Drug information of Pasireotide


Drug group:

Pasireotide is a man-made protein that is similar to a hormone in the body called somatostatin.

Pasireotide is used to treat Cushing's disease or acromegaly (endocrine disorders). Pasireotide is usually given after surgery or other treatments did not work or have stopped working.

Pasireotide may also be used for purposes not listed in this medication guide

Mechanism of effect

Pasireotide is a cyclohexapeptide somatostatin analog, which is a peptide inhibitor of multiple endocrine, neuroendocrine, and exocrine mechanisms. In patients with Cushing disease, pasireotide binds to somatostatin receptor (sst1-5), with high affinity for the sst1, sst2, sst3 subtypes, and highest affinity for the sst5 subtype, resulting in inhibition of ACTH secretion which leads to decreased cortisol secretion. In patients with acromegaly, pasireotide binds to sst2 and sst5, resulting in decreased GH and IGF-1


Primarily eliminated as unchanged drug hepatically (via biliary excretion)
Time to reach the peak
Plasma: Subcutaneous: 0.25 to 0.5 hours
Half life
Subcutaneous: ~12 hours
Feces (~40% to 56%, primarily as unchanged drug); urine (~6% to 10%, primarily as unchanged drug)

Drug indications

Acromegaly (Signifor LAR): Treatment of acromegaly in patients who have had an inadequate response to surgery and/or for whom surgery is not an option

Cushing disease (Signifor and Signifor LAR): Treatment of Cushing disease in patients for whom pituitary surgery is not an option or has not been curative


Usual Adult Dose for Cushing's Syndrome
Intramuscular formulation:
Initial dose: 10 mg intramuscularly every 4 weeks (28 days)
Maximum dose: 40 mg intramuscularly every 4 weeks (28 days), after 4 months of treatment with 10 mg for patients without normalized 24-hour urinary free cortisol (UFC) levels after 4 months treatment who tolerated the 10 mg dose
Subcutaneous formulation:
Initial dose: 0.6 mg or 0.9 mg subcutaneously twice daily.
Maintenance dose: 0.3 to 0.9 mg subcutaneously twice daily.
Maximum dose: 0.9 mg subcutaneously twice daily
Duration of therapy: Treatment should be continued as long as benefit is derived.
Usual Adult Dose for Acromegaly
Intramuscular formulation:
Initial dose: 40 mg, IM, every 28 days
Maximum dose: 60 mg, IM, every 28 days for patients without normalized growth hormone (GH) and/or age and sex adjusted insulin-like growth factor (IGF-1) levels after 3 months treatment who tolerated the 40 mg dose

Drug contraindications

There are no contraindications listed in the manufacturer's labeling.

Side effects

Cardiovascular: Peripheral edema
Central nervous system: Headache, fatigue, hypertension, insomnia, anxiety
Dermatologic: Alopecia
Endocrine & metabolic: Hyperglycemia, diabetes mellitus, hypoglycemia, increased gamma-glutamyl transferase, hypercholesterolemia
Gastrointestinal: Diarrhea, nausea, cholelithiasis, increased serum lipase, abdominal pain, increased serum amylase, upper abdominal pain, abdominal distension, decreased appetite
Hematologic & oncologic: Prolonged partial thromboplastin time, prolonged prothrombin time, elevated glycosylated hemoglobin
Hepatic: Increased serum alanine aminotransferase, increased serum aspartate aminotransferase
Infection: Influenza
Local: Injection site reactions
Neuromuscular & skeletal: Asthenia, increased creatine phosphokinase in blood specimen, myalgia, back pain
Respiratory: Nasopharyngitis
 to 10%
Cardiovascular: Sinus bradycardia, hypotension, atrioventricular block, prolonged QT interval on ECG
Central nervous system: Dizziness, vertigo
Dermatologic: Pruritus, xeroderma
Endocrine & metabolic: Hyperuricemia, hypokalemia, adrenocortical insufficiency, decreased cortisol, weight loss, impaired glucose tolerance/prediabetes, hypothyroidism
Gastrointestinal: Vomiting, constipation, flatulence, cholestasis, cholecystitis, pancreatitis
Hematologic & oncologic: Anemia
Neuromuscular & skeletal: Arthralgia, limb pain
Respiratory: Upper respiratory tract infection, cough
 postmarketing, and/or case reports: Bradycardia, diabetic ketoacidosis, increased serum bilirubin, pancreatitis

