U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
Dolcanatide ia an orally administered analog of the human endogenous natriuretic hormone uroguanylin and guanylate cyclase C (GC-C) agonist, with potential laxative, anti-nociceptive and anti-inflammatory activities. Upon administration, dolcanatide, by mimicking uroguanylin, binds to and activates GC-C locally on endothelial cells in the gastrointestinal (GI) tract, without entering the systemic circulation. Activation of GC-C results in an increase in cyclic guanosine monophosphate (cGMP). Increased concentrations of cGMP lead to the activation of the anion channel cystic fibrosis transmembrane conductance regulator (CFTR). CFTR activation increases the secretion of negatively charged ions, particularly chloride and bicarbonate, into the GI tract lumen, which further drives sodium ions and then water into the lumen. This leads to increased fluid secretion in the GI tract, accelerated transit and changes in stool consistency. In addition, ion channel modulation may decrease muscle contractions and the activity of pain-sensing nerves, thereby decreasing intestinal pain. Also, GC-C may inhibit the secretion of pro-inflammatory cytokines, which may ameliorate GI inflammation. Delconitide is in phase I clinical trial to study how well it works in preventing colorectal cancer in healthy participants.

Approval Year

PubMed

PubMed

TitleDatePubMed
Pharmacology and clinical potential of guanylyl cyclase C agonists in the treatment of ulcerative colitis.
2013
Emerging treatments in Neurogastroenterology: Perspectives of guanylyl cyclase C agonists use in functional gastrointestinal disorders and inflammatory bowel diseases.
2015 Aug
Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis.
2015 Nov 6
The Guanylate Cyclase C-cGMP Signaling Axis Opposes Intestinal Epithelial Injury and Neoplasia.
2018

Sample Use Guides

Single daily dose of 27 mg x 7 days
Route of Administration: Oral
Substance Class Protein
Created
by admin
on Sat Dec 16 08:17:59 UTC 2023
Edited
by admin
on Sat Dec 16 08:17:59 UTC 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
WU977T914K
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DOLCANATIDE
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
D-ASN-ASP-GLU-CYS-GLU-LEU-CYS-VAL-ASN-VAL-ALA-CYS-THR-GLY-CYS-D-LEU (4->12),(7->15)-BIS(DISULFIDE)
Common Name English
Dolcanatide [WHO-DD]
Common Name English
DOLCANATIDE [USAN]
Common Name English
SP-333
Code English
dolcanatide [INN]
Common Name English
D-LEUCINE, D-ASPARAGINYL-L-.ALPHA.-ASPARTYL-L-.ALPHA.-GLUTAMYL-L-CYSTEINYL-L-.ALPHA.-GLUTAMYL-L-LEUCYL-L-CYSTEINYL-L-VALYL-L-ASPARAGINYL-L-VALYL-L-ALANYL-L-CYSTEINYL-L-THREONYLGLYCYL-L-CYSTEINYL-, CYCLIC (4->12),(7->15)-BIS(DISULFIDE)
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C308
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
Code System Code Type Description
NCI_THESAURUS
C153478
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
FDA UNII
WU977T914K
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
INN
10189
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
CAS
1092457-65-2
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
USAN
BC-27
Created by admin on Sat Dec 16 08:18:00 UTC 2023 , Edited by admin on Sat Dec 16 08:18:00 UTC 2023
PRIMARY
ChEMBL
CHEMBL3545122
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
PUBCHEM
91826710
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
DRUG BANK
DB13112
Created by admin on Sat Dec 16 08:17:59 UTC 2023 , Edited by admin on Sat Dec 16 08:17:59 UTC 2023
PRIMARY
From To
1_4 1_12
1_7 1_15
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL