You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
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
Signiforsolution0.6 mgsubcutaneousNovartis Pharmaceuticals Canada Inc2013-11-26Not applicableCanada
Signiforinjection.3 mg/mLsubcutaneousNovartis Pharmaceuticals Corporation2012-12-14Not applicableUs
Signiforsolution0.9 mgsubcutaneousNovartis Pharmaceuticals Canada Inc2013-11-28Not applicableCanada
Signiforinjection.6 mg/mLsubcutaneousNovartis Pharmaceuticals Corporation2012-12-14Not applicableUs
Signiforinjection.9 mg/mLsubcutaneousNovartis Pharmaceuticals Corporation2012-12-14Not applicableUs
Signiforsolution0.3 mgsubcutaneousNovartis Pharmaceuticals Canada Inc2013-11-26Not applicableCanada
Signifor Larpowder for suspension; kit20 mgintramuscularNovartis Pharmaceuticals Canada Inc2016-01-28Not applicableCanada
Signifor LarkitNovartis Pharmaceuticals Corporation2014-12-15Not applicableUs
Signifor LarkitNovartis Pharmaceuticals Corporation2014-12-15Not applicableUs
Signifor Larpowder for suspension; kit60 mgintramuscularNovartis Pharmaceuticals Canada Inc2015-08-04Not applicableCanada
Signifor Larpowder for suspension; kit40 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 KeyInChIKey=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[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
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
Pharmacology
IndicationFor the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.
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.
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
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
Solutionsubcutaneous0.3 mg
Solutionsubcutaneous0.6 mg
Solutionsubcutaneous0.9 mg
Kit
Powder for suspension; kitintramuscular20 mg
Powder for suspension; kitintramuscular40 mg
Powder for suspension; kitintramuscular60 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
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)
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Pasireotide.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Pasireotide.
AcarboseAcarbose may increase the hypoglycemic activities of Pasireotide.
AcebutololAcebutolol may increase the bradycardic activities of Pasireotide.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Pasireotide.
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Pasireotide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Pasireotide.
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Pasireotide.
AicarAicar may increase the hypoglycemic activities of Pasireotide.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Pasireotide.
AlogliptinAlogliptin may increase the hypoglycemic activities of Pasireotide.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Pasireotide.
AmiodaroneAmiodarone may increase the bradycardic activities of Pasireotide.
AmoxapineAmoxapine may increase the hypoglycemic activities of Pasireotide.
AnagrelidePasireotide may increase the QTc-prolonging activities of Anagrelide.
Arsenic trioxidePasireotide may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherPasireotide may increase the QTc-prolonging activities of Artemether.
AsenapinePasireotide may increase the QTc-prolonging activities of Asenapine.
AtenololAtenolol may increase the bradycardic activities of Pasireotide.
AzithromycinPasireotide may increase the QTc-prolonging activities of Azithromycin.
BedaquilinePasireotide may increase the QTc-prolonging activities of Bedaquiline.
BendroflumethiazideBendroflumethiazide may increase the bradycardic activities of Pasireotide.
BenmoxinBenmoxin may increase the hypoglycemic activities of Pasireotide.
BeractantPasireotide may increase the bradycardic activities of Beractant.
BetaxololBetaxolol may increase the bradycardic activities of Pasireotide.
BisoprololBisoprolol may increase the bradycardic activities of Pasireotide.
BretyliumBretylium may increase the bradycardic activities of Pasireotide.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Pasireotide.
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Pasireotide.
BuforminBuformin may increase the hypoglycemic activities of Pasireotide.
CalfactantCalfactant may increase the bradycardic activities of Pasireotide.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Pasireotide.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Pasireotide.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Pasireotide.
CarteololCarteolol may increase the bradycardic activities of Pasireotide.
CarvedilolCarvedilol may increase the bradycardic activities of Pasireotide.
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Pasireotide.
