase the QTc-prolonging activities of Vandetanib.	Approved
Vemurafenib	Pasireotide may increase the QTc-prolonging activities of Vemurafenib.	Approved
Venlafaxine	Venlafaxine may increase the hypoglycemic activities of Pasireotide.	Approved
Verapamil	Verapamil may increase the bradycardic activities of Pasireotide.	Approved
Vildagliptin	The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Pasireotide.	Approved, Investigational
Voglibose	The therapeutic efficacy of Voglibose can be decreased when used in combination with Pasireotide.	Approved, Investigational
Zimelidine	Zimelidine may increase the hypoglycemic activities of Pasireotide.	Withdrawn
Ziprasidone	Pasireotide may increase the QTc-prolonging activities of Ziprasidone.	Approved
Zuclopenthixol	Pasireotide may increase the QTc-prolonging activities of Zuclopenthixol.	Approved, Investigational

Food Interactions

Since Signifor® is administered subcutaneously, food has no effect.

References

Synthesis Reference

Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16.

General References

Weckbecker G, Briner U, Lewis I, Bruns C: SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. Endocrinology. 2002 Oct;143(10):4123-30. [PubMed:12239124 ]

External Links

Resource	Link
KEGG Drug	D10147
PubChem Compound	9941444
PubChem Substance	175427082
ChemSpider	8117062
ChEBI	72312
ChEMBL	CHEMBL3349607
Drug Product Database	22149
RxList	http://www.rxlist.com/signifor-drug.htm
Drugs.com	http://www.drugs.com/signifor.html
Wikipedia	Pasireotide

ATC Codes

H01CB05 — Pasireotide

AHFS Codes

Not Available

PDB Entries

Not Available

FDA label

Download (567 KB)

MSDS

Download (567 KB)

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Active Not Recruiting	Treatment	Neuroendocrine Tumors	2
1	Completed	Not Available	Alcoholism / Hepatic Cirrhosis	1
1	Completed	Treatment	Acromegaly / Carcinoid Tumors	1
1	Completed	Treatment	Carcinoid Tumors / Neuroendocrine Tumors / Progressive Neuroendocrine Tumors of pancreatic origin	1
1	Completed	Treatment	Impaired Renal Function	1
1	Completed	Treatment	Malignant Neoplasm of Pancreas	1
1	Completed	Treatment	Neuroendocrine Tumors	1
1, 2	Active Not Recruiting	Treatment	Adenocarcinoma of the Prostate / Hormone-Resistant Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer	1
1, 2	Active Not Recruiting	Treatment	Castration Resistant Prostate Cancer (CRPC)	1
2	Active Not Recruiting	Treatment	Autosomal Dominant Polycystic Kidney Disease (ADPKD) / Autosomal Dominant Polycystic Liver Disease / Polycystic Liver Disease (PLD) / Somatostatin Analogs	1
2	Active Not Recruiting	Treatment	Carcinoid Tumors / Neuroendocrine Tumors	1
2	Active Not Recruiting	Treatment	Thyroid Cancers	1
2	Completed	Prevention	Cancer, Breast	1
2	Completed	Treatment	Acromegaly	1
2	Completed	Treatment	Advanced Adult Hepatocellular Carcinoma	1
2	Completed	Treatment	Angiodysplasia	1
2	Completed	Treatment	Carcinoid Tumors	1
2	Completed	Treatment	Cushing's Disease	1
2	Completed	Treatment	Dumping Syndrome Patients	1
2	Completed	Treatment	Hepatocellular,Carcinoma	1
2	Completed	Treatment	Hyperglycemias	1
2	Completed	Treatment	Local Recurrent Thymoma / Primary Inoperable Thymoma	1
2	Completed	Treatment	Postoperative Dumping Syndrome	1
2	Not Yet Recruiting	Treatment	Congenital Hyperinsulinism / Hyperinsulinism / Insulinoma	1
2	Not Yet Recruiting	Treatment	Enterostomy	1
2	Recruiting	Treatment	ACTH-producing pituitary tumour / Pituitary Neoplasms	1
2	Recruiting	Treatment	Cluster Headache - Episodic and Chronic	1
2	Recruiting	Treatment	Ectopic Corticotropin Syndrome	1
2	Recruiting	Treatment	Haematological Malignancies	1
2	Terminated	Treatment	Cancers	1
2	Terminated	Treatment	Castrate Resistant Prostate Cancer (CRPC) / Chemotherapy Naive Prostate Cancer / Prostate Cancer	1
2	Terminated	Treatment	Ectopic Corticotropin Syndrome / Nelson Syndrome / Neoplasms, Pancreatic / Pituitary Neoplasms	1
2	Terminated	Treatment	Gonadotroph Adenomas	1
2	Terminated	Treatment	Nelson Syndrome	1
2	Unknown Status	Treatment	Lung Cancer Small Cell Lung Cancer (SCLC)	1
2	Withdrawn	Treatment	Multiple Myeloma (MM)	1
2	Withdrawn	Treatment	Multiple Myeloma (MM) / Multiple Myeloma in Relapse	1
2, 3	Completed	Treatment	Non-functioning Pituitary Adenomas / Prolactinomas	1
3	Active Not Recruiting	Treatment	Acromegaly	2
3	Completed	Treatment	Acromegaly	1
3	Completed	Treatment	Cushing's Disease	1
3	Completed	Treatment	Malignant Neoplasm of Pancreas	1
3	Completed	Treatment	Symptomatic Refractory Resistant Carcinoid Disease	1
4	Active Not Recruiting	Treatment	Acromegaly	1
4	Completed	Treatment	Cushing's Disease	1
4	Enrolling by Invitation	Treatment	BMI >30 kg/m2 / General Surgery / Hypoglycemia	1
4	Recruiting	Prevention	Neoplasms, Pancreatic / Pancreatic Fistula	1
4	Recruiting	Treatment	Acromegaly / Cushing's Disease / Dumping Syndrome / Ectopic ACTH Secreting (EAS) Tumors / Melanoma Negative for bRAF / Melanoma Negative for nRAS / Neuroendocrine Tumors / Pituitary Neoplasms / Prostate Cancer	1
4	Withdrawn	Treatment	Gastro-enteropancreatic Neuroendocrine Tumor	1
Not Available	Available	Not Available	Congenital Hyperinsulinism	1
Not Available	Recruiting	Not Available	Cushings Disease	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

