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Identification
NamePasireotide
Accession NumberDB06663
TypeSmall Molecule
GroupsApproved
DescriptionPasireotide 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
Thumb
Synonyms
cyclo((4R)-4-(2-Aminoethylcarbamoyloxy)-L-prolyl-L-phenylglycyl-D-tryptophyl-L-lysyl-4-O-benzyl-L-tyrosyl-L- phenylalanyl-)
Pasireotida
Pasireotidum
SOM 230
SOM-230
SOM230
External Identifiers
  • SOM230
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SigniforInjection, solution0.9 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforSolution0.6 mgSubcutaneousNovartis Pharmaceuticals Canada Inc2013-11-26Not applicableCanada
SigniforInjection, solution0.3 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection.3 mg/mLSubcutaneousNovartis Pharmaceuticals Corporation2012-12-14Not applicableUs
SigniforInjection, powder, for suspension40 mgIntramuscularNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.6 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.9 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforSolution0.9 mgSubcutaneousNovartis Pharmaceuticals Canada Inc2013-11-28Not applicableCanada
SigniforInjection, solution0.6 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection.6 mg/mLSubcutaneousNovartis Pharmaceuticals Corporation2012-12-14Not applicableUs
SigniforInjection, powder, for suspension60 mgIntramuscularNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.3 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.9 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, powder, for suspension20 mgIntramuscularNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.6 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection.9 mg/mLSubcutaneousNovartis Pharmaceuticals Corporation2012-12-14Not applicableUs
SigniforInjection, powder, for suspension60 mgIntramuscularNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.3 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.9 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforSolution0.3 mgSubcutaneousNovartis Pharmaceuticals Canada Inc2013-11-26Not applicableCanada
SigniforInjection, powder, for suspension40 mgIntramuscularNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.6 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
SigniforInjection, solution0.3 mgSubcutaneousNovartis Europharm Limited2012-04-24Not applicableEu
Signifor LarKit; Powder, for suspension20 mgIntramuscularNovartis Pharmaceuticals Canada Inc2016-01-28Not applicableCanada
Signifor LarKitNovartis Pharmaceuticals Corporation2014-12-15Not applicableUs
Signifor LarKitNovartis Pharmaceuticals Corporation2014-12-15Not applicableUs
Signifor LarKit; Powder, for suspension60 mgIntramuscularNovartis Pharmaceuticals Canada Inc2015-08-04Not applicableCanada
Signifor LarKit; Powder, for suspension40 mgIntramuscularNovartis Pharmaceuticals Canada Inc2015-08-04Not applicableCanada
Signifor LarKitNovartis Pharmaceuticals Corporation2014-12-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Pasireotide diaspartate
Thumb
  • InChI Key: NEEFMPSSNFRRNC-HQUONIRXSA-N
  • Monoisotopic Mass: 1312.576439194
  • Average Mass: 1313.4116
DBSALT000134
Pasireotide pamoate
ThumbNot applicableDBSALT001332
Categories
UNII98H1T17066
CAS number396091-73-9
WeightAverage: 1047.2062
Monoisotopic: 1046.50142376
Chemical FormulaC58H66N10O9
InChI KeyVMZMNAABQBOLAK-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[C@@H]1NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@@H](NC(=O)[C@@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
IndicationFor the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.
Structured Indications
PharmacodynamicsSignifor® is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.
Mechanism of actionPasireotide 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Somatostatin receptor type 1ProteinunknownNot AvailableHumanP30872 details
Somatostatin receptor type 2ProteinunknownNot AvailableHumanP30874 details
Somatostatin receptor type 3ProteinunknownNot AvailableHumanP32745 details
Somatostatin receptor type 5ProteinunknownNot AvailableHumanP35346 details
Related Articles
AbsorptionThe 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 bindingPlasma protein binding is 88%.
Metabolism

Metabolism is minimal.

Route of eliminationPasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).
Half lifeThe 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.

