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
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
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 |
Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, indicated for the treatment of adult
patients with Cushing’s disease for whom pituitary surgery is not an option or
has not been curative. SIGNIFOR is an injectable cyclohexapeptide somatostatin analogue. Pasireotide exerts its
pharmacological activity via binding to somatostatin receptors (ssts). Pasireotide binds and activates the hsst receptors resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion.
Originator
Sources: http://adisinsight.springer.com/drugs/800018195
Curator's Comment: # Novartis
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1917 |
9.3 nM [IC50] | ||
Target ID: CHEMBL1804 |
1.0 nM [IC50] | ||
Target ID: CHEMBL2028 |
1.5 nM [IC50] | ||
Target ID: CHEMBL1792 |
0.16 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | SIGNIFOR Approved UseSIGNIFOR 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 Date2012 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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
Dose | Population | Adverse events |
---|---|---|
1500 ug single, subcutaneous Highest studied dose Dose: 1500 ug Route: subcutaneous Route: single Dose: 1500 ug Sources: |
healthy, 18–40 years |
|
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 |
|
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 |
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%) Sources: 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%) |
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%) Sources: 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%) |
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) Sources: Lipase increased (4 patients) |
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) Other AEs:Hyperglycemia (4 patients) Hyperglycemia (grade 3-4, 6.3%) Sources: Abdominal pain (grade 3-4, 7.7%) Blood alkaline phosphatase increased (grade 3-4, 7.7%) |
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 Health Status: healthy Sources: |
Other AEs: Diarrhea... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
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 Health Status: healthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 5.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 52.0 |
no | |||
Page: 80.0 |
no | |||
Page: 18.0 |
no | |||
Page: 18.0 |
no | |||
Page: 5.0 |
no | |||
Page: 5.0 |
no | |||
Page: 80.0 |
no | |||
Page: 78.0 |
no | |||
Page: 48.0 |
unlikely [IC50 >30 uM] | |||
Page: 80.0 |
unlikely | |||
Page: 80.0 |
unlikely | |||
Page: 77.0 |
weak [IC50 10 uM] | |||
Page: 77.0 |
weak [IC50 10 uM] | |||
Page: 77.0 |
weak [IC50 25 uM] | |||
Page: 77.0 |
weak [IC50 50 uM] | |||
Page: 18.0 |
weak [IC50 80 uM] | |||
Page: 77.0 |
weak [IC50 >100 uM] | |||
Page: 324.0 |
weak [IC50 >59 uM] | |||
Page: 324.0 |
yes [IC50 10 uM] | |||
Page: 324.0 |
yes [IC50 10 uM] | |||
Page: 324.0 |
yes [IC50 5 uM] | |||
Page: 324.0 |
yes [IC50 5 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 12.0 |
likely | yes (co-administration study) Comment: verapamil increased pasireotide permeation Page: 12.0 |
||
Page: 12.0 |
no | |||
Page: 12.0 |
no | |||
Page: 12.0 |
no | |||
Page: 12.0 |
no | |||
Page: 12.0 |
no | |||
Page: 324.0 |
weak | |||
Page: 324.0 |
weak |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 52.0 |
||||
Page: 42.0 |
PubMed
Title | Date | PubMed |
---|---|---|
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
Sample Use Guides
Recommended initial dosage is either 0.6 mg or 0.9 mg by subcutaneous
injection twice a day; recommended dosage range is 0.3 mg to 0.9 mg
twice a day
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22634958
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
Edited
Wed Apr 02 08:24:12 GMT 2025
by
admin
on
Wed Apr 02 08:24:12 GMT 2025
|
Record UNII |
98H1T17066
|
Record Status |
FAILED
|
Record Version |
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Classification Tree | Code System | Code | ||
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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
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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
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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
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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
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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
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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
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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
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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
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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
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Code System | Code | Type | Description | ||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | Merck Index | ||
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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
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PRIMARY | RxNorm | ||
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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
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PRIMARY |
Related Record | Type | Details | ||
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PARENT -> DERIVATIVE |
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SALT/SOLVATE -> PARENT |
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> NON-SUBSTRATE |
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TARGET -> AGONIST |
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> NON-SUBSTRATE |
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> INHIBITOR |
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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.
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TRANSPORTER -> SUBSTRATE |
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TRANSPORTER -> NON-SUBSTRATE |
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TRANSPORTER -> NON-SUBSTRATE |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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SC INJECTION |
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Biological Half-life | PHARMACOKINETIC |
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