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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyPasireotide
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
Structure for DB06663 (Pasireotide)
- 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 Pasireotide diaspartate I4P76SY3N4 820232-50-6 NEEFMPSSNFRRNC-HQUONIRXSA-N Pasireotide pamoate 04F55A7UZ3 396091-79-5 HSXBEUMRBMAVDP-QKXVGOHISA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Signifor Injection, powder, for suspension 60 mg Intramuscular Novartis Europharm Limited 2012-04-24 Not applicable EU 
Signifor Solution 0.3 mg Subcutaneous Novartis 2013-11-26 Not applicable Canada 
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 Injection, powder, for suspension 20 mg Intramuscular 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 .3 mg/mL Subcutaneous Novartis 2012-12-14 Not applicable US 
Signifor Solution 0.9 mg Subcutaneous Novartis 2013-11-28 Not applicable Canada Signifor Injection, solution 0.6 mg Subcutaneous 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 - Categories
- Amino Acids, Peptides, and Proteins
- Bradycardia-Causing Agents
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hyperglycemia-Associated Agents
- Hypoglycemia-Associated Agents
- Hypothalamic Hormones
- Nerve Tissue Proteins
- Neuropeptides
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Pituitary and Hypothalamic Hormones and Analogues
- Pituitary Hormone Release Inhibiting Hormones
- Proteins
- QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying)
- Somatostatin Agonists
- Somatostatin and Analogues
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- 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 Actions Organism USomatostatin receptor type 1 Not Available Human USomatostatin receptor type 2 Not Available Human USomatostatin receptor type 3 Not Available Human USomatostatin receptor type 5 Not Available Human - 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 2,4-thiazolidinedione can be decreased when used in combination with Pasireotide. Investigational 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, Investigational Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Pasireotide. Approved, Investigational, Withdrawn AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Pasireotide. Experimental, Investigational Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Pasireotide. Investigational Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with 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 Bedaquiline Pasireotide may increase the QTc-prolonging activities of Bedaquiline. Approved Bempedoic acid The therapeutic efficacy of Bempedoic acid can be decreased when used in combination with Pasireotide. Investigational Bendroflumethiazide Bendroflumethiazide may increase the bradycardic activities of Pasireotide. Approved Beractant Pasireotide may increase the bradycardic activities of Beractant. Approved Betaxolol Betaxolol may increase the bradycardic activities of Pasireotide. Approved, Investigational 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. Investigational, 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 Carbutamide The therapeutic efficacy of Carbutamide can be decreased when used in combination with Pasireotide. Experimental 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, Investigational, Vet Approved Chlorpromazine Pasireotide may increase the QTc-prolonging activities of Chlorpromazine. Approved, Investigational, Vet Approved Chlorpropamide Chlorpropamide may increase the hypoglycemic activities of Pasireotide. Approved, Investigational Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Pasireotide. Experimental 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 Deoxyspergualin The therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Pasireotide. Investigational Dexmedetomidine Dexmedetomidine may increase the bradycardic activities of Pasireotide. Approved, Vet Approved Digoxin Digoxin may increase the bradycardic activities of Pasireotide. Approved Diltiazem Diltiazem may increase the bradycardic activities of Pasireotide. Approved, Investigational Disopyramide Pasireotide may increase the QTc-prolonging activities of Disopyramide. Approved Dofetilide Pasireotide may increase the QTc-prolonging activities of Dofetilide. Approved, Investigational Dolasetron Pasireotide may increase the QTc-prolonging activities of Dolasetron. Approved, Investigational Domperidone Pasireotide may increase the QTc-prolonging activities of Domperidone. Approved, Investigational, Vet Approved Donepezil Donepezil may increase the bradycardic activities of Pasireotide. Approved Dotatate gallium Ga-68 The therapeutic efficacy of Dotatate gallium Ga-68 can be decreased when used in combination with Pasireotide. Approved, Investigational 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, Investigational 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 Erythromycin Pasireotide may increase the QTc-prolonging activities of Erythromycin. Approved, Investigational, Vet Approved Escitalopram Pasireotide may increase the QTc-prolonging activities of Escitalopram. Approved, Investigational Esmolol Esmolol may increase the bradycardic 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 Fluoxetine Pasireotide may increase the QTc-prolonging activities of Fluoxetine. Approved, Vet Approved Flupentixol Pasireotide may increase the QTc-prolonging activities of Flupentixol. Approved, Investigational, Withdrawn Gadobenic acid Pasireotide may increase the QTc-prolonging activities of Gadobenic acid. Approved, Investigational Galantamine Galantamine may increase the bradycardic activities of Pasireotide. Approved 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. Investigational, 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, Investigational Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Pasireotide. Approved, Investigational 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 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 Ibutilide