sincalide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
4627 25126-32-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sincalide
  • cholecystokinin-8
  • SQ-19844
  • SQ 19844
An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.
  • Molecular weight: 1143.27
  • Formula: C49H62N10O16S3
  • CLOGP: -6.94
  • LIPINSKI: 3
  • HAC: 26
  • HDO: 13
  • TPSA: 426.80
  • ALOGS: -5.41
  • ROTB: 33

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -2.162 Moderate 0.72
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.206 Moderate 0.72
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.089 10^-6 cm/s Moderate 0.72
dh-clint Dog hepatocyte intrinsic clearance 2.061 uL/min/10^6 cells Moderate 0.72
dppb Dog plasma protein binding (% unbound) 50.060 % Moderate 0.72
fcs-ppb Fetal calf serum protein binding (% unbound) 27.500 % Moderate 0.72
herg hERG pIC50 4.599 pIC50 Moderate 0.72
hh-clint Human hepatocyte intrinsic clearance 74.817 uL/min/10^6 cells Moderate 0.72
hlm-clint Human liver microsomal intrinsic clearance 7.379 uL/min/mg protein Moderate 0.72
hppb Human plasma protein binding (% unbound) 40.840 % Moderate 0.72
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 39
kinase-selectivity-class AXL,GRK2,PDK4 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.706 Moderate 0.72
mh-clint Mouse hepatocyte intrinsic clearance 117.761 Moderate 0.72
mppb Mouse plasma protein binding (% unbound) 25.880 Moderate 0.72
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.944 Moderate 0.72
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 15.520 % Moderate 0.72
rh-clint Rat hepatocyte intrinsic clearance 140.605 uL/min/10^6 cells Moderate 0.72
rh-fuinc Rat hepatocyte fraction unbound in incubation 41.120 % Moderate 0.72
rppb Rat plasma protein binding (% unbound) 20.940 % Moderate 0.72
solubility-dd Solubility at pH 7.4 in DMSO 729.458 uM Moderate 0.72

Approvals:

DateAgencyCompanyOrphan
July 21, 1976 FDA BRACCO

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple use of single-use product 166.66 111.55 21 127 1802 90626497

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple use of single-use product 244.51 91.91 28 128 1268 110587875
Therapeutic product effect decreased 141.07 91.91 37 119 244279 110344864

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V04CC03 VARIOUS
DIAGNOSTIC AGENTS
OTHER DIAGNOSTIC AGENTS
Tests for bile duct patency
FDA CS M0004235 Cholecystokinin
FDA EPC N0000175798 Cholecystokinin Analog

Related Drugs by ATC class:

V04CC Tests for bile duct patency 3 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Diagnostic aid indication 2949005
Diagnostic Test for Pancreas Function indication
Gastrointestinal obstruction contraindication 126765001
Pregnancy, function contraindication 289908002
Gallstone Complications contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.68 acidic
pKa2 3.79 acidic
pKa3 12.75 acidic
pKa4 12.79 acidic
pKa5 13.18 acidic
pKa6 13.27 acidic
pKa7 13.67 acidic
pKa8 13.79 acidic
pKa9 8.42 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11110063 April 20, 2038 DIAGNOSIS OF GALL BLADDER DISORDERS OR OTHER DIAGNOSTIC IMAGING BY STIMULATING 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
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11110063 April 20, 2038 DIAGNOSIS OF PANCREATIC DISORDERS BY STIMULATING PANCREATIC SECRETION IN COMBINATION WITH SECRETIN PRIOR TO OBTAINING A DUODENAL ASPIRATE FOR ANALYSIS
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11110063 April 20, 2038 DIAGNOSTIC IMAGING BY ACCELERATING THE TRAN IT OFA 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
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11318100 April 20, 2038 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
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11318100 April 20, 2038 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
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11318100 April 20, 2038 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
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11318100 April 20, 2038 STIMULATE PANCREATIC SECRETION IN COMBINATION WITH SECRETIN PRIOR TO OBTAINING A DUODENAL ASPIRATE FOR ANALYSIS
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11737983 April 20, 2038 DIAGNOSIS OF GALL BLADDER DISORDERS BY STIMULATING 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
0.005MG/VIAL SINCALIDE MAIA PHARMS INC N210850 Nov. 22, 2022 RX POWDER INTRAVENOUS 11737983 April 20, 2038 DIAGNOSIS OF PANCREATIC DISORDERS BY STIMULATING PANCREATIC SECRETION IN COMBINATION WITH SECRETIN PRIOR TO OBTAINING A DUODENAL ASPIRATE FOR ANALYSIS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Cholecystokinin receptor type A GPCR Ki 9.55 CHEMBL
Gastrin/cholecystokinin type B receptor GPCR Ki 9.55 CHEMBL
Cholecystokinin receptor type A GPCR Ki 10.05 CHEMBL
Gastrin/cholecystokinin type B receptor GPCR Ki 9.39 CHEMBL
Gastrin/cholecystokinin type B receptor GPCR IC50 9.52 CHEMBL
Cholecystokinin receptor type A GPCR Ki 9.55 CHEMBL
Cholecystokinin receptor GPCR Ki 9.52 CHEMBL

External reference:

IDSource
D05845 KEGG_DRUG
4017721 VUID
N0000146090 NUI
4017721 VANDF
CHEMBL1121 ChEMBL_ID
3617 INN_ID
DB09142 DRUGBANK_ID
M03GIQ7Z6P UNII
9800 RXNORM
367299 MMSL
5466 MMSL
d03895 MMSL
001215 NDDF
126222003 SNOMEDCT_US
35765001 SNOMEDCT_US
C0037167 UMLSCUI
D012844 MESH_DESCRIPTOR_UI
CHEBI:135946 CHEBI
9833444 PUBCHEM_CID
C410885 MESH_SUPPLEMENTAL_RECORD_UI
M03GIQ7Z6P INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KINEVAC HUMAN PRESCRIPTION DRUG LABEL 1 0270-0556 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 5 ug INTRAVENOUS NDA 23 sections
SIncalide HUMAN PRESCRIPTION DRUG LABEL 1 51808-203 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 3 ug INTRAVENOUS Unapproved drug other 8 sections
SINCALIDE HUMAN PRESCRIPTION DRUG LABEL 1 63323-579 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 5 ug INTRAVENOUS NDA 24 sections
Sincalide Human Prescription Drug Label 1 70511-131 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 5 ug INTRAVENOUS NDA 24 sections
Sincalide HUMAN PRESCRIPTION DRUG LABEL 1 72266-248 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 5 ug INTRAVENOUS NDA 24 sections