Androgens, Antidiabetic Agents, Antidiabetic Agents, Bradycardia-Causing Agents, Ceritinib,
Bromocriptine, Codeine, CycloSPORINE (Systemic), Fexinidazole [INT], Gallium Ga 68 Dotatate,
Gallium Ga 68 Dotatoc, Haloperidol, Herbs (Hypoglycemic Properties), Hypoglycemia-Associated Agents, Ivabradine, Lacosamide, Lutetium Lu 177 Dotatate, Macimorelin, Maitake,
Midodrine, Monoamine Oxidase Inhibitors, Pegvisomant, Pegvisomant, Prothionamide, QT-prolonging Agents (Highest Risk), Quinolones, Ruxolitinib, Salicylates, Selective Serotonin Reuptake Inhibitors, Sincalide, Siponimod, Terlipressin, Tofacitinib


Bradycardia and QT prolongation have been observed with therapy. Use with caution in patients with preexisting cardiac disease, patients with risk factors for bradycardia (eg, high-grade heart block, history of significant bradycardia, receiving concomitant drugs known to cause bradycardia), and/or patients at risk for QT prolongation (eg, congenital long QT, recent MI, heart failure, unstable angina, hypokalemia, hypomagnesemia, receiving concomitant drugs known to cause QT prolongation). Obtain baseline ECG prior to therapy and consider continued monitoring during therapy for an effect on the QTc interval. Correct hypokalemia, hypomagnesemia, and/or hypocalcemia prior to therapy and monitor during therapy

Cholelithiasis and complications of cholelithiasis (eg, cholecystitis, cholangitis, pancreatitis) requiring cholecystectomy have been reported; monitor periodically for cholelithiasis; discontinue and treat appropriately if suspected

Decreases (slight) in thyroid function have been observed during therapy; monitor thyroid function tests prior to therapy and periodically during therapy

Points of recommendation

Pasireotide may lower your cortisol levels. Tell your doctor if you have symptoms such as nausea, vomiting, appetite changes, headache, irritability, confusion, slurred speech, or feeling weak, tired, unsteady, anxious, shaky, or light-headed

Pasireotide can raise your blood sugar and may cause diabetes. Your blood sugar may need to be tested before and during treatment with pasireotide. Call your doctor if you have increased thirst or urination, tiredness, and weight loss even if you are more hungry than usual.

Tell your doctor if you have ever had:
diabetes, or high blood sugar
liver disease
heart problems
an electrolyte imbalance (such as low levels of potassium or magnesium in your blood

It is not known whether pasireotide will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant

Pasireotide may alter hormone levels in a premenopausal woman and may increase the risk of unintended pregnancy. Talk to your doctor about your risk

You should not breast-feed while using pasireotide

Your doctor will perform blood tests to make sure you do not have conditions that would prevent you from safely using pasireotide

Signifor LAR is injected into a muscle once every 4 weeks. A healthcare provider will give you this type of pasireotide injection

Your care provider will show you where on your body to inject pasireotide. Use a different place each time you give an injection. Do not inject into the same place two times in a row. Avoid skin that is red or irritated

Pasireotide can raise your blood sugar, and you may develop diabetes or pre-diabetes. Your blood sugar will need to be tested before and during your treatment with pasireotide. You may need to start using diabetes medication, or adjust the dose of medication you already use. Follow your doctor's instructions very carefully

Your heart function may need to be checked using an electrocardiograph or ECG (sometimes called an EKG).

Store Signifor at room temperature, away from moisture, heat, and light. Throw away an ampule after one use, even if there is still medicine left inside

If you store Signifor LAR at home, keep it in the original carton in the refrigerator. Do not freeze. Take the medicine out of the refrigerator and let it reach room temperature for 30 minutes before injecting your dose. Do not leave the medicine out for longer than 24 hours

Use a needle and syringe only once and then place them in a puncture-proof "sharps" container. Follow state or local laws about how to dispose of this container. Keep it out of the reach of children and pets

Pregnancy level


Limited data with pasireotide in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage

Breast feeding warning

There is no information available on the presence of pasireotide in human milk, the effects of the drug on the breastfed infant, or the effects of the drug on milk production

Drug forms

Signifor, Signifor LAR

Ask a Pharmacist

User's questions
    No comments yet.