Pasireotide may increase the QTc-prolonging activities of Ibutilide. Approved Iloperidone Pasireotide may increase the QTc-prolonging activities of Iloperidone. Approved 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 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, Investigational 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 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 Lopinavir Pasireotide may increase the QTc-prolonging activities of Lopinavir. Approved Lucinactant Lucinactant may increase the bradycardic activities of Pasireotide. Approved, Investigational Lumefantrine Pasireotide may increase the QTc-prolonging activities of Lumefantrine. Approved Lutetium Lu 177 dotatate The therapeutic efficacy of Lutetium Lu 177 dotatate can be decreased when used in combination with Pasireotide. Approved, Investigational Mecasermin Mecasermin may increase the hypoglycemic activities of Pasireotide. Approved, Investigational 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 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 Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Pasireotide. Approved, Investigational Moxifloxacin Pasireotide may increase the QTc-prolonging activities of Moxifloxacin. Approved, Investigational Nadolol Nadolol may increase the bradycardic 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 Nilotinib Pasireotide may increase the QTc-prolonging activities of Nilotinib. Approved, Investigational Octreotide Octreotide may increase the hypoglycemic activities of Pasireotide. Approved, Investigational Ofloxacin Pasireotide may increase the QTc-prolonging activities of Ofloxacin. Approved Ondansetron Pasireotide may increase the QTc-prolonging activities of Ondansetron. Approved Paliperidone Pasireotide may increase the QTc-prolonging activities of Paliperidone. Approved Panobinostat Pasireotide may increase the QTc-prolonging activities of Panobinostat. Approved, Investigational Pazopanib Pasireotide may increase the QTc-prolonging activities of Pazopanib. 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, Investigational Perflutren Pasireotide may increase the QTc-prolonging activities of Perflutren. Approved Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Pasireotide. Approved, Investigational, Withdrawn Pimozide Pasireotide may increase the QTc-prolonging activities of Pimozide. Approved Pindolol Pindolol may increase the bradycardic activities of Pasireotide. Approved, Investigational Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Pasireotide. Approved, Investigational 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 Quetiapine Pasireotide may increase the QTc-prolonging activities of Quetiapine. Approved Quinidine Pasireotide may increase the QTc-prolonging activities of Quinidine. Approved, Investigational Quinine Pasireotide may increase the QTc-prolonging activities of Quinine. 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 Ruxolitinib Ruxolitinib may increase the bradycardic activities of Pasireotide. 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 Sitagliptin The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide. Approved, Investigational Sotagliflozin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Pasireotide. Investigational Sotalol Pasireotide may increase the QTc-prolonging activities of Sotalol. Approved Sufentanil Sufentanil may increase the bradycardic activities of Pasireotide. Approved, Investigational Sulfadiazine Sulfadiazine may increase the hypoglycemic activities of Pasireotide. Approved, Investigational, 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 Tetrabenazine Pasireotide may increase the QTc-prolonging activities of Tetrabenazine. Approved, Investigational Thioridazine Pasireotide may increase the QTc-prolonging activities of Thioridazine. Approved, Withdrawn Timolol Timolol may increase the bradycardic activities of Pasireotide. Approved Tizanidine Tizanidine may increase the bradycardic activities of Pasireotide. Approved, Investigational Tofacitinib Tofacitinib may increase the bradycardic activities of Pasireotide. Approved, Investigational Tolazamide Tolazamide may increase the hypoglycemic activities of Pasireotide. Approved, Investigational Tolbutamide Tolbutamide may increase the hypoglycemic activities of Pasireotide. Approved, Investigational Toremifene Pasireotide may increase the QTc-prolonging activities of Toremifene. Approved, Investigational Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Pasireotide. Investigational, Withdrawn Vandetanib Pasireotide may increase the QTc-prolonging activities of Vandetanib. Approved Vemurafenib Pasireotide may increase the QTc-prolonging activities of Vemurafenib. 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 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
- KEGG Drug
- D10147
- PubChem Compound
- 9941444
- PubChem Substance
- 175427082
- ChemSpider
- 8117062
- ChEBI
- 72312
- ChEMBL
- CHEMBL3349607
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Pasireotide
- ATC Codes
- H01CB05 — Pasireotide
- AHFS Codes
- 68:29.04 — Somatostatin Agonists
- FDA label
- Download (567 KB)
- MSDS
- Download (567 KB)
Clinical Trials
- Clinical Trials
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 US9351923 No 2008-05-23 2028-05-23 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
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- 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 show 11 more
- 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 show 28 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- homodetic cyclic peptide, peptide hormone (CHEBI:72312)
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 stim...
- 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]
- 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 ...
- 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]
- 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]
- 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 act...
- 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 April 23, 2018 23:11