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

Details

Stereochemistry ABSOLUTE
Molecular Formula C58H66N10O9
Molecular Weight 1047.2062
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PASIREOTIDE

SMILES

[H][C@@]12C[C@H](CN1C(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(OCC5=CC=CC=C5)C=C4)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC6=CNC7=C6C=CC=C7)NC(=O)[C@@H](NC2=O)C8=CC=CC=C8)OC(=O)NCCN

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

Description

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.

CNS Activity

Originator

Novartis
170
Curator's Comment: # Novartis

Approval Year

2012
614
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2637
 9.3 nM [IC50]
Agonist
2637
 1.0 nM [IC50]
Agonist
2637
 1.5 nM [IC50]
Agonist
2637
 0.16 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8307
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

1.35544321E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
38.7 ng/mL
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29032486/
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24800725/
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
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
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29032486/
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24800725/
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
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29032486/
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24800725/
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:
https://pubmed.ncbi.nlm.nih.gov/22713526
healthy, 18–40 years
n = 6
Health Status: healthy
Age Group: 18–40 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/22713526
Sources:
https://pubmed.ncbi.nlm.nih.gov/22713526
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:
https://pubmed.ncbi.nlm.nih.gov/22713526
healthy, 18–40 years
n = 6
Health Status: healthy
Age Group: 18–40 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/22713526
Sources:
https://pubmed.ncbi.nlm.nih.gov/22713526
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:
https://pubmed.ncbi.nlm.nih.gov/24088755
healthy, 27 years
n = 1
Health Status: healthy
Age Group: 27 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24088755
Disc. AE: Xanthoma...
AEs leading to
discontinuation/dose reduction:
Xanthoma (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24088755
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
Disc. AE: Diarrhea, Lipase increased...
AEs leading to
discontinuation/dose reduction:
Diarrhea (4 patients)
Lipase increased (4 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf
healthy
Health Status: healthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf
Other AEs: Diarrhea...
Other AEs:
Diarrhea
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/24088755
healthy, 27 years
n = 1
Health Status: healthy
Age Group: 27 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24088755
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://pubmed.ncbi.nlm.nih.gov/28721067
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf
healthy
Health Status: healthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1670
inducer
372

