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Details

Stereochemistry ABSOLUTE
Molecular Formula C58H66N10O9.C23H16O6
Molecular Weight 1435.5758
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PASIREOTIDE PAMOATE

SMILES

OC(=O)C1=CC2=CC=CC=C2C(CC3=C(O)C(=CC4=CC=CC=C34)C(O)=O)=C1O.[H][C@@]56C[C@H](CN5C(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CC8=CC=C(OCC9=CC=CC=C9)C=C8)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC%10=CNC%11=C%10C=CC=C%11)NC(=O)[C@@H](NC6=O)C%12=CC=CC=C%12)OC(=O)NCCN

InChI

InChIKey=HSXBEUMRBMAVDP-QKXVGOHISA-N
InChI=1S/C58H66N10O9.C23H16O6/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72);1-10,24-25H,11H2,(H,26,27)(H,28,29)/t43-,46+,47+,48-,49+,50+,51+;/m1./s1

HIDE SMILES / InChI

Molecular Formula C23H16O6
Molecular Weight 388.3695
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C58H66N10O9
Molecular Weight 1047.2062
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 0
Optical Activity UNSPECIFIED

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, indicated for the treatment of adult patients with Cushing’s disease for whom pituitary surgery is not an option or has not been curative. SIGNIFOR is an injectable cyclohexapeptide somatostatin analogue. Pasireotide exerts its pharmacological activity via binding to somatostatin receptors (ssts). Pasireotide binds and activates the hsst receptors resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion.

Originator

Curator's Comment: # Novartis

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SIGNIFOR

Approved Use

SIGNIFOR is a somatostatin analog indicated for the treatment of adult patients with Cushing’s disease for whom pituitary surgery is not an option or has not been curative.

Launch Date

2012
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
38.7 ng/mL
0.6 mg 2 times / day steady-state, subcutaneous
dose: 0.6 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.9 ng/mL
60 mg single, subcutaneous
dose: 60 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.3 ng/mL
40 mg single, intramuscular
dose: 40 mg
route of administration: intramuscular
experiment type: single
co-administered:
PASIREOTIDE unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
16.2 ng/mL
60 mg 1 times / month multiple, intramuscular
dose: 60 mg
route of administration: intramuscular
experiment type: multiple
co-administered:
PASIREOTIDE unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
17 ng/mL
60 mg single, intramuscular
dose: 60 mg
route of administration: intramuscular
experiment type: single
co-administered:
PASIREOTIDE unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
17.3 ng/mL
40 mg 1 times / month multiple, intramuscular
dose: 40 mg
route of administration: intramuscular
experiment type: multiple
co-administered:
PASIREOTIDE unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
7.18999999999999 ng/mL
20 mg single, intramuscular
dose: 20 mg
route of administration: intramuscular
experiment type: single
co-administered:
PASIREOTIDE unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
8.22999999999999 ng/mL
20 mg 1 times / month multiple, intramuscular
dose: 20 mg
route of administration: intramuscular
experiment type: multiple
co-administered:
PASIREOTIDE unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
161.1 ng × h/mL
0.6 mg 2 times / day steady-state, subcutaneous
dose: 0.6 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4090 ng × h/mL
60 mg single, subcutaneous
dose: 60 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.4 h
0.6 mg 2 times / day steady-state, subcutaneous
dose: 0.6 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12 h
60 mg single, subcutaneous
dose: 60 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
1500 ug single, subcutaneous
Highest studied dose
Dose: 1500 ug
Route: subcutaneous
Route: single
Dose: 1500 ug
Sources:
healthy, 18–40 years
n = 6
Health Status: healthy
Age Group: 18–40 years
Sex: M
Population Size: 6
Sources:
750 ug 2 times / day steady, subcutaneous
Highest studied dose
Dose: 750 ug, 2 times / day
Route: subcutaneous
Route: steady
Dose: 750 ug, 2 times / day
Sources:
healthy, 18–40 years
n = 6
Health Status: healthy
Age Group: 18–40 years
Sex: M
Population Size: 6
Sources:
0.9 mg 2 times / day multiple, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: multiple
Dose: 0.9 mg, 2 times / day
Sources:
healthy, 27 years
n = 1
Health Status: healthy
Age Group: 27 years
Sex: M
Population Size: 1
Sources:
Disc. AE: Xanthoma...
AEs leading to
discontinuation/dose reduction:
Xanthoma (1 patient)
Sources:
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Disc. AE: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (1.2%)
Nausea (1.2%)
Fatigue (1.2%)
Cholelithiasis (1.2%)
GGT increased (3.7%)
Hepatic enzyme increased (1.2%)
Lipase increased (1.2%)
Hyperglycemia (2.4%)
Tremor (1.2%)
Sources: Page: p. 71-72
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Disc. AE: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (2.5%)
Nausea (1.3%)
Fatigue (1.3%)
Pituitary tumor benign (1.3%)
GGT increased (2.5%)
Cranial nerve paralysis (1.3%)
Confusion state (1.3%)
Hyperglycemia (3.8%)
Tongue paralysis (1.3%)
Adrenal insufficiency (1.3%)
Fecal incontinence (1.3%)
Asthenia (1.3%)
ALT increased (1.3%)
AST increased (1.3%)
Immunoglobulin E increased (1.3%)
QT interval prolonged (1.3%)
Urinary incontinence (1.3%)
Urticaria (1.3%)
Hot flush (1.3%)
Hypotension (1.3%)
Sources: Page: p. 71-72
80 mg 1 times / day steady, intramuscular
Dose: 80 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 80 mg, 1 times / day
Sources:
unhealthy, 58.0 years (range: 42–78 years)
n = 13
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
Population Size: 13
Sources:
Disc. AE: Diarrhea, Lipase increased...
AEs leading to
discontinuation/dose reduction:
Diarrhea (4 patients)
Lipase increased (4 patients)
Sources:
120 mg 1 times / day steady, intramuscular
MTD
Dose: 120 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, 60.0 years (range: 44–76 years)
n = 16
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
Population Size: 16
Sources:
Disc. AE: Gamma-glutamyltransferase increased, Hyperglycemia...
Other AEs: Hyperglycemia, Abdominal pain...
AEs leading to
discontinuation/dose reduction:
Gamma-glutamyltransferase increased (4 patients)
Hyperglycemia (4 patients)
Other AEs:
Hyperglycemia (grade 3-4, 6.3%)
Abdominal pain (grade 3-4, 7.7%)
Blood alkaline phosphatase increased (grade 3-4, 7.7%)
Sources:
2.1 mg 2 times / day multiple, subcutaneous
Overdose
Dose: 2.1 mg, 2 times / day
Route: subcutaneous
Route: multiple
Dose: 2.1 mg, 2 times / day
Sources:
healthy
Other AEs: Diarrhea...
AEs