ToxicityThe most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Pasireotide.Experimental
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Pasireotide.Approved, Investigational
AcebutololAcebutolol may increase the bradycardic activities of Pasireotide.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Pasireotide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Pasireotide.Approved, Vet Approved
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Pasireotide.Experimental
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Pasireotide.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Pasireotide.Approved
AmiodaronePasireotide may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AnagrelidePasireotide may increase the QTc-prolonging activities of Anagrelide.Approved
Arsenic trioxidePasireotide may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherPasireotide may increase the QTc-prolonging activities of Artemether.Approved
AsenapinePasireotide may increase the QTc-prolonging activities of Asenapine.Approved
AtenololAtenolol may increase the bradycardic activities of Pasireotide.Approved
AzithromycinPasireotide may increase the QTc-prolonging activities of Azithromycin.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Pasireotide.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
BedaquilinePasireotide may increase the QTc-prolonging activities of Bedaquiline.Approved
BendroflumethiazideBendroflumethiazide may increase the bradycardic activities of Pasireotide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Pasireotide.Withdrawn
BeractantPasireotide may increase the bradycardic activities of Beractant.Approved
BetaxololBetaxolol may increase the bradycardic activities of Pasireotide.Approved
BisoprololBisoprolol may increase the bradycardic activities of Pasireotide.Approved
BretyliumBretylium may increase the bradycardic activities of Pasireotide.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Pasireotide.Approved, Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Pasireotide.Withdrawn
CalfactantCalfactant may increase the bradycardic activities of Pasireotide.Approved
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Pasireotide.Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Pasireotide.Withdrawn
CarteololCarteolol may increase the bradycardic activities of Pasireotide.Approved
CarvedilolCarvedilol may increase the bradycardic activities of Pasireotide.Approved, Investigational
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Pasireotide.Experimental
CeritinibPasireotide may increase the bradycardic activities of Ceritinib.Approved
ChloroquinePasireotide may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazinePasireotide may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Pasireotide.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Pasireotide.Experimental
CinoxacinCinoxacin may increase the hypoglycemic activities of Pasireotide.Approved, Withdrawn
CiprofloxacinPasireotide may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisapridePasireotide may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramPasireotide may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinPasireotide may increase the QTc-prolonging activities of Clarithromycin.Approved
ClonidineClonidine may increase the bradycardic activities of Pasireotide.Approved
ClozapinePasireotide may increase the QTc-prolonging activities of Clozapine.Approved
CodeineThe metabolism of Codeine can be decreased when combined with Pasireotide.Approved, Illicit
CrizotinibPasireotide may increase the QTc-prolonging activities of Crizotinib.Approved
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Pasireotide.Approved, Investigational, Vet Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Pasireotide.Investigational
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Pasireotide.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Pasireotide.Investigational
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Pasireotide.Approved
DexmedetomidineDexmedetomidine may increase the bradycardic activities of Pasireotide.Approved, Vet Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Pasireotide.Approved
DigoxinDigoxin may increase the bradycardic activities of Pasireotide.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Pasireotide.Illicit
DiltiazemDiltiazem may increase the bradycardic activities of Pasireotide.Approved
DisopyramidePasireotide may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilidePasireotide may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronPasireotide may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidonePasireotide may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DonepezilDonepezil may increase the bradycardic activities of Pasireotide.Approved
DronedaronePasireotide may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolPasireotide may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Pasireotide.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Pasireotide.Approved
EliglustatPasireotide may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Pasireotide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Pasireotide.Approved
ErythromycinPasireotide may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramPasireotide may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
EsmololEsmolol may increase the bradycardic activities of Pasireotide.Approved
EtoperidoneEtoperidone may increase the hypoglycemic activities of Pasireotide.Approved
