Identification
- Summary
Sincalide is a diagnostic agent used to stimulate gallbladder contraction or pancreatic secretion during diagnostic tests, and accelerate fluoroscopy and x-ray examination of the intestinal tract.
- Brand Names
- Kinevac
- Generic Name
- Sincalide
- DrugBank Accession Number
- DB09142
- Background
Sincalide is a medication given by injection to assist in the diagnosis of gallbladder and pancreas disorders. It is identified as the 8-amino acid C-terminal segment of cholecystokinin and is also known as CCK-8. Naturally occurring cholecystokinin is a gastrointestinal peptide hormone normally essential for stimulating protein and fat digestion in the body. When injected intravenously, sincalide produces a substantial reduction in gallbladder size by causing this organ to contract. The evacuation of bile that results is similar to that which occurs physiologically in response to endogenous cholecystokinin. Furthermore, sincalide stimulates the pancreatic secretion of bicarbonate and enzymes.1
As the product Kinevac (FDA), sincalide is used to stimulate the duodenum, pancreas, and small bowel for cholesterol analysis, enzymatic activity analysis, and x-ray examination respectively.3
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones / Peptides - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- CCK C-terminal octapeptide
- CCK-8
- Cholecystokinin C-terminal octapeptide
- Sincalide
- External IDs
- SQ 19844
- SQ-19844
- SQ19844
Pharmacology
- Indication
As the product Kinevac (FDA), sincalide is used for the following indications: 1) to stimulate gallbladder contraction, as may be assessed by various methods of diagnostic imaging, or to obtain by duodenal aspiration a sample of concentrated bile for analysis of cholesterol, bile salts, phospholipids, and crystals; (2) to stimulate pancreatic secretion in combination with secretin prior to obtaining a duodenal aspirate for analysis of enzyme activity, composition, and cytology; (3) to accelerate the transit of a barium meal through the small bowel, thereby decreasing the time and extent of radiation associated with fluoroscopy and x-ray examination of the intestinal tract.3
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- Contraindications & Blackbox Warnings
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Following an intravenous (bolus) injection of 0.02 mcg/kg of sincalide, maximal contraction of the gallbladder occurred in 5 to 15 minutes. Sincalide reduced gallbladder radiographic size by at least 40%, generally considered satisfactory contraction.3
- Mechanism of action
When injected intravenously, sincalide produces a substantial reduction in gallbladder size by causing this organ to contract. The evacuation of bile that results is similar to that which occurs physiologically in response to endogenous cholecystokinin. Like cholecystokinin, sincalide stimulates pancreatic secretion; concurrent administration with secretin increases both the volume of pancreatic secretion and the output of bicarbonate and protein (enzymes) by the gland. This combined effect of secretin and sincalide permits the assessment of specific pancreatic function through measurement and analysis of the duodenal aspirate.3
Target Actions Organism ACholecystokinin receptor type A agonistHumans AGastrin/cholecystokinin type B receptor agonistHumans - Absorption
The intravenous (bolus) administration of sincalide causes a prompt contraction of the gallbladder that becomes maximal in 5 to 15 minutes, as compared with the stimulus of a fatty meal which causes a progressive contraction that becomes maximal after approximately 40 minutes.1
- Volume of distribution
Limited information is available on the volume of distribution of sincalide.
- Protein binding
Limited information is available on the protein binding of sincalide.
- Metabolism
Limited information is available on the metabolism of sincalide.
- Route of elimination
Limited information is available on the route of elimination of sincalide
- Half-life
Limited information is available on the half-life of sincalide.