CastanospermineCastanospermine may increase the hypoglycemic activities of Pasireotide.
CeritinibPasireotide may increase the bradycardic activities of Ceritinib.
ChloroquinePasireotide may increase the QTc-prolonging activities of Chloroquine.
ChlorpromazinePasireotide may increase the QTc-prolonging activities of Chlorpromazine.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Pasireotide.
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Pasireotide.
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Pasireotide.
CiglitazoneCiglitazone may increase the hypoglycemic activities of Pasireotide.
CiprofloxacinPasireotide may increase the QTc-prolonging activities of Ciprofloxacin.
CisapridePasireotide may increase the QTc-prolonging activities of Cisapride.
CitalopramCitalopram may increase the hypoglycemic activities of Pasireotide.
CitalopramPasireotide may increase the QTc-prolonging activities of Citalopram.
ClarithromycinPasireotide may increase the QTc-prolonging activities of Clarithromycin.
ClomipramineClomipramine may increase the hypoglycemic activities of Pasireotide.
ClonidineClonidine may increase the bradycardic activities of Pasireotide.
ClozapinePasireotide may increase the QTc-prolonging activities of Clozapine.
CodeineThe metabolism of Codeine can be decreased when combined with Pasireotide.
CrizotinibPasireotide may increase the QTc-prolonging activities of Crizotinib.
CrizotinibCrizotinib may increase the bradycardic activities of Pasireotide.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Pasireotide.
DapoxetineDapoxetine may increase the hypoglycemic activities of Pasireotide.
DexmedetomidineDexmedetomidine may increase the bradycardic activities of Pasireotide.
DiflunisalDiflunisal may increase the hypoglycemic activities of Pasireotide.
DigoxinDigoxin may increase the bradycardic activities of Pasireotide.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Pasireotide.
DiltiazemDiltiazem may increase the bradycardic activities of Pasireotide.
DisopyramideDisopyramide may increase the hypoglycemic activities of Pasireotide.
DofetilidePasireotide may increase the QTc-prolonging activities of Dofetilide.
DolasetronPasireotide may increase the QTc-prolonging activities of Dolasetron.
DomperidonePasireotide may increase the QTc-prolonging activities of Domperidone.
DonepezilDonepezil may increase the bradycardic activities of Pasireotide.
DronedaroneDronedarone may increase the bradycardic activities of Pasireotide.
DroperidolPasireotide may increase the QTc-prolonging activities of Droperidol.
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Pasireotide.
DulaglutideDulaglutide may increase the hypoglycemic activities of Pasireotide.
EliglustatPasireotide may increase the QTc-prolonging activities of Eliglustat.
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Pasireotide.
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Pasireotide.
ErythromycinPasireotide may increase the QTc-prolonging activities of Erythromycin.
EscitalopramEscitalopram may increase the hypoglycemic activities of Pasireotide.
EscitalopramPasireotide may increase the QTc-prolonging activities of Escitalopram.
EsmololEsmolol may increase the bradycardic activities of Pasireotide.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Pasireotide.
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Pasireotide.
ExenatideExenatide may increase the hypoglycemic activities of Pasireotide.
FenfluramineFenfluramine may increase the hypoglycemic activities of Pasireotide.
FingolimodPasireotide may increase the bradycardic activities of Fingolimod.
FlecainidePasireotide may increase the QTc-prolonging activities of Flecainide.
FluoxetineFluoxetine may increase the hypoglycemic activities of Pasireotide.
FluoxetinePasireotide may increase the QTc-prolonging activities of Fluoxetine.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Pasireotide.
FlupentixolPasireotide may increase the QTc-prolonging activities of Flupentixol.
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Pasireotide.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Pasireotide.
Gadobenic acidPasireotide may increase the QTc-prolonging activities of Gadobenic acid.
GalantamineGalantamine may increase the bradycardic activities of Pasireotide.
