Pasireotide

Pasireotide Brand Name– SIGNIFOR | SIGNIFOR LAR

What is Pasireotide

Pasireotide is a somatostatin analog. It is indicated for the treatment of adults with Cushing’s disease or acromegaly for whom pituitary surgery is not an option or has not been curative.

The drug inhibits ACTH secretion and, thus, decreases cortisol secretion. In patients with Cushing’s disease, the drug normalizes mean free urinary cortisol concentrations and improves objective clinical signs and symptoms of the disease.

Of patients with persistent or recurrent Cushing’s disease despite pituitary surgery or for whom surgery is not indicated or is refused, the drug is effective in normalizing mean 24-hour urinary free cortisol concentrations after 6 to 7 months of therapy (normal range, 30 to 145 nmol/24 hours), and providing symptomatic disease improvement.

Biochemical control is also able to be achieved in acromegaly patients. In patients naive to drugs used to treat acromegaly, long-acting pasireotide was compared to a somatostatin analog active comparator; the efficacy endpoint was the proportion of patients biochemically controlled (i.e., mean GH level less than 2.5 mcg/L and a normal IGF-1 levels) at month 12. The proportion of patients achieving this level of control was 31.3% and 19.2% for long-acting pasireotide and active comparator, respectively.

In patients with pre-existing acromegaly inadequately controlled on other somatostatin analogs, the proportion of patients achieving biochemical control was 15.4%, 20%, and 0% for long-acting pasireotide 40 mg, long-acting pasireotide 60 mg, or continued pre-trial therapy, respectively, at 6 months.

Hyperglycemia is an expected adverse event of pasireotide even in patients with normal glycemic control; the drug can also prolong the QT interval.

Indications

1. acromegaly
2. Cushing’s syndrome
3. pancreatic fistula

For the treatment of Cushing’s syndrome (Cushing’s disease) in patients for whom pituitary surgery is not an option or has not been curative

Side Effects

1. abdominal pain
2. adrenocortical insufficiency
3. alopecia
4. anemia
5. anorexia
6. anxiety
7. arthralgia
8. asthenia
9. asthenia
10. AV block
11. back pain
12. bradycardia
13. cholelithiasis
14. constipation
15. cough
16. diabetes mellitus
17. diabetic ketoacidosis
18. diarrhea
19. dizziness
20. elevated hepatic enzymes
21. fatigue
22. flatulence
23. headache
24. hematoma
25. hyperamylasemia
26. hyperbilirubinemia
27. hypercholesterolemia
28. hyperglycemia
29. hypertension
30. hyperuricemia
31. hypoglycemia
32. hypokalemia
33. hyponatremia
34. hypopituitarism
35. hypotension
36. hypothyroidism
37. infection
38. influenza
39. injection site reaction
40. insomnia
41. jaundice
42. myalgia
43. myalgia
44. nausea
45. pancreatitis
46. peripheral edema
47. pharyngitis
48. pruritus
49. QT prolongation
50. vertigo
51. vomiting
52. weakness
53. weight loss

Monitoring Parameters

• blood glucose
• blood pressure
• ECG
• gallbladder ultrasound
• glycosylated hemoglobin A1c (HbA1c)
• heart rate
• LFTs
• serum cortisol
• serum magnesium
• serum potassium
• urinary free cortisol

Contraindications

• adrenal insufficiency
• angina
• apheresis
• AV block
• bradycardia
• breast-feeding
• cardiac disease
• cardiomyopathy
• celiac disease
• children
• cholelithiasis
• diabetes mellitus
• diabetic ketoacidosis
• females
• fever
• gallbladder disease
• geriatric
• heart failure
• hepatic disease
• human immunodeficiency virus (HIV) infection
• hyperglycemia
• hyperparathyroidism
• hyperthyroidism
• hypocalcemia
• hypokalemia
• hypomagnesemia
• hypopituitarism
• hypothermia
• hypothyroidism
• infants
• intravenous administration
• long QT syndrome
• myocardial infarction
• neonates
• pancreatitis
• pheochromocytoma
• pituitary insufficiency
• pregnancy
• QT prolongation
• rheumatoid arthritis
• sickle cell disease
• sleep deprivation
• stroke
• systemic lupus erythematosus (SLE)
• thyroid disease

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