AEs

AESignificanceDosePopulation
Xanthoma 1 patient
Disc. AE
0.9 mg 2 times / day multiple, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: multiple
Dose: 0.9 mg, 2 times / day
Sources:
healthy, 27 years
n = 1
Health Status: healthy
Age Group: 27 years
Sex: M
Population Size: 1
Sources:
Cholelithiasis 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Diarrhea 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Fatigue 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Hepatic enzyme increased 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Lipase increased 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Nausea 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Tremor 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
Hyperglycemia 2.4%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
GGT increased 3.7%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous (starting)
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 82
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 82
Sources: Page: p. 71-72
ALT increased 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
AST increased 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Adrenal insufficiency 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Asthenia 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Confusion state 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Cranial nerve paralysis 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Fatigue 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Fecal incontinence 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Hot flush 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Hypotension 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Immunoglobulin E increased 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Nausea 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Pituitary tumor benign 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
QT interval prolonged 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Tongue paralysis 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Urinary incontinence 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Urticaria 1.3%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Diarrhea 2.5%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
GGT increased 2.5%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Hyperglycemia 3.8%
Disc. AE
0.9 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.9 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.9 mg, 2 times / day
Sources: Page: p. 71-72
unhealthy, 40 years
n = 80
Health Status: unhealthy
Condition: Cushing’s disease
Age Group: 40 years
Sex: M+F
Population Size: 80
Sources: Page: p. 71-72
Diarrhea 4 patients
Disc. AE
80 mg 1 times / day steady, intramuscular
Dose: 80 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 80 mg, 1 times / day
Sources:
unhealthy, 58.0 years (range: 42–78 years)
n = 13
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
Population Size: 13
Sources:
Lipase increased 4 patients
Disc. AE
80 mg 1 times / day steady, intramuscular
Dose: 80 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 80 mg, 1 times / day
Sources:
unhealthy, 58.0 years (range: 42–78 years)
n = 13
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
Population Size: 13
Sources:
Gamma-glutamyltransferase increased 4 patients
Disc. AE
120 mg 1 times / day steady, intramuscular
MTD
Dose: 120 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, 60.0 years (range: 44–76 years)
n = 16
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
Population Size: 16
Sources:
Hyperglycemia 4 patients
Disc. AE
120 mg 1 times / day steady, intramuscular
MTD
Dose: 120 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, 60.0 years (range: 44–76 years)
n = 16
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
Population Size: 16
Sources:
Hyperglycemia grade 3-4, 6.3%
120 mg 1 times / day steady, intramuscular
MTD
Dose: 120 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, 60.0 years (range: 44–76 years)
n = 16
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
Population Size: 16
Sources:
Abdominal pain grade 3-4, 7.7%
120 mg 1 times / day steady, intramuscular
MTD
Dose: 120 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, 60.0 years (range: 44–76 years)
n = 16
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
Population Size: 16
Sources:
Blood alkaline phosphatase increased grade 3-4, 7.7%
120 mg 1 times / day steady, intramuscular
MTD
Dose: 120 mg, 1 times / day
Route: intramuscular
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, 60.0 years (range: 44–76 years)
n = 16
Health Status: unhealthy
Condition: neuroendocrine tumors
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
Population Size: 16
Sources:
Diarrhea
2.1 mg 2 times / day multiple, subcutaneous
Overdose
Dose: 2.1 mg, 2 times / day
Route: subcutaneous
Route: multiple
Dose: 2.1 mg, 2 times / day
Sources:
healthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
unlikely [IC50 >30 uM]
unlikely
unlikely
weak [IC50 10 uM]
weak [IC50 10 uM]
weak [IC50 25 uM]
weak [IC50 50 uM]
weak [IC50 80 uM]
weak [IC50 >100 uM]
weak [IC50 >59 uM]
yes [IC50 10 uM]
yes [IC50 10 uM]
yes [IC50 5 uM]
yes [IC50 5 uM]
Drug as victimTox targets
PubMed