Form	Route	Strength
Injection	Subcutaneous	.3 mg/mL
Injection	Subcutaneous	.6 mg/mL
Injection	Subcutaneous	.9 mg/mL
Injection, powder, for suspension	Intramuscular	20 mg
Injection, powder, for suspension	Intramuscular	40 mg
Injection, powder, for suspension	Intramuscular	60 mg
Injection, solution	Subcutaneous	0.3 mg
Injection, solution	Subcutaneous	0.6 mg
Injection, solution	Subcutaneous	0.9 mg
Solution	Subcutaneous	0.3 mg
Solution	Subcutaneous	0.6 mg
Solution	Subcutaneous	0.9 mg
Kit
Kit; powder, for suspension	Intramuscular	20 mg
Kit; powder, for suspension	Intramuscular	40 mg
Kit; powder, for suspension	Intramuscular	60 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US6225284	No	1996-06-28	2016-06-28	US
US7473761	No	2005-07-29	2025-07-29	US
US8299209	No	2005-12-27	2025-12-27	US
US8822637	No	2003-08-06	2023-08-06	US
US7759308	No	2006-10-25	2026-10-25	US

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	Soluble in water.	From The Merck Index.

Predicted Properties

Property	Value	Source
Water Solubility	0.00203 mg/mL	ALOGPS
logP	3.03	ALOGPS
logP	2.68	ChemAxon
logS	-5.7	ALOGPS
pKa (Strongest Acidic)	9.09	ChemAxon
pKa (Strongest Basic)	10.43	ChemAxon
Physiological Charge	2	ChemAxon
Hydrogen Acceptor Count	10	ChemAxon
Hydrogen Donor Count	9	ChemAxon
Polar Surface Area	281.2 Å²	ChemAxon
Rotatable Bond Count	18	ChemAxon
Refractivity	286.66 m³·mol^-1	ChemAxon
Polarizability	111.29 Å³	ChemAxon
Number of Rings	8	ChemAxon
Bioavailability	0	ChemAxon
Rule of Five	No	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	Yes	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9926
Blood Brain Barrier	-	0.5389
Caco-2 permeable	-	0.8325
P-glycoprotein substrate	Substrate	0.656
P-glycoprotein inhibitor I	Non-inhibitor	0.6717
P-glycoprotein inhibitor II	Non-inhibitor	0.6843
Renal organic cation transporter	Non-inhibitor	0.777
CYP450 2C9 substrate	Non-substrate	0.8878
CYP450 2D6 substrate	Non-substrate	0.758
CYP450 3A4 substrate	Substrate	0.521
CYP450 1A2 substrate	Non-inhibitor	0.7641
CYP450 2C9 inhibitor	Non-inhibitor	0.7676
CYP450 2D6 inhibitor	Non-inhibitor	0.8704
CYP450 2C19 inhibitor	Inhibitor	0.5307
CYP450 3A4 inhibitor	Inhibitor	0.575
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.6561
Ames test	Non AMES toxic	0.7722
Carcinogenicity	Non-carcinogens	0.8568
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.4609 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.8711
hERG inhibition (predictor II)	Inhibitor	0.7476

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum Type	Description	Splash Key
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Negative	Not Available

Taxonomy

Description

This compound belongs to the class of chemical entities known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.

