plecanatide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
peptides and glycopeptides	5208	467426-54-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: plecanatide trulance SP-304	Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. Molecular weight: 1681.89 Formula: C65H104N18O26S4 CLOGP: -2.52 LIPINSKI: None HAC: 44 HDO: 23 TPSA: 718.13 ALOGS: -3.83 ROTB: 28

Molecule

Description

Molfile Inchi Smiles

Synonyms:

plecanatide
trulance
SP-304

Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit.

Molecular weight: 1681.89
Formula: C65H104N18O26S4
CLOGP: -2.52
LIPINSKI: None
HAC: 44
HDO: 23
TPSA: 718.13
ALOGS: -3.83
ROTB: 28

Drug dosage:

Dose	Unit	Route
3	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Jan. 19, 2017	FDA	SYNERGY PHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A06AX07	ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation
MeSH PA	D020536	Enzyme Activators
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D000074268	Guanylyl Cyclase C Agonists
FDA MoA	N0000185499	Guanylate Cyclase Activators
FDA EPC	N0000185500	Guanylate Cyclase-C Agonist

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

Disease	Relation	SNOMED_ID	DOID
Chronic idiopathic constipation	indication	82934008

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.25	acidic
pKa2	3.45	acidic
pKa3	3.97	acidic
pKa4	4.37	acidic
pKa5	11.74	acidic
pKa6	12.37	acidic
pKa7	12.62	acidic
pKa8	12.7	acidic
pKa9	13.22	acidic
pKa10	13.36	acidic
pKa11	13.36	acidic
pKa12	13.57	acidic
pKa13	13.71	acidic
pKa14	13.79	acidic
pKa15	7.52	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
3MG	TRULANCE	SALIX	N208745	Jan. 19, 2017	RX	TABLET	ORAL	9610321	Sept. 15, 2031	CHRONIC IDIOPATHIC CONSTIPATION
3MG	TRULANCE	SALIX	N208745	Jan. 19, 2017	RX	TABLET	ORAL	9610321	Sept. 15, 2031	IRRITABLE BOWEL SYNDROME WITH CONSTIPATION
3MG	TRULANCE	SALIX	N208745	Jan. 19, 2017	RX	TABLET	ORAL	9919024	Sept. 15, 2031	CHRONIC IDIOPATHIC CONSTIPATION
3MG	TRULANCE	SALIX	N208745	Jan. 19, 2017	RX	TABLET	ORAL	9919024	Sept. 15, 2031	IRRITABLE BOWEL SYNDROME WITH CONSTIPATION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Heat-stable enterotoxin receptor	Enzyme	P25092	GUC2C_HUMAN	AGONIST	EC50	6.72	SCIENTIFIC LITERATURE	DRUG LABEL
Tumor necrosis factor	Cytokine	P01375	TNFA_HUMAN		Kd	8.42	CHEMBL
Tumor necrosis factor ligand superfamily member 11	Cytokine	O14788	TNF11_HUMAN		IC50	6	CHEMBL
Tumor necrosis factor receptor superfamily member 1A	Unclassified	P19438	TNR1A_HUMAN		IC50	4.66	CHEMBL

External reference:

ID	Source
7IK8Z952OK	UNII
4036439	VANDF
C3711911	UMLSCUI
CHEMBL2103867	ChEMBL_ID
70693500	PUBCHEM_CID
DB13170	DRUGBANK_ID
D09948	KEGG_DRUG
CHEMBL255489	ChEMBL_ID
CHEMBL2105240	ChEMBL_ID
9367	INN_ID
9069	IUPHAR_LIGAND_ID
250462	MMSL
32292	MMSL
d08521	MMSL
017076	NDDF
725134000	SNOMEDCT_US
763544006	SNOMEDCT_US
1873752	RXNORM
C584575	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
TrulanceImmediate release	HUMAN PRESCRIPTION DRUG LABEL	1	65649-003	TABLET	3 mg	ORAL	NDA	26 sections
TrulanceImmediate release	HUMAN PRESCRIPTION DRUG LABEL	1	65649-003	TABLET	3 mg	ORAL	NDA	26 sections
TrulanceImmediate release	HUMAN PRESCRIPTION DRUG LABEL	1	70194-003	TABLET	3 mg	ORAL	NDA	27 sections