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Pasireotide.Approved, Investigational
FingolimodPasireotide may increase the bradycardic activities of Fingolimod.Approved, Investigational
FlecainidePasireotide may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FleroxacinFleroxacin may increase the hypoglycemic activities of Pasireotide.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Pasireotide.Withdrawn
FluoxetinePasireotide may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Pasireotide.Approved, Illicit
FlupentixolPasireotide may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
FurazolidoneFurazolidone may increase the hypoglycemic activities of Pasireotide.Approved, Vet Approved
Gadobenic acidPasireotide may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineGalantamine may increase the bradycardic activities of Pasireotide.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Pasireotide.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
GemifloxacinPasireotide may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Pasireotide.Withdrawn
GliclazideGliclazide may increase the hypoglycemic activities of Pasireotide.Approved
GlimepirideGlimepiride may increase the hypoglycemic activities of Pasireotide.Approved
GlipizideGlipizide may increase the hypoglycemic activities of Pasireotide.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Pasireotide.Approved
GlyburideGlyburide may increase the hypoglycemic activities of Pasireotide.Approved
GoserelinPasireotide may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronPasireotide may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Pasireotide.Withdrawn
GuanfacineGuanfacine may increase the bradycardic activities of Pasireotide.Approved, Investigational
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Pasireotide.Investigational
HaloperidolPasireotide may increase the QTc-prolonging activities of Haloperidol.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Pasireotide.Approved
IbutilidePasireotide may increase the QTc-prolonging activities of Ibutilide.Approved
IloperidonePasireotide may increase the QTc-prolonging activities of Iloperidone.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Pasireotide.Investigational, Withdrawn
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Pasireotide.Approved
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Pasireotide.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Pasireotide.Approved
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Pasireotide.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Pasireotide.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pasireotide.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Pasireotide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Pasireotide.Withdrawn
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Pasireotide.Approved
IvabradinePasireotide may increase the bradycardic activities of Ivabradine.Approved
LabetalolLabetalol may increase the bradycardic activities of Pasireotide.Approved
LacosamidePasireotide may increase the atrioventricular blocking (AV block) activities of Lacosamide.Approved
LanreotidePasireotide may increase the hypoglycemic activities of Lanreotide.Approved
LenvatinibPasireotide may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolidePasireotide may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevobunololLevobunolol may increase the bradycardic activities of Pasireotide.Approved
LevofloxacinPasireotide may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Pasireotide.Approved
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pasireotide.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Pasireotide.Approved
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Pasireotide.Approved
LopinavirPasireotide may increase the QTc-prolonging activities of Lopinavir.Approved
LucinactantLucinactant may increase the bradycardic activities of Pasireotide.Approved
LumefantrinePasireotide may increase the QTc-prolonging activities of Lumefantrine.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Pasireotide.Withdrawn
MecaserminMecasermin may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
MesalazineMesalazine may increase the hypoglycemic activities of Pasireotide.Approved
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Pasireotide.Approved
MethadonePasireotide may increase the QTc-prolonging activities of Methadone.Approved
MethyldopaMethyldopa may increase the bradycardic activities of Pasireotide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Pasireotide.Investigational
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Pasireotide.Approved
MetipranololMetipranolol may increase the bradycardic activities of Pasireotide.Approved
MetoprololMetoprolol may increase the bradycardic activities of Pasireotide.Approved, Investigational
MifepristoneMifepristone may increase the QTc-prolonging activities of Pasireotide.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Pasireotide.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Pasireotide.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Pasireotide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Pasireotide.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Pasireotide.Approved, Investigational
MoclobemideMoclobemide may increase the hypoglycemic activities of Pasireotide.Approved
MoxifloxacinPasireotide may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
NadololNadolol may increase the bradycardic activities of Pasireotide.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Pasireotide.Approved