PubMed

TitleDatePubMed
SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs.
2002 Oct
Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors.
2004
Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230.
2005
New aspects in the diagnosis and treatment of Cushing disease.
2006
Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.
2010 Jan
Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.
2011 Jun
Involvement of bone morphogenetic protein activity in somatostatin actions on ovarian steroidogenesis.
2013 Mar
Patents

Patents

Sample Use Guides

Recommended initial dosage is either 0.6 mg or 0.9 mg by subcutaneous injection twice a day; recommended dosage range is 0.3 mg to 0.9 mg twice a day
Route of Administration: Other
Primary cultures from normal human and rat adrenals were incubated with 10-100 nM Pasireotide with and without 10nM ACTH. Dose-response studies with 1 nM-1 uM Pasireotide were performed on rat adrenals. Cortisol/corticosterone levels in medium were measured after 4 and 24h. Pasireotide (10nM) significantly increased corticosteroid levels after 24h incubation in both human (36.4 ± 0.43 ng/well vs 27.7 ± 3.17 ng/well, p<0.05) and rat (16.2 ± 1.16 ng/well vs 11.6 ± 0.92 ng/well p<0.05) adrenals; lesser effects were observed with 100 nM Pasireotide (33.4 ± 2.59 ng/well vs 27.7 ± 3.17 ng/well p<0.05; 13.4 ± 0.82 ng/well vs 11.6 ± 0.92 ng/well, N.S. vs baseline secretion for human and rat adrenals, respectively). Dose-response curves confirmed maximal effect at 10nM Pasireotide.
Substance Class Chemical
Created
by admin
on Sat Dec 16 09:22:19 GMT 2023
Edited
by admin
on Sat Dec 16 09:22:19 GMT 2023
Record UNII
04F55A7UZ3
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PASIREOTIDE PAMOATE
Common Name English
SIGNIFOR LAR
Brand Name English
Pasireotide embonate [WHO-DD]
Common Name English
PASIREOTIDE PAMOATE [JAN]
Common Name English
PASIREOTIDE PAMOATE [ORANGE BOOK]
Common Name English
SOM230 PAMOATE
Code English
SOM-230 PAMOATE
Code English
PASIREOTIDE EMBONATE
WHO-DD  
Common Name English
CYCLO((2S)-2-PHENYLGLYCYL-D-TRYPTOPHYL-L-LYSYL-O-(PHENYLMETHYL)-L-TYROSYL-L-PHENYLALANYL-(4R)-4-((((2-AMINOETHYL)AMINO)CARBONYL)OXY)-L-PROLYL), 4,4'-METHYLENEBIS(3-HYDROXY-2-NAPHTHALENECARBOXYLATE) (1:1)
Systematic Name English
Code System Code Type Description
EVMPD
SUB129748
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
CAS
396091-79-5
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
DRUG BANK
DBSALT001332
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
EPA CompTox
DTXSID601026631
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
ChEMBL
CHEMBL3039583
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
SMS_ID
100000155674
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
RXCUI
1597818
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY RxNorm
PUBCHEM
11982961
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
FDA UNII
04F55A7UZ3
Created by admin on Sat Dec 16 09:22:19 GMT 2023 , Edited by admin on Sat Dec 16 09:22:19 GMT 2023
PRIMARY
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PARENT -> SALT/SOLVATE
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ACTIVE MOIETY