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

Similar Structures

Synonyms

cyclo((4R)-4-(2-aminoethylcarbamoyloxy)-L-prolyl-L-phenylglycyl-D-tryptophyl-L-lysyl-4-O-benzyl-L-tyrosyl-L- phenylalanyl-)
Pasireotida
Pasireotide
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
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Signifor	Solution	0.3 mg	Subcutaneous	Novartis	2013-11-26	Not applicable
Signifor	Injection, solution	0.9 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection, powder, for suspension	60 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection, solution	0.3 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection, solution	0.9 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection	0.9 mg/1mL	Subcutaneous	Novartis Pharmaceuticals Corporation	2012-12-14	Not applicable
Signifor	Injection, powder, for suspension	40 mg	Intramuscular	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection, solution	0.3 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection, solution	0.6 mg	Subcutaneous	Novartis Europharm Limited	2012-04-24	Not applicable
Signifor	Injection	0.6 mg/1mL	Subcutaneous	Novartis Pharmaceuticals Corporation	2012-12-14	Not applicable

Additional Data Available

Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands

Signifor / Signifor LAR

Categories

UNII

98H1T17066

CAS number

396091-73-9

Weight

Average: 1047.2062
Monoisotopic: 1046.50142376

Chemical Formula

C₅₈H₆₆N₁₀O₉

InChI Key

VMZMNAABQBOLAK-DBILLSOUSA-N

InChI

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

IUPAC Name

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

SMILES

NCCCC[C@@H]1NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@@H](NC(=O)[C@@H]2C[C@H](CN2C(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](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.

Associated Conditions

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	Humans
USomatostatin receptor type 2	Not Available	Humans
USomatostatin receptor type 3	Not Available	Humans
USomatostatin receptor type 5	Not Available	Humans

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Additional Data Available

Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available

Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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(R)-warfarin	The serum concentration of (R)-warfarin can be increased when it is combined with Pasireotide.
(S)-Warfarin	The serum concentration of (S)-Warfarin can be increased when it is combined with Pasireotide.
2,4-thiazolidinedione	The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Pasireotide.
4-hydroxycoumarin	The metabolism of 4-hydroxycoumarin can be decreased when combined with Pasireotide.
9-aminocamptothecin	The metabolism of 9-aminocamptothecin can be decreased when combined with Pasireotide.
Abexinostat	The risk or severity of QTc prolongation can be increased when Pasireotide is combined with Abexinostat.
Acarbose	The therapeutic efficacy of Acarbose can be decreased when used in combination with Pasireotide.
Acebutolol	The risk or severity of QTc prolongation can be increased when Pasireotide is combined with Acebutolol.
Acenocoumarol	The serum concentration of Acenocoumarol can be increased when it is combined with Pasireotide.
Aceprometazine	The risk or severity of QTc prolongation can be increased when Pasireotide is combined with Aceprometazine.

Additional Data Available

Extended Description

Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

A severity rating for each drug interaction, from minor to major.

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Evidence Level

A rating for the strength of the evidence supporting each drug interaction.

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Action

An effect category for each drug interaction. Know how this interaction affects the subject drug.

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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

