Information about Pasireotide
Pasireotide is a synthetic polypeptide analogue of somatostatin that resembles the native hormone in its ability to suppress levels and activity of growth hormone, insulin, glucagon and many other gastrointestinal peptides. Because its half-life is longer than somatostatin, pasireotide can be used clinically to treat neuroendocrine pituitary tumors that secrete excessive amounts of growth hormone causing acromegaly, or adrenocorticotropic hormone (ACTH) causing Cushing disease.
Liver safety of Pasireotide
Pasireotide has many side effects including suppression of gall bladder contractility and bile production, and maintenance therapy can cause cholelithiasis and accompanying elevations in serum enzymes and bilirubin.
Mechanism of action of Pasireotide
Pasireotide (pa" ze ree' oh tide) is a synthetic octapeptide and analogue of somatostatin that is used for its ability to suppress levels and activities of hormones (growth hormone, insulin, gastrin, secretin, glucagon) or active neuropeptides (serotonin, vasoactive intestinal polypeptide [VIP]). Natural somatostatin is produced in the hypothalamus and acts to suppress growth hormone release from the pituitary. Somatostatin is also found in other neurons throughout the body and particularly in intestinal and pancreatic neurons, where it is active in suppressing release of hormones and neuropeptides such as insulin, glucagon, ACTH, gastrin, secretin, motilin, VIP, serotonin and cholecystokinin. Because of its short half-life (~3 minutes), somatostatin is impractical as a therapeutic agent, and analogues have been developed that have a more favorable pharmacological profile such as octreotide, pasireotide and lanreotide, all three of which have been marketed in long acting release (LAR) forms to allow once weekly or monthly administration. Pasireotide appears to interact largely with the somatostatin subtypes 1, 2 and 3 and possibly subtype 5 receptors, but otherwise acts in a similar manner to somatostatin. Pasireotide therapy has been shown to improve symptoms and complications of several neuroendocrine tumors including abnormal growth in acromegaly due to growth hormone secreting pituitary tumors and symptoms of excessive glucocorticoid production due to ACTH secreting pituitary tumors.
FDA approval information for Pasireotide
Pasireotide was approved for use in treating Cushing disease in the United States in 2012 and a long acting form for as treatment of acromegaly in 2014.
Brand name for Pasireotide
Pasireotide is available under the brand name Signifor in single dose ampules of 0.3, 0.6 and 0.8 mg in one mL solution for injection which is administered as a subcutaneous injection in doses of 0.3 to 0.9 mg twice daily (for Cushing disease). Pasireotide has been formulated also in a long acting release form under the brand name Signifor LAR, in 20, 40 and 60 mg vials of powder for reconstitution, the recommended dose (acromegaly) being 40 mg by intramuscular injection every 4 weeks with subsequent titration based upon efficacy and tolerance.
Side effects of Pasireotide
Side effects are common. Adverse events from single injections include influenza-like symptoms of fatigue, headache, nausea and vomiting and local infusion reactions. With continued therapy, adverse events can include diarrhea, abdominal pain, back pain, headache, dizziness, hypothyroidism, hypo- and hyperglycemia, arrhythmias and gall bladder disease.
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