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Identification
- Summary
Secretin human is a secretin hormone used to stimulate pancreatic or gastric secretions to diagnose exocrine pancreas dysfunction, gastrinoma, and abnormalities in the bile and pancreatic ducts.
- Brand Names
- Chirhostim
- Generic Name
- Secretin human
- DrugBank Accession Number
- DB09532
- Background
Human secretin is a gastrointestinal peptide hormone that regulates secretions in the stomach, pancreas, and liver. The hormone is produced from the enterochromaffin cells in the duodenum in response to the duodenal content with the pH less than 4.5 5. The main action of secretin is to stimulate the pancreas to secrete pancreatic juice for pH regulation in the small intestines. Secretin is also responsible in body fluid homeostasis 4 and bile production. Although it is a gastrointestinal hormone, secretin is also considered as a neuropeptide hormone since it is also expressed in the central nervous system 3.
Purified synthetic human secretin, also referred to as RG1068, is available as an intravenous injection under the market name ChiRhoStim ® in the U.S.. It contains an amino acid sequence identical to the naturally occurring hormone consisting of 27 amino acids Label that supports α-helical formation 3. The carboxyl-terminal amino acid, valine, is amidated. Synthetic human secretin displays equivalent biological activity and properties as naturally-occurring secretin 1. It is indicated for the stimulation of the pancreatic and gastric secretions to aid in the diagnosis of pancreatic exocrine dysfunction and the diagnosis of gastrinoma, and facilitate the identification of the ampulla of Vater and accessory papilla during endoscopic retrograde cholangiopancreatography (ERCP).
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Structure
- Protein Chemical Formula
- C130H220N44O39
- Protein Average Weight
- 3039.44 Da
- Sequences
>Human Secretin HSDGTFTSELSRLREGARLQRLLQGLV
Download FASTA Format- Synonyms
- Human secretin
- Secretin
- Secretin (human)
- Secretin human
- Secretin synthetic human
- Synthetic human secretin
- External IDs
- RG-1068
- RG1068
Pharmacology
- Indication
Indicated for the stimulation of:
pancreatic secretions, including bicarbonate, to aid in the diagnosis of pancreatic exocrine dysfunction Label.
gastrin secretion to aid in the diagnosis of gastrinoma Label.
pancreatic secretions to facilitate the identification of the ampulla of Vater and accessory papilla during endoscopic retrograde cholangiopancreatography (ERCP) Label.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Gastrinoma •••••••••••• Diagnostic agent Pancreatic exocrine dysfunction •••••••••••• - Contraindications & Blackbox Warnings
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In clinical trials, intravenous administration of synthetic human secretin stimulated the exocrine pancreas to promote juice and bicarbonate secretion, with variable responses depending on the pancreatic function of the individual Label. Having an identical amino acid sequence to the biologically-derived secretin, synthetic human secretin exhibits an equivalent biological activity as the natural hormone. The biological activity of synthetic human secretin was approximately 5.0 CU per mcg Label. In patients with suspected or known exocrine pancreatic dysfunction, a volume response of less than 2 mL/kg/hr, peak bicarbonate concentration of less than 80 mEq/L, and a bicarbonate output of less than 0.2 mEq/kg/hr following intravenous synthetic human secretin Label. Administration in healthy subjects in three crossover studies led to overall pancreatic secretory response of a mean peak bicarbonate concentration of 100 mEq/L, a mean total volume over one hour of 260.7 mL, and a peak bicarbonate concentrations ≥ 80 mEq/L Label.
In a baseline-controlled study of patients with acute and acute recurrent pancreatitis undergoing magnetic resonance cholangiopancreatography (MRCP), administration of synthetic human secretin resulted in higher levels of sensitivity with minimal loss in specificity. This indicates that the stimulation of pancreatic secretions by synthetic secretin facilitates the diagnosis and clinical decision making of patients acute, acute recurrent, or chronic pancreatitis 2.
