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This repository is under review for potential modification in compliance with Administration directives.

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

[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 1047.2084
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
177
Curator's Comment: # Novartis

Approval Year

2012
608
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2752
 9.3 nM [IC50]
Agonist
2752
 1.0 nM [IC50]
Agonist
2752
 1.5 nM [IC50]
Agonist
2752
 0.16 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
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
8.23 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
20 mg 1 times / 4 weeks multiple, intramuscular
dose: 20 mg
route of administration: intramuscular
experiment type: multiple
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
17.3 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
40 mg 1 times / 4 weeks multiple, intramuscular
dose: 40 mg
route of administration: intramuscular
experiment type: multiple
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
16.2 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01673646
60 mg 1 times / 4 weeks multiple, intramuscular
dose: 60 mg
route of administration: Intramuscular
experiment type: MULTIPLE
co-administered:
PASIREOTIDE plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.19 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 plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
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 plasma
Homo sapiens
population: unhealthy
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
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 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
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
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
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
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
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
Health Status: healthy
Age Group: 18–40 years
Sex: M
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
Health Status: healthy
Age Group: 18–40 years
Sex: M
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
Health Status: healthy
Age Group: 27 years
Sex: M
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
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
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)
Health Status: unhealthy
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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
Health Status: healthy
Age Group: 27 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24088755
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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
unhealthy, 40 years
Health Status: unhealthy
Age Group: 40 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
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)
Health Status: unhealthy
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 58.0 years (range: 42–78 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 60.0 years (range: 44–76 years)
Sex: M+F
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
1946
inducer
440

inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1741

UGT1A1
246

MRP2
499

BSEP
550

CYP2B6
926

OATP1B1
1079

OATP1B3
961

CYP1A2
2153

CYP2C8
1057

CYP2C19
2057

CYP2E1
1060

CYP3A4/5
296

K+ channels
73

L-type Ca2+ channels
28

Nav1.5
116

BCRP
910

OCT1
620

OATP2B1
157
P-gp
2052

BCRP
697

OCT1
393

OATP1B1
503

OATP1B3
435

OATP2B1
122

CYP3A5
446
CYP1A2
832

CYP2B6
669

CYP2C8
198

CYP2C19
329

CYP3A
142

CYP1A1
151

CYP1B1
71

CYP2J2
3

P-gp
301

MRP2
146

UGT1A1
78
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no
CYP1A1
272
 no
CYP1A2
2333
 no
CYP1B1
93
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C8
1117
 no
CYP2J2
36
 no
CYP3A
317
 no
L-type Ca2+ channels
30
 no
MRP2
625
 no
OATP1B1
1095
 no
OATP1B3
970
 no
OATP2B1
162
 no
OCT1
656
 no
P-gp
1932
 no
P-gp
1932
 no
K+ channels
73
 unlikely [IC50 >30 uM]
CYP2C9
2497
 unlikely
UGT1A1
303
 unlikely
CYP1A2
2333
 weak [IC50 10 uM]
CYP3A4/5
357
 weak [IC50 10 uM]
CYP2C19
2141
 weak [IC50 25 uM]
CYP2C8
1117
 weak [IC50 50 uM]
CYP2B6
1160
 weak [IC50 80 uM]
CYP2E1
1146
 weak [IC50 >100 uM]
UGT1A1
303
 weak [IC50 >59 uM]
BSEP
554
 yes [IC50 10 uM]
MRP2
625
 yes [IC50 10 uM]
CYP2C9
2497
 yes [IC50 5 uM]
CYP2D6
2546
 yes [IC50 5 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
2052
 likely
yes (co-administration study)
Comment: verapamil increased pasireotide permeation
Page: 12.0
BCRP
697
 no
OATP1B1
503
 no
OATP1B3
435
 no
OATP2B1
122
 no
OCT1
393
 no
CYP3A4
1946
 weak
CYP3A5
446
 weak
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Nav1.5
119
hERG
2263
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
eNovation Chemicals
D678245
https://www.enovationchem.com/ProductDetails.asp?ProductID=D678245
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
PubMed

PubMed

TitleDatePubMed
Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230.
2005
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

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 Wed Apr 02 08:24:12 GMT 2025
Edited
by admin
on Wed Apr 02 08:24:12 GMT 2025
Record UNII
98H1T17066
Record Status FAILED
Record Version
  • Download
Name Type Language
PASIREOTIDE
INN   MART.   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
SOM-230
Preferred 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
PASIREOTIDE [VANDF]
Common Name English
PASIREOTIDE [MI]
Common Name English
PASIREOTIDE [MART.]
Common Name English
SOM230
Code English
Pasireotide [WHO-DD]
Common Name English
PASIREOTIDE [USAN]
Common Name English
Classification Tree Code System Code
WHO-VATC QH01CB05
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
NCI_THESAURUS C62799
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
EU-Orphan Drug EU/3/09/671
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
FDA ORPHAN DRUG 188804
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
FDA ORPHAN DRUG 288709
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
NDF-RT N0000175904
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
EMA ASSESSMENT REPORTS SIGNIFOR (AUTHORIZED: ACROMEGALY, PITUITARY ACTH HYPERSECRETION)
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
WHO-ATC H01CB05
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
FDA ORPHAN DRUG 288609
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
Code System Code Type Description
MESH
C517782
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
DRUG BANK
DB06663
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
DRUG CENTRAL
4329
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
PUBCHEM
9941444
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
IUPHAR
2018
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
CHEBI
72313
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
CAS
396091-73-9
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
EVMPD
SUB31564
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
INN
8384
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
ChEMBL
CHEMBL3039583
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
LACTMED
Pasireotide
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
NCI_THESAURUS
C69131
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
SMS_ID
100000124200
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
CHEBI
72312
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
DAILYMED
98H1T17066
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
WIKIPEDIA
PASIREOTIDE
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
FDA UNII
98H1T17066
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
EPA CompTox
DTXSID501026040
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
MERCK INDEX
m8425
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY Merck Index
RXCUI
1364105
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY RxNorm
USAN
YY-117
Created by admin on Wed Apr 02 08:24:12 GMT 2025 , Edited by admin on Wed Apr 02 08:24:12 GMT 2025
PRIMARY
Related Record Type Details
Structure of SOMATOSTATIN
PARENT -> DERIVATIVE
Structure of PASIREOTIDE DIASPARTATE
SALT/SOLVATE -> PARENT
Structure of PASIREOTIDE PAMOATE
SALT/SOLVATE -> PARENT
OATP-B
TRANSPORTER -> NON-SUBSTRATE
SOMATOSTATIN RECEPTOR TYPE 5
TARGET -> AGONIST
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
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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