GemifloxacinPasireotide may increase the QTc-prolonging activities of Gemifloxacin.
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Pasireotide.
GlibornurideGlibornuride may increase the hypoglycemic activities of Pasireotide.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Pasireotide.
GliclazideGliclazide may increase the hypoglycemic activities of Pasireotide.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Pasireotide.
GlimepirideGlimepiride may increase the hypoglycemic activities of Pasireotide.
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Pasireotide.
GlipizideGlipizide may increase the hypoglycemic activities of Pasireotide.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Pasireotide.
GliquidoneGliquidone may increase the hypoglycemic activities of Pasireotide.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Pasireotide.
GlyburideGlyburide may increase the hypoglycemic activities of Pasireotide.
GoserelinPasireotide may increase the QTc-prolonging activities of Goserelin.
GranisetronPasireotide may increase the QTc-prolonging activities of Granisetron.
GuanfacineGuanfacine may increase the bradycardic activities of Pasireotide.
HaloperidolPasireotide may increase the QTc-prolonging activities of Haloperidol.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Pasireotide.
IbutilidePasireotide may increase the QTc-prolonging activities of Ibutilide.
IloperidonePasireotide may increase the QTc-prolonging activities of Iloperidone.
IndalpineIndalpine may increase the hypoglycemic activities of Pasireotide.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Pasireotide.
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Pasireotide.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Pasireotide.
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Pasireotide.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Pasireotide.
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Pasireotide.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Pasireotide.
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Pasireotide.
Insulin HumanInsulin Human may increase the hypoglycemic activities of Pasireotide.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Pasireotide.
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Pasireotide.
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pasireotide.
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Pasireotide.
IproclozideIproclozide may increase the hypoglycemic activities of Pasireotide.
IproniazidIproniazid may increase the hypoglycemic activities of Pasireotide.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Pasireotide.
IvabradinePasireotide may increase the bradycardic activities of Ivabradine.
LabetalolLabetalol may increase the bradycardic activities of Pasireotide.
LacosamidePasireotide may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LanreotidePasireotide may increase the hypoglycemic activities of Lanreotide.
LenvatinibPasireotide may increase the QTc-prolonging activities of Lenvatinib.
LeuprolidePasireotide may increase the QTc-prolonging activities of Leuprolide.
LevobunololLevobunolol may increase the bradycardic activities of Pasireotide.
LevofloxacinPasireotide may increase the QTc-prolonging activities of Levofloxacin.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Pasireotide.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pasireotide.
LinagliptinLinagliptin may increase the hypoglycemic activities of Pasireotide.
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Pasireotide.
LiraglutideLiraglutide may increase the hypoglycemic activities of Pasireotide.
LopinavirPasireotide may increase the QTc-prolonging activities of Lopinavir.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Pasireotide.
LucinactantLucinactant may increase the bradycardic activities of Pasireotide.
LumefantrinePasireotide may increase the QTc-prolonging activities of Lumefantrine.
MebanazineMebanazine may increase the hypoglycemic activities of Pasireotide.
MecaserminMecasermin may increase the hypoglycemic activities of Pasireotide.
MesalazineMesalazine may increase the hypoglycemic activities of Pasireotide.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Pasireotide.
MetforminMetformin may increase the hypoglycemic activities of Pasireotide.
MethadonePasireotide may increase the QTc-prolonging activities of Methadone.
MethyldopaMethyldopa may increase the bradycardic activities of Pasireotide.
Methylene blueMethylene blue may increase the hypoglycemic activities of Pasireotide.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Pasireotide.
MetipranololMetipranolol may increase the bradycardic activities of Pasireotide.
MetoprololMetoprolol may increase the bradycardic activities of Pasireotide.
MifepristoneMifepristone may increase the hypoglycemic activities of Pasireotide.
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Pasireotide.
MiglitolMiglitol may increase the hypoglycemic activities of Pasireotide.
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Pasireotide.