Kingdom

Chemical entities

Super Class

Organic compounds

Class

Organic acids and derivatives

Sub Class

Carboxylic acids and derivatives

Direct Parent

Oligopeptides

Alternative Parents

Cyclic peptides / Macrolactams / 3-alkylindoles / Alpha amino acids and derivatives / Phenol ethers / Phenoxy compounds / Alkyl aryl ethers / Substituted pyrroles / Pyrrolidines / Heteroaromatic compounds

Substituents

Alpha-oligopeptide / Cyclic alpha peptide / Macrolactam / Alpha-amino acid or derivatives / 3-alkylindole / Indole or derivatives / Indole / Phenoxy compound / Phenol ether / Alkyl aryl ether

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

homodetic cyclic peptide, peptide hormone (CHEBI:72312 )

Targets

Details

1. Somatostatin receptor type 1

Kind: Protein
Organism: Human
Pharmacological action: unknown

General Function:: Somatostatin receptor activity
Specific Function:: Receptor for somatostatin with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
Gene Name:: SSTR1
Uniprot ID:: P30872
Uniprot Name:: Somatostatin receptor type 1
Molecular Weight:: 42685.77 Da

References

Zatelli MC, Piccin D, Vignali C, Tagliati F, Ambrosio MR, Bondanelli M, Cimino V, Bianchi A, Schmid HA, Scanarini M, Pontecorvi A, De Marinis L, Maira G, degli Uberti EC: Pasireotide, a multiple somatostatin receptor subtypes ligand, reduces cell viability in non-functioning pituitary adenomas by inhibiting vascular endothelial growth factor secretion. Endocr Relat Cancer. 2007 Mar;14(1):91-102. [PubMed:17395978 ]
Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16. [PubMed:11980628 ]

Details

2. Somatostatin receptor type 2

Kind: Protein
Organism: Human
Pharmacological action: unknown

General Function:: Somatostatin receptor activity
Specific Function:: Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and PLC via pertussis toxin insensitive as well as sensitive G proteins. Inhibits calcium entry by suppressing voltage-dependent calcium channels. Acts as the functionally dominant somatostatin receptor i...
Gene Name:: SSTR2
Uniprot ID:: P30874
Uniprot Name:: Somatostatin receptor type 2
Molecular Weight:: 41332.37 Da

References

Zatelli MC, Piccin D, Vignali C, Tagliati F, Ambrosio MR, Bondanelli M, Cimino V, Bianchi A, Schmid HA, Scanarini M, Pontecorvi A, De Marinis L, Maira G, degli Uberti EC: Pasireotide, a multiple somatostatin receptor subtypes ligand, reduces cell viability in non-functioning pituitary adenomas by inhibiting vascular endothelial growth factor secretion. Endocr Relat Cancer. 2007 Mar;14(1):91-102. [PubMed:17395978 ]
Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16. [PubMed:11980628 ]

Details

3. Somatostatin receptor type 3

Kind: Protein
Organism: Human
Pharmacological action: unknown

General Function:: Somatostatin receptor activity
Specific Function:: Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase.
Gene Name:: SSTR3
Uniprot ID:: P32745
Uniprot Name:: Somatostatin receptor type 3
Molecular Weight:: 45846.995 Da

References

Zatelli MC, Piccin D, Vignali C, Tagliati F, Ambrosio MR, Bondanelli M, Cimino V, Bianchi A, Schmid HA, Scanarini M, Pontecorvi A, De Marinis L, Maira G, degli Uberti EC: Pasireotide, a multiple somatostatin receptor subtypes ligand, reduces cell viability in non-functioning pituitary adenomas by inhibiting vascular endothelial growth factor secretion. Endocr Relat Cancer. 2007 Mar;14(1):91-102. [PubMed:17395978 ]
Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16. [PubMed:11980628 ]

Details

4. Somatostatin receptor type 5

Kind: Protein
Organism: Human
Pharmacological action: unknown

General Function:: Somatostatin receptor activity
Specific Function:: Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Increases cell growth inhibition activity of SSTR2 following heterodimerization.
Gene Name:: SSTR5
Uniprot ID:: P35346
Uniprot Name:: Somatostatin receptor type 5
Molecular Weight:: 39201.925 Da

References

Zatelli MC, Piccin D, Vignali C, Tagliati F, Ambrosio MR, Bondanelli M, Cimino V, Bianchi A, Schmid HA, Scanarini M, Pontecorvi A, De Marinis L, Maira G, degli Uberti EC: Pasireotide, a multiple somatostatin receptor subtypes ligand, reduces cell viability in non-functioning pituitary adenomas by inhibiting vascular endothelial growth factor secretion. Endocr Relat Cancer. 2007 Mar;14(1):91-102. [PubMed:17395978 ]
Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16. [PubMed:11980628 ]

Drug created on March 19, 2008 10:46 / Updated on September 01, 2017 11:29

Structure for DB06663 (Pasireotide)

Targets

References

References

References

References