Identification | |||||
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Name | Pasireotide | ||||
Accession Number | DB06663 | ||||
Type | small molecule | ||||
Description | Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor(R), which is used in the treatment of Cushing's disease. | ||||
Structure |
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Categories (*) | |||||
Molecular Weight | Not Available | ||||
Groups | approved | ||||
Monoisotopic Weight | Not Available | ||||
Pharmacology | |||||
Indication | For the treatment of Cushing's disease, specifically for those patients whom pituitary surgery has not been curative or is not an option. | ||||
Mechanism of action | Pasireotide activates a broad spectrum of somatostatin receptors, exhbiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in Cushing's disease patients. Also this agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin. | ||||
Absorption | The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC. | ||||
Protein binding | Plasma protein binding is 88%. | ||||
Biotransformation | Metabolism is minimal. | ||||
Route of elimination | Pasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%). | ||||
Toxicity | The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus. | ||||
Affected organisms |
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Interactions | |||||
Drug Interactions |
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Food Interactions |
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Somatostatin receptor type 1 | |
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Name | Somatostatin receptor type 1 |
Gene Name | SSTR1 |
Pharmacological action | unknown |
Actions | Not Available |
References |
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DTHybrid score | 1.3485 |
Somatostatin receptor type 2 | |
Name | Somatostatin receptor type 2 |
Gene Name | SSTR2 |
Pharmacological action | unknown |
Actions | Not Available |
References |
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DTHybrid score | 1.6541 |
Somatostatin receptor type 3 | |
Name | Somatostatin receptor type 3 |
Gene Name | SSTR3 |
Pharmacological action | unknown |
Actions | Not Available |
References |
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DTHybrid score | 1.0516 |
Somatostatin receptor type 5 | |
Name | Somatostatin receptor type 5 |
Gene Name | SSTR5 |
Pharmacological action | unknown |
Actions | Not Available |
References |
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DTHybrid score | 1.6533 |
Id | Partner name | Gene Name | Score |
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427 | Substance-P receptor | TACR1 | 0.277 |
1757 | Myeloperoxidase | MPO | 0.2226 |