- Mechanism of action
Synthetic human secretin mediates the same biological effects as the naturally-occurring gastrointestinal peptide hormone. Secretin is normally released from enterochromaffin cells and S cells in the intestinal mucosa of duodenum upon exposure of proximal intestinal lumen to the acidic gastric content, or fatty acids and amino acids Label. Secretin mediates an inhibitory effect on acid secretion by parietal cells of the stomach, and causes alkalinazation of the duodenal content by stimulating the release of pancreatic juice, which has high amounts of water and bicarbonate ions 5. Bicarbonate ions are released into the duodenum from the centroacinar cells, and epithelia lining the pancreatic and biliary ducts 3. Human secretin is a ligand at G-protein coupled secretin receptors which are expressed in the basolateral domain of several tissue cell types 3, including pancreas, stomach, liver, colon and other tissues Label. Upon interaction, levels of cAMP increase and initiates the cAMP-mediated signalling cascade that results in phosphorylation of protein kinase A (PKA) and activation of cystic fibrosis transmembrane conductance regulator (CFTR) 3. Activation of CFTR activates Cl-/HCO3- anion exchanger 2 and leads to secretion of bicarbonate-rich-pancreatic fluid 3. Via the same cAMP signalling pathway, secretin promotes the secretion of water and electrolytes in cholangiocytes 3. Secretin may work through vagal-vagal neural pathways since stimulation of the efferent vagus nerve stimulates bicarbonate secretion and atropine blocks secretin-stimulated pancreatic secretion Label. Additionally, secretin acts as a diuretic to increase urinary volume and bicarbonate excretion 3,4.
Target Actions Organism ASecretin receptor ligandHumans - Absorption
Following intravenous bolus administration of 0.4 mcg/kg, synthetic human secretin concentration rapidly declines to baseline secretin levels within 90 to 120 minutes Label.
- Volume of distribution
The volume of distribution is 2.7 L Label.
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
The elimination half life of synthetic human secretin is 45 minutes Label.
- Clearance
The clearance of synthetic human secretin is 580.9 ± 51.3 mL/min Label.
- Adverse Effects
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In acute toxicity studies with mice and rabbits, a dose of 20 μg/kg of synthetic human secretin was not lethal with no clinical symptoms of toxicity. The no-observed-effect level (NOEL) in rats was 10 μg/kg/day in a 14-day intravenous toxicity study without any evidence of adverse toxicity. The NOEL was 5 μg/kg/day in dogs 5.
Studies assessing the carcinogenic potential, mutagenicity, or potential for impairment of fertility have not been conducted with synthetic human secretin Label.
- 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 Integrate drug-drug
interactions in your softwareAclidinium The therapeutic efficacy of Secretin human can be decreased when used in combination with Aclidinium. Amantadine The therapeutic efficacy of Secretin human can be decreased when used in combination with Amantadine. Amitriptyline The therapeutic efficacy of Secretin human can be decreased when used in combination with Amitriptyline. Amobarbital The therapeutic efficacy of Secretin human can be decreased when used in combination with Amobarbital. Amoxapine The therapeutic efficacy of Secretin human can be decreased when used in combination with Amoxapine. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Secretin human pentahydrochloride 7HP60U6HMM 108072-62-4 Not applicable - International/Other Brands
- SecreFlo (Repligen Corp) / Secremax (Repligen Corp)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image ChiRhoStim Injection, powder, lyophilized, for solution 16 ug/8mL Intravenous ChiRhoClin, Inc. 2004-08-01 Not applicable US 
ChiRhoStim 40 Injection, powder, lyophilized, for solution 40 ug/10mL Intravenous ChiRhoClin, Inc. 2007-06-01 Not applicable US Secretin Inj 75unit/vial Powder, for solution 75 unit / vial Intravenous Ferring Pharmaceuticals 1990-12-31 1999-08-04 Canada 
Categories
- ATC Codes
- V04CK01 — Secretin
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Diagnostic Agents
- Gastrointestinal Agents
- Gastrointestinal Hormones