Phase	Status	Purpose	Conditions	Count
1	Completed	Not Available	Alcohol Dependence / Hepatic Cirrhosis	1
1	Completed	Prevention	Atypical Ductal Breast Hyperplasia / Atypical Lobular Hyperplasia (ALH) of Breast / Lobular Carcinoma in Situ (LCIS)	1
1	Completed	Treatment	Acromegaly / Carcinoid Tumors	1
1	Completed	Treatment	Carcinoid Tumors / Neuroendocrine Tumors / Progressive Neuroendocrine Tumors of pancreatic origin	1
1	Completed	Treatment	Castration Resistant Prostate Cancer (CRPC)	1
1	Completed	Treatment	Gastroenteropancreatic Neuroendocrine Tumor of the Pulmonary ot Gastroenteropancreatic System	1
1	Completed	Treatment	Gastrointestinal Tumors	1
1	Completed	Treatment	Malignant Neoplasm of Pancreas	1
1	Completed	Treatment	Metastatic Melanoma and Merkel Cell Carcinoma	1
1	Completed	Treatment	Neuroendocrine Tumors	3
1	Completed	Treatment	Impaired kidney function	1
1	Recruiting	Treatment	Healthy Volunteers	1
1	Recruiting	Treatment	Hyperinsulinemic Hypoglycemia / Post Gastrointestinal Tract Surgery Hypoglycaemia	1
1, 2	Active Not Recruiting	Treatment	Adenocarcinoma of the Prostate / Hormone-Resistant Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer	1
1, 2	Terminated	Treatment	Ductal Carcinoma In Situ	1
2	Active Not Recruiting	Treatment	ACTH-producing pituitary tumour / Pituitary Neoplasms	1
2	Active Not Recruiting	Treatment	Carcinoid Tumors / Neuroendocrine Tumors	1
2	Active Not Recruiting	Treatment	Cushings Disease	1
2	Active Not Recruiting	Treatment	Neuroendocrine Carcinoma of the Lung and Thymus	1
2	Completed	Prevention	Breast Cancer	1
2	Completed	Treatment	Acromegaly	2
2	Completed	Treatment	Acromegaly / Acromegaly, Pituitary Gigantism / Pituitary Gigantism	1
2	Completed	Treatment	Advanced Adult Hepatocellular Carcinoma	1
2	Completed	Treatment	Angiodysplasia	1
2	Completed	Treatment	Autosomal Dominant Polycystic Kidney Disease （ADPKD) / Autosomal Dominant Polycystic Liver Disease / Polycystic Liver Disease (PLD) / Somatostatin Analogs	1
2	Completed	Treatment	Carcinoid Tumors	1
2	Completed	Treatment	Cushing's Syndrome	1
2	Completed	Treatment	Cushings Disease	1
2	Completed	Treatment	Dumping Syndrome Patients	1
2	Completed	Treatment	Haematological Malignancies	1
2	Completed	Treatment	Hepatocellular,Carcinoma	1
2	Completed	Treatment	Hyperglycemia	1
2	Completed	Treatment	Local Recurrent Thymoma / Primary Inoperable Thymoma	1
2	Completed	Treatment	Medullary Thyroid Cancer (MTC)	1
2	Completed	Treatment	Meningiomas	1
2	Completed	Treatment	Non-functioning Pituitary Adenomas	1
2	Completed	Treatment	Postoperative Dumping Syndrome	1
2	Completed	Treatment	Thyroid Cancers	1
2	Completed	Treatment	Uveal Melanoma	1
2	Recruiting	Treatment	Enterostomy	1
2	Terminated	Treatment	Castrate Resistant Prostate Cancer (CRPC) / Chemotherapy Naive Prostate Cancer / Prostate Cancer	1
2	Terminated	Treatment	Cluster Headache - Episodic and Chronic	1
2	Terminated	Treatment	Ectopic Corticotropin Syndrome / Nelson Syndrome / Neoplasms, Pancreatic / Pituitary Neoplasms	1
2	Terminated	Treatment	Gonadotroph Adenomas	1
2	Terminated	Treatment	Islet Cell Tumor	1
2	Terminated	Treatment	Malignancies	1
2	Terminated	Treatment	Nelson Syndrome	1
2	Unknown Status	Treatment	Lung Cancer Small Cell Lung Cancer (SCLC)	1
2	Withdrawn	Treatment	Congenital Hyperinsulinism / Hyperinsulinism / Insulinoma	1
2	Withdrawn	Treatment	Ectopic Corticotropin Syndrome	1
2	Withdrawn	Treatment	Multiple Myeloma (MM)	1
2	Withdrawn	Treatment	Multiple Myeloma (MM) / Multiple Myeloma in Relapse	1
2, 3	Completed	Treatment	Non-functioning Pituitary Adenomas / Prolactinomas	1
3	Active Not Recruiting	Treatment	Acromegaly	1
3	Completed	Treatment	Acromegaly	2
3	Completed	Treatment	Cushings Disease	3
3	Completed	Treatment	Malignant Neoplasm of Pancreas	1
3	Completed	Treatment	Symptomatic Dominant Liver Cyst	1
3	Completed	Treatment	Symptomatic Refractory Resistant Carcinoid Disease	1
4	Active Not Recruiting	Prevention	Neoplasms, Pancreatic / Pancreatic Fistula	1
4	Active Not Recruiting	Treatment	Acromegaly	1
4	Completed	Supportive Care	Acromegaly / Cushings Disease	1
4	Completed	Treatment	BMI >30 kg/m2 / General Surgery / Hypoglycemia	1
4	Completed	Treatment	Cushings Disease	1
4	Enrolling by Invitation	Treatment	Hypoglycemia, Reactive	1
4	Recruiting	Treatment	Acromegaly / Cushings Disease / Dumping Syndrome / Ectopic ACTH Secreting (EAS) Tumors / Melanoma Negative for bRAF / Melanoma Negative for nRAS / Neuroendocrine Tumors / Pituitary Neoplasms / Prostate Cancer	1
4	Withdrawn	Treatment	Gastro-enteropancreatic Neuroendocrine Tumor	1
Not Available	Approved for Marketing	Not Available	Acromegaly	1
Not Available	Available	Not Available	Congenital Hyperinsulinism	1
Not Available	Recruiting	Not Available	Cushings Disease	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

Form	Route	Strength
Injection	Subcutaneous	0.3 mg/1mL
Injection	Subcutaneous	0.6 mg/1mL
Injection	Subcutaneous	0.9 mg/1mL
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
Injection, powder, for suspension, extended release; kit	Intramuscular	10 mg
Injection, powder, for suspension, extended release; kit	Intramuscular	20 mg
Injection, powder, for suspension, extended release; kit	Intramuscular	30 mg
Injection, powder, for suspension, extended release; kit	Intramuscular	40 mg
Injection, powder, for suspension, extended release; kit	Intramuscular	60 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
Unlock Additional Data
US6225284	No	2001-05-01	2016-06-28
US7473761	No	2009-01-06	2025-07-29
US8299209	No	2012-10-30	2025-12-27
US8822637	No	2014-09-02	2023-08-06
US7759308	No	2010-07-20	2026-10-25
US9351923	No	2016-05-31	2028-05-23

Additional Data Available

Filed On

The date on which a patent was filed with the relevant government.

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Properties

State

Solid

Experimental Properties

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

Predicted Properties

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

Predicted ADMET features

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

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

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	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

Details1. Somatostatin receptor type 1

Kind: Protein
Organism: Humans
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]

Details2. Somatostatin receptor type 2

Kind: Protein
Organism: Humans
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]

Details3. Somatostatin receptor type 3

Kind: Protein
Organism: Humans
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]

Details4. Somatostatin receptor type 5

Kind: Protein
Organism: Humans
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]

Enzymes

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Inhibitor

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

Drug created on March 19, 2008 10:46 / Updated on January 21, 2020 16:27

Pasireotide

Identification

Structure for Pasireotide (DB06663)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

References

References

References

References

Enzymes