Plecanatide

Therapeutic

Treatment of chronic idiopathic constipation (CIC)

Structural features

SMILES

[H][C@@]12CSSC[C@H](NC(=O)CNC(=O)[C@@]([H])(NC(=O)[C@]([H])(CSSC[C@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N1)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC2=O)C(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(O)=O

Sequence

NDEC(1)ELC(2)VNVAC(1)TGC(2)L

Molar mass

1681.89 g/mol

Constitutional members:

16

Natural amino acids

16

D-Amino acids

0

N-terminus

H

C-terminus

COOH

Cyclic

yes

Members/cycle

multicyclic

Bond to form cycle

2 side chain-to-side chain (disulfide)

Lipidation

no

Glycosylation

no

Route of administration

ORAL

Terminal half-life

Half-life (t½) cannot be calculated due to negligible systemic absorbance

Protein binding

Plecanatide exhibits little to no binding to human serum albumin or human α-1-acid glycoprotein.

Absorption and Bioavailability

Plecanatide is minimally absorbed with negligible systemic availability following oral administration. Concentrations of plecanatide and its active metabolite in plasma are below the limit of quantitation after an oral dose of 3 mg. Therefore, standard pharmacokinetic parameters such as AUC, maximum concentration (Cmax), and half-life (t½) cannot be calculated.

References