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Nerve Tissue Proteins
- Neuropeptides
- Peptide Hormones
- Peptides
- Proteins
- Secretin
- Secretin-class Hormone
- Tests for Pancreatic Function
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- A0426J905J
- CAS number
- 108153-74-8
References
- General References
- Lankisch PG, Creutzfeldt W: Effect of synthetic and natural secretin on the function of the exocrine pancreas in man. Digestion. 1981;22(2):61-5. doi: 10.1159/000198596. [Article]
- Sherman S, Freeman ML, Tarnasky PR, Wilcox CM, Kulkarni A, Aisen AM, Jacoby D, Kozarek RA: Administration of secretin (RG1068) increases the sensitivity of detection of duct abnormalities by magnetic resonance cholangiopancreatography in patients with pancreatitis. Gastroenterology. 2014 Sep;147(3):646-654.e2. doi: 10.1053/j.gastro.2014.05.035. Epub 2014 Jun 4. [Article]
- Afroze S, Meng F, Jensen K, McDaniel K, Rahal K, Onori P, Gaudio E, Alpini G, Glaser SS: The physiological roles of secretin and its receptor. Ann Transl Med. 2013 Oct;1(3):29. doi: 10.3978/j.issn.2305-5839.2012.12.01. [Article]
- Chu JY, Cheng CY, Lee VH, Chan YS, Chow BK: Secretin and body fluid homeostasis. Kidney Int. 2011 Feb;79(3):280-7. doi: 10.1038/ki.2010.397. Epub 2010 Oct 13. [Article]
- 21-256 Synthetic Human Secretin Pharmacology Review - FDA [Link]
- External Links
- PubChem Substance
- 347827873
- ChemSpider
- 17314768
- 606396
- ChEBI
- 135913
- ChEMBL
- CHEMBL3039582
- FDA label
- Download (98.3 KB)
Clinical Trials
- Clinical Trials
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Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data4 Completed Diagnostic Sphincter of Oddi Dysfunction 1 somestatus stop reason just information to hide 4 Enrolling by Invitation Diagnostic Diabetes Mellitus / Pancreatitis 1 somestatus stop reason just information to hide 3 Completed Diagnostic Pancreatic Diseases 1 somestatus stop reason just information to hide 3 Completed Diagnostic Pancreatitis 1 somestatus stop reason just information to hide 3 Completed Treatment Autism Disorder 2 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 16 ug/8mL Injection, powder, lyophilized, for solution Intravenous 40 ug/10mL Injection, powder, lyophilized, for solution Intravenous Powder, for solution Intravenous 75 unit / vial - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Receptor for secretin (SCT), which is involved in different processes such as regulation of the pH of the duodenal content, food intake and water homeostasis (PubMed:25332973, PubMed:7612008). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (By similarity). Upon binding to secretin, regulates the pH of the duodenum by (1) inhibiting the secretion of gastric acid from the parietal cells of the stomach and (2) stimulating the production of bicarbonate (NaHCO(3)) from the ductal cells of the pancreas (By similarity). In addition to regulating the pH of the duodenal content, plays a central role in diet induced thermogenesis: acts as a non-sympathetic brown fat (BAT) activator mediating prandial thermogenesis, which consequentially induces satiation. Mechanistically, secretin released by the gut after a meal binds to secretin receptor (SCTR) in brown adipocytes, activating brown fat thermogenesis by stimulating lipolysis, which is sensed in the brain and promotes satiation. Also able to stimulate lipolysis in white adipocytes. Also plays an important role in cellular osmoregulation by regulating renal water reabsorption. Also plays a role in the central nervous system: required for synaptic plasticity (By similarity)
- Specific Function
- G protein-coupled peptide receptor activity
- Gene Name
- SCTR
- Uniprot ID
- P47872
- Uniprot Name
- Secretin receptor
- Molecular Weight
- 50206.135 Da
References
- Miller LJ, Dong M, Harikumar KG: Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor. Br J Pharmacol. 2012 May;166(1):18-26. doi: 10.1111/j.1476-5381.2011.01463.x. [Article]
- Korner M, Hayes GM, Rehmann R, Zimmermann A, Friess H, Miller LJ, Reubi JC: Secretin receptors in normal and diseased human pancreas: marked reduction of receptor binding in ductal neoplasia. Am J Pathol. 2005 Oct;167(4):959-68. doi: 10.1016/S0002-9440(10)61186-8. [Article]
Drug created at November 30, 2015 19:10 / Updated at May 21, 2021 10:21