- Clearance
Not Available
- Adverse Effects
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Based on limited human data and mechanism of action, sincalide may cause preterm labor or spontaneous abortion. Available data with sincalide for injection are insufficient to establish a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal embryo-fetal development studies in which sincalide was administered to hamsters and rats during the period of organogenesis, no effects were seen at doses comparable to the maximum recommended clinical dose on a mg/kg basis. However, in a prenatal development study in which rats were administered sincalide during organogenesis through parturition, decreased weight gain and developmental delays were observed at a dose 122 times higher than the maximum recommended human dose based on body surface area.3
In the event of an overdose, symptoms related to vagal stimulation, such as gastrointestinal symptoms (abdominal cramps, nausea, vomiting, and diarrhea), hypotension with dizziness or fainting may occur. Overdosage symptoms should be treated symptomatically and should be of short duration.3
A single bolus intravenous injection of 0.05 mcg/kg (approximately 2 to 3 times the human dose of 0.02 mcg/kg), sincalide caused hypotension and bradycardia in dogs. In addition, higher doses injected intravenously once or repeatedly in dogs caused syncope and ECG changes (approximately 5 times the human dose of 0.02 mcg/kg). These effects were attributed to sincalide-induced vagal stimulation in that all were prevented by pretreatment with atropine or bilateral vagotomy.3
- 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 softwareAsunaprevir The excretion of Sincalide can be decreased when combined with Asunaprevir. Ataluren The excretion of Sincalide can be decreased when combined with Ataluren. Atazanavir The excretion of Sincalide can be decreased when combined with Atazanavir. Beclomethasone dipropionate The excretion of Sincalide can be decreased when combined with Beclomethasone dipropionate. Bempedoic acid The excretion of Sincalide can be decreased when combined with Bempedoic acid. - 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Kinevac Powder, for solution 5 mcg / vial Intravenous Bracco Imaging S.P.A. 1998-07-08 Not applicable Canada 
Kinevac Injection, powder, lyophilized, for solution 5 ug/5mL Intravenous General Injectables & Vaccines 2010-11-05 2017-01-17 US 
Kinevac Injection, powder, lyophilized, for solution 5 ug/5mL Intravenous Bracco Diagnostics Inc. 1976-07-21 Not applicable US Kinevac Injection, powder, lyophilized, for solution 5 ug/5mL Intravenous Jubilant Hollisterstier Llc 2007-09-05 2018-02-01 US Kinevac Pws Inj 5mcg/vial Powder, for solution 5 mcg / vial Intravenous Squibb Diagnostics, Division Of Bristol Myers Squibb Canada Inc. 1979-12-31 1998-07-30 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image SIncalide Sincalide (3 ug/1) Injection, powder, lyophilized, for solution Intravenous Anazao Health Corporation 2012-06-19 Not applicable US
Categories
- ATC Codes
- V04CC03 — Sincalide
- Drug Categories
- 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
- M03GIQ7Z6P
- CAS number
- 25126-32-3
References
- General References
- Maher KA: Kinevac (sincalide for injection)/Squibb Diagnostics. Gastroenterol Nurs. 1991 Oct;14(2):98-100. doi: 10.1097/00001610-199110000-00008. [Article]
- FDA Approved Drug Products: KINEVAC (sincalide) injection [Link]
- FDA Approved Drug Products: KINEVAC (sincalide for injection), for intravenous use (October 2023) [Link]
- External Links
- KEGG Drug
- D05845
- PubChem Compound
- 9833444
- PubChem Substance
- 310265055
- ChemSpider
- 8009168
- BindingDB
- 21147
- 9800
- ChEBI
- 135946
- ChEMBL
- CHEMBL1121
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Sincalide
- FDA label
- Download (1.5 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Type 2 Diabetes Mellitus 1 3 Completed Other Healthy Volunteers (HV) 1 1 Completed Treatment Healthy Volunteers (HV) 1 Not Available Completed Treatment Cholestasis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 5 ug/5mL Powder, for solution Intravenous 5 mcg / vial Injection, powder, lyophilized, for solution Intravenous 3 ug/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6803046 No 2004-10-12 2022-08-16 US US11318100 No 2018-04-20 2038-04-20 US US11110063 No 2021-09-07 2038-04-20 US US11737983 No 2018-04-20 2038-04-20 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- Curator comments
- Presumably to target since it acts like cholecystokinin
- General Function
- Peptide binding
- Specific Function
- Receptor for cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gas...
- Gene Name
- CCKAR
- Uniprot ID
- P32238
- Uniprot Name
- Cholecystokinin receptor type A
- Molecular Weight
- 47840.645 Da
References
- FDA Approved Drug Products: KINEVAC (sincalide for injection), for intravenous use (October 2023) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- Curator comments
- Presumably to target since it acts like cholecystokinin
- General Function
- Type b gastrin/cholecystokinin receptor binding
- Specific Function
- Receptor for gastrin and cholecystokinin. The CKK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor me...
- Gene Name
- CCKBR
- Uniprot ID
- P32239
- Uniprot Name
- Gastrin/cholecystokinin type B receptor
- Molecular Weight
- 48418.51 Da
References
- FDA Approved Drug Products: KINEVAC (sincalide for injection), for intravenous use (October 2023) [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [Article]
Drug created at September 30, 2015 18:56 / Updated at April 19, 2024 20:55