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
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 | 1047.2062 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, indicated for the treatment of adult
patients with Cushing’s disease for whom pituitary surgery is not an option or
has not been curative. SIGNIFOR is an injectable cyclohexapeptide somatostatin analogue. Pasireotide exerts its
pharmacological activity via binding to somatostatin receptors (ssts). Pasireotide binds and activates the hsst receptors resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion.
Originator
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 |
---|---|---|---|---|
38.7 ng/mL |
0.6 mg 2 times / day steady-state, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
PASIREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5.9 ng/mL 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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
161.1 ng × h/mL |
0.6 mg 2 times / day steady-state, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
PASIREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4090 ng × h/mL 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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.4 h |
0.6 mg 2 times / day steady-state, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered: |
PASIREOTIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
12 h 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
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 n = 6 Health Status: healthy Age Group: 18–40 years Sex: M Population Size: 6 Sources: |
|
750 ug 2 times / day steady, subcutaneous Highest studied dose Dose: 750 ug, 2 times / day Route: subcutaneous Route: steady Dose: 750 ug, 2 times / day Sources: |
healthy, 18–40 years n = 6 Health Status: healthy Age Group: 18–40 years Sex: M Population Size: 6 Sources: |
|
0.9 mg 2 times / day multiple, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: multiple Dose: 0.9 mg, 2 times / day Sources: |
healthy, 27 years n = 1 Health Status: healthy Age Group: 27 years Sex: M Population Size: 1 Sources: |
Disc. AE: Xanthoma... AEs leading to discontinuation/dose reduction: Xanthoma (1 patient) Sources: |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Disc. AE: Diarrhea, Nausea... AEs leading to discontinuation/dose reduction: Diarrhea (1.2%) Sources: Page: p. 71-72Nausea (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: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Disc. AE: Diarrhea, Nausea... AEs leading to discontinuation/dose reduction: Diarrhea (2.5%) Sources: Page: p. 71-72Nausea (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) n = 13 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 58.0 years (range: 42–78 years) Sex: M+F Population Size: 13 Sources: |
Disc. AE: Diarrhea, Lipase increased... AEs leading to discontinuation/dose reduction: Diarrhea (4 patients) 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) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 Sources: |
Disc. AE: Gamma-glutamyltransferase increased, Hyperglycemia... Other AEs: Hyperglycemia, Abdominal pain... AEs leading to discontinuation/dose reduction: Gamma-glutamyltransferase increased (4 patients) 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 n = 1 Health Status: healthy Age Group: 27 years Sex: M Population Size: 1 Sources: |
Cholelithiasis | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Diarrhea | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Fatigue | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Hepatic enzyme increased | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Lipase increased | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Nausea | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Tremor | 1.2% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
Hyperglycemia | 2.4% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
GGT increased | 3.7% Disc. AE |
0.6 mg 2 times / day steady, subcutaneous (starting) Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: Page: p. 71-72 |
ALT increased | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
AST increased | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Adrenal insufficiency | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Asthenia | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Confusion state | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Cranial nerve paralysis | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Fatigue | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Fecal incontinence | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Hot flush | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Hypotension | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Immunoglobulin E increased | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Nausea | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Pituitary tumor benign | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
QT interval prolonged | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Tongue paralysis | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Urinary incontinence | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Urticaria | 1.3% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Diarrhea | 2.5% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
GGT increased | 2.5% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Hyperglycemia | 3.8% Disc. AE |
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: Page: p. 71-72 |
unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: Page: p. 71-72 |
Diarrhea | 4 patients Disc. AE |
80 mg 1 times / day steady, intramuscular Dose: 80 mg, 1 times / day Route: intramuscular Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 58.0 years (range: 42–78 years) n = 13 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 58.0 years (range: 42–78 years) Sex: M+F Population Size: 13 Sources: |
Lipase increased | 4 patients Disc. AE |
80 mg 1 times / day steady, intramuscular Dose: 80 mg, 1 times / day Route: intramuscular Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 58.0 years (range: 42–78 years) n = 13 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 58.0 years (range: 42–78 years) Sex: M+F Population Size: 13 Sources: |
Gamma-glutamyltransferase increased | 4 patients Disc. AE |