inhibitor
1695
inhibitor
1789
inhibitor
1570

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1401

UGT1A1
200

MRP2
363

BSEP
392

CYP2B6
770

OATP1B1
770

OATP1B3
691

CYP1A2
1463

CYP2C8
869

CYP2C19
1410

CYP2E1
846

CYP3A4/5
261

K+ channels
55

L-type Ca2+ channels
25

Nav1.5
95

BCRP
678

OCT1
498

OATP2B1
121
P-gp
1491

BCRP
545

OCT1
317

OATP1B1
389

OATP1B3
333

OATP2B1
103

CYP3A5
383
CYP1A2
671

CYP2B6
521

CYP2C8
163

CYP2C19
283

CYP3A
125

CYP1A1
103

CYP1B1
50

CYP2J2
3

P-gp
252

MRP2
108

UGT1A1
66
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
751
 no
CYP1A1
206
 no
CYP1A2
1620
 no
CYP1B1
66
 no
CYP2B6
946
 no
CYP2C19
1484
 no
CYP2C8
923
 no
CYP2J2
19
 no
CYP3A
291
 no
L-type Ca2+ channels
27
 no
MRP2
452
 no
OATP1B1
785
 no
OATP1B3
700
 no
OATP2B1
124
 no
OCT1
513
 no
P-gp
1588
 no
P-gp
1588
 no
K+ channels
55
 unlikely [IC50 >30 uM]
CYP2C9
1747
 unlikely
UGT1A1
249
 unlikely
CYP1A2
1620
 weak [IC50 10 uM]
CYP3A4/5
314
 weak [IC50 10 uM]
CYP2C19
1484
 weak [IC50 25 uM]
CYP2C8
923
 weak [IC50 50 uM]
CYP2B6
946
 weak [IC50 80 uM]
CYP2E1
929
 weak [IC50 >100 uM]
UGT1A1
249
 weak [IC50 >59 uM]
BSEP
393
 yes [IC50 10 uM]
MRP2
452
 yes [IC50 10 uM]
CYP2C9
1747
 yes [IC50 5 uM]
CYP2D6
1826
 yes [IC50 5 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
1491
 likely
yes (co-administration study)
Comment: verapamil increased pasireotide permeation
Page: 12.0
BCRP
545
 no
OATP1B1
389
 no
OATP1B3
333
 no
OATP2B1
103
 no
OCT1
317
 no
CYP3A4
1670
 weak
CYP3A5
383
 weak
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Nav1.5
98
hERG
1603
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA00C6E9
https://www.aablocks.com/goods/Goods/detail?id=AA00C6E9
Achemtek
0102-014407
http://www.achemtek.com/396091-73-9
Alsachim
3608
http://www.alsachim.com/product-C6134-glo.bal-view.html
BioCrick
BCC5300
http://www.biocrick.com/Pasireotide-BCC5300.html
Chem Scene
CS-2328
http://www.chemscene.com/396091-73-9.html
Lab Network
LN02181389
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN02181389
MedChem Express
HY-16381
https://www.medchemexpress.com/pasireotide.html
MuseChem
I003446
https://www.musechem.com/product/I003446.html
Smolecule
S538667
http://www.smolecule.com/products/s538667
THE BioTek
bt-278884
https://www.thebiotek.com/product/inhibitors/bt-278884
eNovation Chemicals
D678245
https://www.enovationchem.com/ProductDetails.asp?ProductID=D678245
PubMed

PubMed

TitleDatePubMed
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
Patents

Patents

20050014686
3

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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 Sun Dec 18 19:11:30 UTC 2022
Edited
by admin
on Sun Dec 18 19:11:30 UTC 2022
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 Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
NCI_THESAURUS C62799
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
EU-Orphan Drug EU/3/09/671
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
FDA ORPHAN DRUG 188804
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
FDA ORPHAN DRUG 288709
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
NDF-RT N0000175904
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
EMA ASSESSMENT REPORTS SIGNIFOR (AUTHORIZED: ACROMEGALY, PITUITARY ACTH HYPERSECRETION)
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
WHO-ATC H01CB05
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
FDA ORPHAN DRUG 288609
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
Code System Code Type Description
MESH
C517782
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
DRUG BANK
DB06663
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
DRUG CENTRAL
4329
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
PUBCHEM
9941444
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
IUPHAR
2018
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
CHEBI
72313
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
CAS
396091-73-9
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
EVMPD
SUB31564
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
INN
8384
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
ChEMBL
CHEMBL3039583
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
LACTMED
Pasireotide
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
NCI_THESAURUS
C69131
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
CHEBI
72312
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
DAILYMED
98H1T17066
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
WIKIPEDIA
PASIREOTIDE
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
FDA UNII
98H1T17066
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
EPA CompTox
DTXSID501026040
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
MERCK INDEX
M8425
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY Merck Index
RXCUI
1364105
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY RxNorm
USAN
YY-117
Created by admin on Sun Dec 18 19:11:32 UTC 2022 , Edited by admin on Sun Dec 18 19:11:32 UTC 2022
PRIMARY
Related Record Type Details
Structure of PASIREOTIDE DIASPARTATE
SALT/SOLVATE -> PARENT
Structure of PASIREOTIDE PAMOATE
SALT/SOLVATE -> PARENT
OATP-B
TRANSPORTER -> NON-SUBSTRATE
Structure of PASIREOTIDE ACETATE
SALT/SOLVATE -> PARENT
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> NON-SUBSTRATE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A1
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.
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
OATP1B1
TRANSPORTER -> NON-SUBSTRATE
OATP-8
TRANSPORTER -> NON-SUBSTRATE
Related Record Type Details
Structure of PASIREOTIDE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC SC INJECTION

Biological Half-life PHARMACOKINETIC
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