e-Drug3D

1577

PASIREOTIDE

INN
PASIREOTIDE

cas 396091-73-9

CLASS

HORMONES
CUSHING’S DISEASE
SOMATOSTATIN ANALOGUE
HUMAN SOMATOSTATIN RECEPTORS (HSST) AGONISTS
LEADS TO DECREASED CORTISOL SECRETION
HSST1 (IC50 = 9.3 NANOMOLAR)
HSST2 (IC50 = 1.0 NANOMOLAR)
HSST3 (IC50 = 1.5 NANOMOLAR)
HSST4 (IC50 > 1000 NANOMOLAR)
HSST5 (IC50 = 0.16 NANOMOLAR)

ROUTE (list)

SUBCUTANEOUS INTRAMUSCULAR

ATC code

H01CB05

PK parameters

VD 100 LITER
Cl 7.6 LITER / HOUR
PPB 88 PERCENT
t1/2 12 HOUR

Target

TARGET SOMATOSTATIN RECEPTORS (SST)

DrugCentral

Somatostatin receptor type 2 UNIPROT P30874 SSTR2

Somatostatin receptor type 3 UNIPROT P32745 SSTR3

Download SDF file

Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl]

Formula:
C58H66N10O9

Calculated chemical properties:

MW 1047.21
NB_atoms 77
XLogP 3.37
PSA 249.08
NB_HD 11
NB_HA 19
fsp3 0.33
Lipinski(0=no;1=yes) 0

FDA
NDA 200677 (label) INN (PASIREOTIDE DIASPARTATE) SIGNIFOR (RECORDATI RARE) APPROVAL= AP YEAR= 2012 NEWMOLECULARENTITY
NDA 203255 (label) INN (PASIREOTIDE PAMOATE) SIGNIFOR LAR KIT (RECORDATI RARE) APPROVAL= AP YEAR= 2014