NateglinideNateglinide may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Pasireotide.Investigational
NebivololNebivolol may increase the bradycardic activities of Pasireotide.Approved, Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Pasireotide.Approved, Withdrawn
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Pasireotide.Investigational
NialamideNialamide may increase the hypoglycemic activities of Pasireotide.Withdrawn
NilotinibPasireotide may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Pasireotide.Investigational
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Pasireotide.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Pasireotide.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
OfloxacinPasireotide may increase the QTc-prolonging activities of Ofloxacin.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Pasireotide.Approved
OndansetronPasireotide may increase the QTc-prolonging activities of Ondansetron.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Pasireotide.Approved, Illicit
PaliperidonePasireotide may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatPasireotide may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PargylinePargyline may increase the hypoglycemic activities of Pasireotide.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
PazopanibPasireotide may increase the QTc-prolonging activities of Pazopanib.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Pasireotide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Pasireotide.Approved
PegvisomantThe risk or severity of adverse effects can be increased when Pasireotide is combined with Pegvisomant.Approved
PenbutololPenbutolol may increase the bradycardic activities of Pasireotide.Approved, Investigational
PentamidinePasireotide may increase the QTc-prolonging activities of Pentamidine.Approved
PerflutrenPasireotide may increase the QTc-prolonging activities of Perflutren.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Pasireotide.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Pasireotide.Approved, Withdrawn
PheniprazinePheniprazine may increase the hypoglycemic activities of Pasireotide.Withdrawn
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Pasireotide.Withdrawn
PimozidePasireotide may increase the QTc-prolonging activities of Pimozide.Approved
PindololPindolol may increase the bradycardic activities of Pasireotide.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Pasireotide.Approved, Investigational
PirlindolePirlindole may increase the hypoglycemic activities of Pasireotide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Pasireotide.Withdrawn
Poractant alfaPasireotide may increase the bradycardic activities of Poractant alfa.Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Pasireotide.Approved, Investigational
PrimaquinePasireotide may increase the QTc-prolonging activities of Primaquine.Approved
ProcainamidePasireotide may increase the QTc-prolonging activities of Procainamide.Approved
PromazinePasireotide may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenonePasireotide may increase the QTc-prolonging activities of Propafenone.Approved
PropranololPropranolol may increase the bradycardic activities of Pasireotide.Approved, Investigational
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Pasireotide.Investigational
QuetiapinePasireotide may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidinePasireotide may increase the QTc-prolonging activities of Quinidine.Approved
QuininePasireotide may increase the QTc-prolonging activities of Quinine.Approved
RasagilineRasagiline may increase the hypoglycemic activities of Pasireotide.Approved
RepaglinideRepaglinide may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
RivastigmineRivastigmine may increase the bradycardic activities of Pasireotide.Approved, Investigational
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pasireotide.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Pasireotide.Approved
RuxolitinibRuxolitinib may increase the bradycardic activities of Pasireotide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Pasireotide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Pasireotide.Approved, Vet Approved
SaquinavirPasireotide may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pasireotide.Approved
SelegilineSelegiline may increase the hypoglycemic activities of Pasireotide.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Pasireotide.Approved
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide.Approved, Investigational
SotalolPasireotide may increase the QTc-prolonging activities of Sotalol.Approved
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Pasireotide.Approved
StanozololStanozolol may increase the hypoglycemic activities of Pasireotide.Approved, Vet Approved
SufentanilSufentanil may increase the bradycardic activities of Pasireotide.Approved, Investigational
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Pasireotide.Approved, Vet Approved
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Pasireotide.Approved
SulfisoxazolePasireotide may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Pasireotide.Approved, Investigational
SunitinibSunitinib may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
TelavancinPasireotide may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinPasireotide may increase the QTc-prolonging activities of Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Pasireotide.Withdrawn
TestosteroneTestosterone may increase the hypoglycemic activities of Pasireotide.Approved, Investigational
