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pasireotide (Signifor, Signifor LAR): Dosing and Uses

 

Classes: Somatostatin Analogs

Medically reviewed by Min Clinic Staff | Updated: January 2026

Dosing and uses of Signifor, Signifor LAR (pasireotide)

 

Adult dosage forms and strengths

SC injection solution (Signifor)

  • 0.3mg/mL
  • 0.6mg/mL
  • 0.9mg/mL

IM injection suspension (Signifor LAR)

  • 20mg/vial
  • 40mg/vial
  • 60mg/vial

 

Cushing Disease

Indicated for treatment of adults with Cushing disease in whom pituitary surgery is not an option or has not been curative

Signifor: 0.6-0.9 mg SC BID initially; titrate dose based on response and tolerability

Dosage range: 0.3-0.9 mg SC BId

 

Dosage modifications (Cushing Disease)

If started on 0.6 mg BID, a dosage increase to 0.9 mg BID may be considered if treatment tolerated

Temporarily reduce dose for significant adverse effects by decrements of 0.3 mg/injection

Renal impairment: No dosage adjustment required

Hepatic impairment (Cushing Disease)

  • Moderate (Child Pugh B): 0.3 mg SC BID initially; not to exceed 0.6 mg BID
  • Severe (Child Pugh C): Avoid use

 

Acromegaly

Indicated for the treatment of patients with acromegaly who have had an inadequate response to surgery and/or for whom surgery is not an option

Signifor LAR (initial dose): 40 mg IM q4wk

If tolerated, may increase dose to a maximum of 60 mg for patients who have not normalized growth hormone (GH) and/or age and sex adjusted insulin-like growth factor-1 (IGF-1) levels after 3 months of treatment with 40 mg

 

Dosage modifications (Acromegaly)

Renal impairment: No dosage adjustment required

Adverse effect/over-response

  • Adverse reactions or over-response to treatment (age and sex adjusted IGF-1 less than the lower limit of normal) may require dose reduction
  • Decrease the dose, either temporarily or permanently, by 20 mg decrements

Hepatic impairment

  • Mild (Child-Pugh C): No dosage adjustment required
  • Moderate (Child-Pugh B): 20 mg IM q4wk; not to exceed 40 mg q4wk
  • Severe (Child-Pugh C): Avoid use

 

Dosing Considerations

Evaluation for treatment response is based on reduction in 24-hr urinary free cortisol levels and/or improvement in disease signs and symptoms

Maximum urinary free cortisol reduction typically seen by 2 months of treatment

Continue treatment as long as benefit is derived

Intensively optimize antidiabetic therapy (if blood glucose poorly controlled) before initiating pasireotide

Baseline tests

  • Obtain the following before initiating:
  • -Fasting plasma glucose
  • -Hemoglobin A1c
  • -Liver tests
  • -Electrocardiogram
  • -Gallbladder ultrasound

 

Administration

SC injection (Signifor)

  • Visually inspect solution for particulate matter and discoloration; do not use if particulates and/or discoloration observed
  • Avoid injection in sites showing signs of inflammation or irritation
  • Gently pinch skin at the injection site and hold the needle/syringe at an angle of approximately 45 degrees
  • Administer SC by self-injection into the top of thigh or abdomen
  • Rotate injection sites; use of the same injection site for 2 consecutive injections is not recommended

IM injection (Signafor LAR)

  • Remove kit from refrigerator and let it sit for at least 30 min (but not longer than 24 hr)
  • Reconstitute with supplied diluent until powder is completely suspended (see package instructions)
  • Insert the needle fully into the left or right gluteus at a 90° angle to the skin
  • Slowly pull back the plunger to check that no blood vessel has been penetrated (reposition if a blood vessel has been penetrated)
  • Slowly depress the plunger until the syringe is empty
  • Withdraw the needle from the injection site and activate the safety guard

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Signifor, Signifor LAR (pasireotide) adverse (side) effects

>10%

Diarrhea (58%)

Nausea (52%)

Hyperglycemia (40%)

Cholelithiasis (30%)

Headache (28%)

Abdominal pain (24%)

Fatigue (19%)

Diabetes mellitus (18%)

Injection site reactions (17%)

Nasopharyngitis (13%)

Alopecia (12%)

Asthenia (11%)

Increased A1c (11%)

 

1-10%

Increased ALT (10%)

Increased GGT (10%)

Edema, peripheral (10%)

Upper abdominal pain (10%)

Decreased appetite (10%)

Hypercholesterolemia (10%)

Hypertension (10%)

Dizziness (9%)

Hypoglycemia (9%)

Type 2 diabetes mellitus (9%)

Anxiety (9%)

Influenza (9%)

Insomnia (9%)

Myalgia (9%)

Arthralgia (8%)

Pruritus (8%)

Increased lipase (7%)

Constipation (7%)

Hypotension (7%)

Vomiting (7%)

Back pain (6%)

Dry skin (6%)

Prolonged QT interval (6%)

Hypokalemia (6%)

Pain in extremity (6%)

Sinus bradycardia (6%)

Vertigo (6%)

Abdominal distension (6%)

Adrenal insufficiency (6%)

Increased AST (6%)

Increased blood glucose (6%)

Anemia (4%)

Increased amylase (2%)

Prolonged PTT (2%)

 

Warnings

Contraindications

None

 

Cautions

Suppresses ACTH, which may lead to decreased cortisol and potential hypocortisolism; monitor for weakness, fatigue, anorexia, nausea, vomiting, hypotension, hyponatremia, or hypoglycemia

Nearly all patients develop worsening glycemia in first 2 weeks of treatment; higher risk in poorly controlled diabetics (ie, HBA1c >8%)

May cause bradycardia and QT prolongation; obtain baseline and periodic ECG, and potassium and magnesium levels; correct/supplement potassium and /or magnesium if clinically warranted

Increased liver enzymes may require dose interruption and reduction

Cholelithiasis reported; perform gallbladder ultrasound at baseline and at 6- to 12-months

Monitor for pituitary hormone deficiency (eg, TSH/free T4, GH/IGF-1)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Unknown whether distributed in human breast milk; excreted in rat milk at levels 30% of the plasma level; cannot exclude risk to breastfeeding children

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Signifor, Signifor LAR (pasireotide)

Mechanism of action

Cyclohexapeptide somatostatin analog; binds to human somatostatin receptors (hsst) 1, 2, 3, 4 and 5

 

Absorption

Peak plasma time: 0.25-.5 hr

 

Distribution

Protein bound: 88%

Vd: >100 L

P-gp substrate (low)

 

Metabolism

Since somatropin increases CYP450 enzymes, suppression of growth hormone secretion by somatostatin analogs may decrease clearance of compounds metabolized by CYP450 enzymes

 

Elimination

Total body clearance: 3.8 L/hr

Excretion: bile (main), renal (small)