Sincalide

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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Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

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

TargetActionsOrganism
ACholecystokinin receptor type A
agonist
Humans
AGastrin/cholecystokinin type B receptor
agonist
Humans
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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Toxicity

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.
DrugInteraction
AsunaprevirThe excretion of Sincalide can be decreased when combined with Asunaprevir.
AtalurenThe excretion of Sincalide can be decreased when combined with Ataluren.
AtazanavirThe excretion of Sincalide can be decreased when combined with Atazanavir.
Beclomethasone dipropionateThe excretion of Sincalide can be decreased when combined with Beclomethasone dipropionate.
Bempedoic acidThe excretion of Sincalide can be decreased when combined with Bempedoic acid.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
KinevacInjection, powder, lyophilized, for solution5 ug/5mLIntravenousGeneral Injectables & Vaccines2010-11-052017-01-17US flag
KinevacInjection, powder, lyophilized, for solution5 ug/5mLIntravenousBracco Diagnostics Inc.1976-07-21Not applicableUS flag
KinevacInjection, powder, lyophilized, for solution5 ug/5mLIntravenousJubilant Hollisterstier Llc2007-09-052018-02-01US flag
KinevacPowder, for solution5 mcg / vialIntravenousBracco Imaging S.P.A.1998-07-08Not applicableCanada flag
Kinevac Pws Inj 5mcg/vialPowder, for solution5 mcg / vialIntravenousSquibb Diagnostics, Division Of Bristol Myers Squibb Canada Inc.1979-12-311998-07-30Canada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
SIncalideSincalide (3 ug/1)Injection, powder, lyophilized, for solutionIntravenousAnazao Health Corporation2012-06-19Not applicableUS flag

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
  1. Maher KA: Kinevac (sincalide for injection)/Squibb Diagnostics. Gastroenterol Nurs. 1991 Oct;14(2):98-100. doi: 10.1097/00001610-199110000-00008. [Article]
  2. FDA Approved Drug Products: KINEVAC (sincalide) injection [Link]
  3. FDA Approved Drug Products: KINEVAC (sincalide for injection), for intravenous use (October 2023) [Link]
KEGG Drug
D05845
PubChem Compound
9833444
PubChem Substance
310265055
ChemSpider
8009168
BindingDB
21147
RxNav
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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package
PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
4CompletedTreatmentType 2 Diabetes Mellitus1somestatusstop reasonjust information to hide
3CompletedOtherHealthy Volunteers (HV)1somestatusstop reasonjust information to hide
1CompletedTreatmentHealthy Volunteers (HV)1somestatusstop reasonjust information to hide
Not AvailableCompletedTreatmentCholestasis1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous5 ug/5mL
Powder, for solutionIntravenous5 mcg / vial
Injection, powder, lyophilized, for solutionIntravenous3 ug/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6803046No2004-10-122022-08-16US flag
US11318100No2018-04-202038-04-20US flag
US11110063No2021-09-072038-04-20US flag
US11737983No2018-04-202038-04-20US flag

Properties

State
Solid
Experimental Properties
Not Available

Targets

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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
  1. 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
  1. 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
  1. 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 July 22, 2024 03:26