TetrabenazinePasireotide may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Pasireotide.Investigational
ThioridazinePasireotide may increase the QTc-prolonging activities of Thioridazine.Approved
TimololTimolol may increase the bradycardic activities of Pasireotide.Approved
TizanidineTizanidine may increase the bradycardic activities of Pasireotide.Approved
TofacitinibTofacitinib may increase the bradycardic activities of Pasireotide.Approved, Investigational
TolazamideTolazamide may increase the hypoglycemic activities of Pasireotide.Approved
TolbutamideTolbutamide may increase the hypoglycemic activities of Pasireotide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Pasireotide.Approved
ToremifenePasireotide may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Pasireotide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Pasireotide.Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Pasireotide.Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Pasireotide.Approved, Withdrawn
VandetanibPasireotide may increase the QTc-prolonging activities of Vandetanib.Approved
VemurafenibPasireotide may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Pasireotide.Approved
VerapamilVerapamil may increase the bradycardic activities of Pasireotide.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Pasireotide.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Pasireotide.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Pasireotide.Withdrawn
ZiprasidonePasireotide may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolPasireotide 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
  1. 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
ATC CodesH01CB05
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (567 KB)
MSDSDownload (567 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9926
Blood Brain Barrier-0.5389
Caco-2 permeable-0.8325
P-glycoprotein substrateSubstrate0.656
P-glycoprotein inhibitor INon-inhibitor0.6717
P-glycoprotein inhibitor IINon-inhibitor0.6843
Renal organic cation transporterNon-inhibitor0.777
CYP450 2C9 substrateNon-substrate0.8878
CYP450 2D6 substrateNon-substrate0.758
CYP450 3A4 substrateSubstrate0.521
CYP450 1A2 substrateNon-inhibitor0.7641
CYP450 2C9 inhibitorNon-inhibitor0.7676
CYP450 2D6 inhibitorNon-inhibitor0.8704
CYP450 2C19 inhibitorInhibitor0.5307
CYP450 3A4 inhibitorInhibitor0.575
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6561
Ames testNon AMES toxic0.7722
CarcinogenicityNon-carcinogens0.8568
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.4609 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8711
hERG inhibition (predictor II)Inhibitor0.7476
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
InjectionSubcutaneous.3 mg/mL
InjectionSubcutaneous.6 mg/mL
InjectionSubcutaneous.9 mg/mL
Injection, powder, for suspensionIntramuscular20 mg
Injection, powder, for suspensionIntramuscular40 mg
Injection, powder, for suspensionIntramuscular60 mg
Injection, solutionSubcutaneous0.3 mg
Injection, solutionSubcutaneous0.6 mg
Injection, solutionSubcutaneous0.9 mg
SolutionSubcutaneous0.3 mg
SolutionSubcutaneous0.6 mg
SolutionSubcutaneous0.9 mg
Kit
Kit; powder, for suspensionIntramuscular20 mg
Kit; powder, for suspensionIntramuscular40 mg
Kit; powder, for suspensionIntramuscular60 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6225284 No1996-06-282016-06-28Us
US7473761 No2005-07-292025-07-29Us
US7759308 No2006-10-252026-10-25Us
US8299209 No2005-12-272025-12-27Us
US8822637 No2003-08-062023-08-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySoluble in water.From The Merck Index.
Predicted Properties
PropertyValueSource
Water Solubility0.00203 mg/mLALOGPS
logP3.03ALOGPS
logP2.68ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)9.09ChemAxon
pKa (Strongest Basic)10.43ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count9ChemAxon
Polar Surface Area281.2 Å2ChemAxon
Rotatable Bond Count18ChemAxon
Refractivity286.66 m3·mol-1ChemAxon
Polarizability111.29 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as cyclic peptides. These are compounds containing a cyclic moiety bearing a peptide backbone.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentCyclic peptides
Alternative Parents
Substituents
  • Cyclic alpha peptide
  • Macrolactam
  • Indole or derivatives
  • Indole
  • Phenol ether
  • Alkyl aryl ether
  • Benzenoid
  • Substituted pyrrole
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Pyrrolidine
  • Pyrrole
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

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
Molecular Weight:
42685.77 Da
References
  1. 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 ]
  2. 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 ]
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
Molecular Weight:
41332.37 Da
References
  1. 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 ]
  2. 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 ]
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
Molecular Weight:
45846.995 Da
References
  1. 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 ]
  2. 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 ]
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
Molecular Weight:
39201.925 Da
References
  1. 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 ]
  2. 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 ]
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Drug created on March 19, 2008 10:46 / Updated on December 02, 2016 02:44