MiglustatMiglustat may increase the hypoglycemic activities of Pasireotide.
MilnacipranMilnacipran may increase the hypoglycemic activities of Pasireotide.
MinaprineMinaprine may increase the hypoglycemic activities of Pasireotide.
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Pasireotide.
MitiglinideMitiglinide may increase the hypoglycemic activities of Pasireotide.
MoclobemideMoclobemide may increase the hypoglycemic activities of Pasireotide.
MoxifloxacinPasireotide may increase the QTc-prolonging activities of Moxifloxacin.
NadololNadolol may increase the bradycardic activities of Pasireotide.
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Pasireotide.
NateglinideNateglinide may increase the hypoglycemic activities of Pasireotide.
NebivololNebivolol may increase the bradycardic activities of Pasireotide.
NialamideNialamide may increase the hypoglycemic activities of Pasireotide.
NilotinibPasireotide may increase the QTc-prolonging activities of Nilotinib.
OctamoxinOctamoxin may increase the hypoglycemic activities of Pasireotide.
OctreotideOctreotide may increase the hypoglycemic activities of Pasireotide.
OfloxacinPasireotide may increase the QTc-prolonging activities of Ofloxacin.
OlanzapineOlanzapine may increase the hypoglycemic activities of Pasireotide.
OndansetronPasireotide may increase the QTc-prolonging activities of Ondansetron.
OxandroloneOxandrolone may increase the hypoglycemic activities of Pasireotide.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Pasireotide.
PaliperidonePasireotide may increase the QTc-prolonging activities of Paliperidone.
PanobinostatPasireotide may increase the QTc-prolonging activities of Panobinostat.
PargylinePargyline may increase the hypoglycemic activities of Pasireotide.
ParoxetineParoxetine may increase the hypoglycemic activities of Pasireotide.
PazopanibPasireotide may increase the QTc-prolonging activities of Pazopanib.
PegvisomantPegvisomant may increase the hypoglycemic activities of Pasireotide.
PegvisomantThe risk or severity of adverse effects can be increased when Pasireotide is combined with Pegvisomant.
PenbutololPenbutolol may increase the bradycardic activities of Pasireotide.
PentamidinePasireotide may increase the QTc-prolonging activities of Pentamidine.
PentamidinePentamidine may increase the hypoglycemic activities of Pasireotide.
PerflutrenPasireotide may increase the QTc-prolonging activities of Perflutren.
PhenelzinePhenelzine may increase the hypoglycemic activities of Pasireotide.
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Pasireotide.
PhenforminPhenformin may increase the hypoglycemic activities of Pasireotide.
PheniprazinePheniprazine may increase the hypoglycemic activities of Pasireotide.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Pasireotide.
PimozidePasireotide may increase the QTc-prolonging activities of Pimozide.
PindololPindolol may increase the bradycardic activities of Pasireotide.
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Pasireotide.
PioglitazonePioglitazone may increase the hypoglycemic activities of Pasireotide.
PirlindolePirlindole may increase the hypoglycemic activities of Pasireotide.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Pasireotide.
Poractant alfaPasireotide may increase the bradycardic activities of Poractant alfa.
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Pasireotide.
PramlintidePramlintide may increase the hypoglycemic activities of Pasireotide.
PrimaquinePasireotide may increase the QTc-prolonging activities of Primaquine.
ProcainamidePasireotide may increase the QTc-prolonging activities of Procainamide.
PromazinePasireotide may increase the QTc-prolonging activities of Promazine.
PropafenonePasireotide may increase the QTc-prolonging activities of Propafenone.
PropafenonePropafenone may increase the bradycardic activities of Pasireotide.
PropranololPropranolol may increase the bradycardic activities of Pasireotide.
QuetiapinePasireotide may increase the QTc-prolonging activities of Quetiapine.
QuinidinePasireotide may increase the QTc-prolonging activities of Quinidine.
