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Pasireotide is a second-generation somatostatin analogue that hits more receptor types than octreotide. It is approved for Cushing's disease and acromegaly caused by pituitary tumours when surgery has not cured them, at the cost of frequent high blood sugar.
Pasireotide (SOM230) was developed by Novartis and is now marketed by Recordati. The FDA approved the twice-daily subcutaneous form in 2012 for Cushing's disease when surgery is not an option or has failed, the first drug approved for that indication, and the monthly long-acting depot in 2014 for acromegaly inadequately controlled by surgery. It normalises cortisol in a minority and growth hormone and IGF-1 in a larger fraction of patients, and shrinks tumours in many.
Hyperglycaemia, from suppression of insulin and incretins, is the main side effect and often needs treatment. Beyond the pituitary, the phase 2 LUNA trial tested it alone and with everolimus in lung and thymic neuroendocrine tumours and found activity in each arm, without a placebo comparison. The pituitary tumours and lung neuroendocrine tumour pages name it.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
Binds somatostatin receptors 1, 2, 3 and 5, with far higher affinity for SSTR5 than octreotide; SSTR5 dominates on corticotroph adenomas, so it suppresses ACTH in Cushing's disease and growth hormone in acromegaly resistant to first-generation analogues. Connects to Somatostatin receptor 2.
1.Pasireotide binds Somatostatin receptor 2.
| Region | Year | Indication |
|---|---|---|
| US | 2012 | Cushing's disease when pituitary surgery is not an option or has not been curative |
| US | 2014 | Acromegaly inadequately controlled by surgery or for whom surgery is not an option (long-acting depot) |
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Query for this drug: (TITLE:"Pasireotide" OR ABSTRACT:"Pasireotide" OR TITLE:"Signifor" OR ABSTRACT:"Signifor" OR TITLE:"Signifor LAR" OR ABSTRACT:"Signifor LAR" OR TITLE:"SOM230" OR ABSTRACT:"SOM230") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Pasireotide, not a curated reading list.
Shares Recordati, Corticotroph pituitary neuroendocrine tumour (Cushing disease and silent corticotroph tumour), Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma and the tag subtype-drugs-wave.
Shares Somatotroph pituitary neuroendocrine tumour (acromegaly), Corticotroph pituitary neuroendocrine tumour (Cushing disease and silent corticotroph tumour), Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma and the tag subtype-drugs-wave.
Shares Somatostatin analogues (octreotide, lanreotide), Somatostatin receptor 2 and the tag subtype-drugs-wave.
Shares Corticotroph pituitary neuroendocrine tumour (Cushing disease and silent corticotroph tumour) and the tag subtype-drugs-wave.
Shares Everolimus and the tag subtype-drugs-wave.
Shares Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma and the tag subtype-drugs-wave.
Shares Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma and the tag subtype-drugs-wave.
Shares Thyrotroph pituitary neuroendocrine tumour (TSH-secreting), Somatotroph pituitary neuroendocrine tumour (acromegaly), Corticotroph pituitary neuroendocrine tumour (Cushing disease and silent corticotroph tumour), Pituitary tumours (pituitary neuroendocrine tumours) and pituitary carcinoma.