Product Name

Pasireotide Diaspartate

CAS Number

820232-50-6

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Product Name:
Pasireotide Diaspartate
CAS Number:
820232-50-6
Indication:
For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.
Mode 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.

Pharmacodynamics:

Signifor® is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.

Metabolism:

Metabolism is minimal.

Toxicity:

The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.

ATC:
H01CB05
DrugBank:
DB06663
Formula:
C58-H66-N10-O9.2C4-H7-N-O4
Molecular Mass:
1313.425
Synonyms:
Cyclo((2R)-2-phenylglycyl-d-tryptophyl-l-lysyl-o-(phenylmethyl)-l-tyrosyl-l-phenylalanyl-(4R)-4-((((2-aminoethyl)amino)carbonyl)oxy)-l-prolyl), l-aspartate (1:2), Pasireotide diaspartate, Pasireotide diaspartate [EMA EPAR], Signifor, UNII-I4P76SY3N4
SMILES:
c1ccc(cc1)C[C@H]2C(=O)N3C[C@@H](C[C@H]3C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2)Cc4ccc(cc4)OCc5ccccc5)CCCCN)Cc6c[nH]c7c6cccc7)c8ccccc8)OC(=O)NCCN.C([C@@H](C(=O)O)N)C(=O)O.C([C@@H](C(=O)O)N)C(=O)O
General Reference:
General Reference:

  1. Weckbecker G, Briner U, Lewis I, Bruns C: SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. Endocrinology. 2002 Oct;143(10):4123-30. Pubmed

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