QuinineQuinine may increase the hypoglycemic activities of Pasireotide.
RasagilineRasagiline may increase the hypoglycemic activities of Pasireotide.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Pasireotide.
RepaglinideRepaglinide may increase the hypoglycemic activities of Pasireotide.
RivastigmineRivastigmine may increase the bradycardic activities of Pasireotide.
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pasireotide.
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Pasireotide.
RuxolitinibRuxolitinib may increase the bradycardic activities of Pasireotide.
SafrazineSafrazine may increase the hypoglycemic activities of Pasireotide.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Pasireotide.
SaquinavirPasireotide may increase the QTc-prolonging activities of Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pasireotide.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Pasireotide.
SelegilineSelegiline may increase the hypoglycemic activities of Pasireotide.
SertralineSertraline may increase the hypoglycemic activities of Pasireotide.
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide.
SitagliptinSitagliptin may increase the hypoglycemic activities of Pasireotide.
SotalolSotalol may increase the bradycardic activities of Pasireotide.
StanozololStanozolol may increase the hypoglycemic activities of Pasireotide.
SufentanilSufentanil may increase the bradycardic activities of Pasireotide.
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Pasireotide.
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Pasireotide.
SulfisoxazolePasireotide may increase the QTc-prolonging activities of Sulfisoxazole.
SulfisoxazoleSulfisoxazole may increase the hypoglycemic activities of Pasireotide.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Pasireotide.
SulodexideSulodexide may increase the hypoglycemic activities of Pasireotide.
SunitinibSunitinib may increase the hypoglycemic activities of Pasireotide.
TelavancinPasireotide may increase the QTc-prolonging activities of Telavancin.
TelithromycinPasireotide may increase the QTc-prolonging activities of Telithromycin.
TestosteroneTestosterone may increase the hypoglycemic activities of Pasireotide.
TetrabenazinePasireotide may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazinePasireotide may increase the QTc-prolonging activities of Thioridazine.
TimololTimolol may increase the bradycardic activities of Pasireotide.
TizanidineTizanidine may increase the bradycardic activities of Pasireotide.
TofacitinibTofacitinib may increase the bradycardic activities of Pasireotide.
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Pasireotide.
TolazamideTolazamide may increase the hypoglycemic activities of Pasireotide.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Pasireotide.
TolbutamideTolbutamide may increase the hypoglycemic activities of Pasireotide.
ToloxatoneToloxatone may increase the hypoglycemic activities of Pasireotide.
ToremifenePasireotide may increase the QTc-prolonging activities of Toremifene.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Pasireotide.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Pasireotide.
TrazodoneTrazodone may increase the hypoglycemic activities of Pasireotide.
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Pasireotide.
TroglitazoneTroglitazone may increase the hypoglycemic activities of Pasireotide.
VandetanibPasireotide may increase the QTc-prolonging activities of Vandetanib.
VemurafenibPasireotide may increase the QTc-prolonging activities of Vemurafenib.
VerapamilVerapamil may increase the bradycardic activities of Pasireotide.
VilazodoneVilazodone may increase the hypoglycemic activities of Pasireotide.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Pasireotide.
VildagliptinVildagliptin may increase the hypoglycemic activities of Pasireotide.
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Pasireotide.
VogliboseVoglibose may increase the hypoglycemic activities of Pasireotide.
VortioxetineVortioxetine may increase the hypoglycemic activities of Pasireotide.
ZimelidineZimelidine may increase the hypoglycemic activities of Pasireotide.
ZiprasidonePasireotide may increase the QTc-prolonging activities of Ziprasidone.
ZuclopenthixolPasireotide may increase the QTc-prolonging activities of Zuclopenthixol.
Food Interactions
  • Since Signifor® is administered subcutaneously, food has no effect.

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 ]
Comments
comments powered by Disqus
Drug created on March 19, 2008 10:46 / Updated on September 29, 2016 02:28