120 mg 1 times / day steady, intramuscular MTD Dose: 120 mg, 1 times / day Route: intramuscular Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, 60.0 years (range: 44–76 years) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 Sources: |
Hyperglycemia | 4 patients Disc. AE |
120 mg 1 times / day steady, intramuscular MTD Dose: 120 mg, 1 times / day Route: intramuscular Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, 60.0 years (range: 44–76 years) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 Sources: |
Hyperglycemia | grade 3-4, 6.3% | 120 mg 1 times / day steady, intramuscular MTD Dose: 120 mg, 1 times / day Route: intramuscular Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, 60.0 years (range: 44–76 years) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 Sources: |
Abdominal pain | grade 3-4, 7.7% | 120 mg 1 times / day steady, intramuscular MTD Dose: 120 mg, 1 times / day Route: intramuscular Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, 60.0 years (range: 44–76 years) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 Sources: |
Blood alkaline phosphatase increased | grade 3-4, 7.7% | 120 mg 1 times / day steady, intramuscular MTD Dose: 120 mg, 1 times / day Route: intramuscular Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, 60.0 years (range: 44–76 years) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 Sources: |
Diarrhea | 2.1 mg 2 times / day multiple, subcutaneous Overdose Dose: 2.1 mg, 2 times / day Route: subcutaneous Route: multiple Dose: 2.1 mg, 2 times / day Sources: |
healthy 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 |
---|---|---|
SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. | 2002 Oct |
|
Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors. | 2004 |
|
Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230. | 2005 |
|
New aspects in the diagnosis and treatment of Cushing disease. | 2006 |
|
Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways. | 2010 Jan |
|
Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists. | 2011 Jun |
|
Involvement of bone morphogenetic protein activity in somatostatin actions on ovarian steroidogenesis. | 2013 Mar |
Patents
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
Sat Dec 16 16:47:27 GMT 2023
by
admin
on
Sat Dec 16 16:47:27 GMT 2023
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Record UNII |
98H1T17066
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Record Status |
Validated (UNII)
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Record Version |
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-
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Official Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English |
Classification Tree | Code System | Code | ||
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WHO-VATC |
QH01CB05
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NCI_THESAURUS |
C62799
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EU-Orphan Drug |
EU/3/09/671
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FDA ORPHAN DRUG |
188804
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FDA ORPHAN DRUG |
288709
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NDF-RT |
N0000175904
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EMA ASSESSMENT REPORTS |
SIGNIFOR (AUTHORIZED: ACROMEGALY, PITUITARY ACTH HYPERSECRETION)
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WHO-ATC |
H01CB05
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FDA ORPHAN DRUG |
288609
Created by
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Code System | Code | Type | Description | ||
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C517782
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PRIMARY | |||
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DB06663
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PRIMARY | |||
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4329
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PRIMARY | |||
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9941444
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PRIMARY | |||
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2018
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PRIMARY | |||
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72313
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PRIMARY | |||
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396091-73-9
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PRIMARY | |||
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SUB31564
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PRIMARY | |||
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8384
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PRIMARY | |||
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CHEMBL3039583
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PRIMARY | |||
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Pasireotide
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PRIMARY | |||
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C69131
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PRIMARY | |||
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100000124200
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PRIMARY | |||
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72312
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PRIMARY | |||
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98H1T17066
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PRIMARY | |||
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PASIREOTIDE
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PRIMARY | |||
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98H1T17066
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PRIMARY | |||
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DTXSID501026040
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PRIMARY | |||
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m8425
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PRIMARY | Merck Index | ||
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1364105
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PRIMARY | RxNorm | ||
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YY-117
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
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 |
---|---|---|---|---|---|---|
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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