U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C58H66N10O9
Molecular Weight 1047.2084
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PASIREOTIDE

SMILES

c1ccc(cc1)C[C@@]2([H])C(=O)N3C[C@@]([H])(C[C@@]3([H])C(=N[C@@]([H])(c4ccccc4)C(=N[C@]([H])(Cc5c[nH]c6ccccc56)C(=N[C@@]([H])(CCCCN)C(=N[C@@]([H])(Cc7ccc(cc7)OCc8ccccc8)C(=N2)O)O)O)O)O)OC(=NCCN)O

InChI

InChIKey=VMZMNAABQBOLAK-DBILLSOUSA-N
InChI=1S/C58H66N10O9/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/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)/t43-,46+,47+,48-,49+,50+,51+/m1/s1

HIDE SMILES / InChI

Molecular Formula C58H66N10O9
Molecular Weight 1047.2084
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 0
Optical Activity UNSPECIFIED

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

1355443200000
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
Health Status: healthy
Age Group: 18–40 years
Sex: M
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
Health Status: healthy
Age Group: 18–40 years
Sex: M
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
Health Status: healthy
Age Group: 27 years
Sex: M
Sources:
Disc. AE: Xanthoma...
AEs leading to
discontinuation/dose reduction:
Xanthoma (1 patient)
Sources:
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
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)
Health Status: unhealthy
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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
Health Status: healthy
Age Group: 27 years
Sex: M
Sources:
Cholelithiasis 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Diarrhea 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Fatigue 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Hepatic enzyme increased 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Lipase increased 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Nausea 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Tremor 1.2%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
Hyperglycemia 2.4%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
GGT increased 3.7%
Disc. AE
0.6 mg 2 times / day steady, subcutaneous
Recommended
Dose: 0.6 mg, 2 times / day
Route: subcutaneous
Route: steady
Dose: 0.6 mg, 2 times / day
Sources:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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:
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
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)
Health Status: unhealthy
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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
Sourcing
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
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 Jun 26 01:31:38 UTC 2021
Edited
by admin
on Sat Jun 26 01:31:38 UTC 2021
Record UNII
98H1T17066
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PASIREOTIDE
INN   MART.   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
PASIREOTIDE [INN]
Common Name English
CYCLO((4R)-4-(2-AMINOETHYLCARBAMOYLOXY)-L-PROLYL-L-PHENYLGLYCYL-D-TRYPTOPHYL-L-LYSYL-4-O-BENZYL-L-TYROSYL-L-PHENYLALANYL-)
Common Name English
SOM230
Code English
PASIREOTIDE [VANDF]
Common Name English
PASIREOTIDE [MI]
Common Name English
PASIREOTIDE [MART.]
Common Name English
SOM 230
Code English
PASIREOTIDE [WHO-DD]
Common Name English
PASIREOTIDE [USAN]
Common Name English
SOM-230
Code English
Classification Tree Code System Code
WHO-VATC QH01CB05
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
NCI_THESAURUS C62799
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
EU-Orphan Drug EU/3/09/671
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
FDA ORPHAN DRUG 188804
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
FDA ORPHAN DRUG 288709
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
NDF-RT N0000175904
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
EMA ASSESSMENT REPORTS SIGNIFOR (AUTHORIZED: ACROMEGALY, PITUITARY ACTH HYPERSECRETION)
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
WHO-ATC H01CB05
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
FDA ORPHAN DRUG 288609
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
Code System Code Type Description
MESH
C517782
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
DRUG BANK
DB06663
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
DRUG CENTRAL
4329
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
PUBCHEM
9941444
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
IUPHAR
2018
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
CAS
396091-73-9
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
EVMPD
SUB31564
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
INN
8384
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
ChEMBL
CHEMBL3039583
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
LACTMED
Pasireotide
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
NCI_THESAURUS
C69131
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
WIKIPEDIA
PASIREOTIDE
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
FDA UNII
98H1T17066
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY
MERCK INDEX
M8425
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY Merck Index
RXCUI
1364105
Created by admin on Sat Jun 26 01:31:38 UTC 2021 , Edited by admin on Sat Jun 26 01:31:38 UTC 2021
PRIMARY RxNorm
Related Record Type Details
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
TRANSPORTER -> NON-SUBSTRATE
SALT/SOLVATE -> PARENT
TRANSPORTER -> NON-SUBSTRATE
BINDER->LIGAND
BINDING
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> NON-SUBSTRATE
in vitro study results indicate that pasireotide is not a substrate, inhibitor, or inducer for metabolic isozymes including UGT1A1 particularly at the proposed dosing range.
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> NON-SUBSTRATE
TRANSPORTER -> NON-SUBSTRATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC SC INJECTION

Biological Half-life PHARMACOKINETIC