Lanreotide Acetate (Monograph)

Brand name: Somatuline Depot
Drug class: Somatostatin Agonists

Medically reviewed by Drugs.com on Nov 10, 2024. Written by ASHP.

Introduction

Synthetic octapeptide pharmacologically related to somatostatin.

Uses for Lanreotide Acetate

Acromegaly

Long-term treatment of acromegaly in patients who have had inadequate responses to or are not candidates for surgical resection and/or radiotherapy (designated an orphan drug by FDA for this use).

Goal of therapy is to normalize concentrations of growth hormone (GH) and insulin-like growth factor 1 (IGF-1).

Improves certain manifestations of acromegaly (asthenia, joint pain, swelling of extremities, excessive perspiration, headache).

Surgical resection of pituitary adenoma is first-line treatment whenever possible. Medical therapy (e.g., long-acting octreotide, lanreotide) recommended in patients with persistent disease despite surgical resection.

Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs)

Treatment of adults with unresectable, well- or moderately differentiated, locally advanced or metastatic GEP-NETs to improve progression-free survival (designated an orphan drug by FDA for this use).

Carcinoid Syndrome

Treatment of carcinoid syndrome in adults. (designated an orphan drug by FDA for this use).

Lanreotide Acetate Dosage and Administration

General

Pretreatment Screening

• Evaluate patients for bradycardia. In patients with preexisting bradycardia, initiate lanreotide with caution.

• Monitor blood glucose concentrations when initiating treatment.

Patient Monitoring

• Acromegaly: Monitor serum GH and IGF-1 concentrations to assess response to therapy and adjust dosage accordingly.

• Monitor blood glucose concentrations when lanreotide dosage is altered; adjust antidiabetic treatment accordingly.

• Periodically monitor for gallstones or complications of gallstones.

• Monitor thyroid function as clinically indicated.

Administration

Administer by deep sub-Q injection only by a healthcare provider.

Sub-Q Administration

Administer by deep sub-Q injection into the superior external quadrant of the buttock; alternate injection sites every 4 weeks between the right and left buttock.

Commercially available as a prefilled syringe.

Allow product to reach room temperature by removing sealed pouch from refrigerator 30 minutes prior to administration. Keep pouch sealed until time of administration.

Insert the needle rapidly to its full length at an angle perpendicular to the skin; the skin should not be pinched prior to administration.

Prefilled syringes are for single-use only; discard after use.

Dosage

Available as lanreotide acetate; dosage expressed in terms of lanreotide.

Adults

Acromegaly

Sub-Q

Initially, 90 mg once every 4 weeks for 3 months.

After 3 months, adjust subsequent dosages based on response (GH and IGF-1 concentrations and clinical response) (see Table 1).

In patients who are controlled on a lanreotide dosage of 60 or 90 mg once every 4 weeks, may consider extending the dosing interval to 120 mg once every 6 or 8 weeks. Determine GH and IGF-I concentrations at 6 weeks after this change in dosing regimen to evaluate for continued patient response.

Continue to monitor patient response (biochemical and clinical control) and adjust dosage as necessary.

Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs)

Sub-Q

120 mg once every 4 weeks.

Carcinoid Syndrome

Sub-Q

120 mg once every 4 weeks.

Patients receiving lanreotide for treatment of GEP-NETs should not receive an additional dose of lanreotide for treatment of carcinoid syndrome.

Special Populations

Hepatic Impairment

Acromegaly

Sub-Q

In patients with moderate to severe hepatic impairment (Child-Pugh class B or C), initially, 60 mg once every 4 weeks for 3 months. Adjust subsequent dosage based on GH and IGF-1 concentrations and clinical response. Caution is advised when considering an extended dosing interval of 120 mg every 6 or 8 weeks in patients with moderate or severe hepatic impairment.

Renal Impairment

Acromegaly

Sub-Q

In patients with moderate to severe renal impairment (Cl_cr<60 mL/minute), initially, 60 mg once every 4 weeks for 3 months. Adjust subsequent dosage based on GH and IGF-1 concentrations and clinical response. Caution is advised when considering an extended dosing interval of 120 mg every 6 or 8 weeks in patients with moderate or severe renal impairment.

Geriatric Patients

Cautious dosage selection because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Cautions for Lanreotide Acetate

Contraindications

• History of hypersensitivity to lanreotide; angioedema and anaphylaxis have been reported following administration.

Warnings/Precautions

Cholelithiasis and Complications

Biliary abnormalities (e.g., cholelithiasis, biliary sludge) occur commonly, due to decreased gallbladder motility, inhibited gallbladder contractility, and decreased bile secretion. Incidence may be related to dose and duration of therapy. Perform gallbladder studies periodically.

Cholelithiasis resulting in complications (e.g., cholecystitis, cholangitis, pancreatitis) and requiring cholecystectomy reported in postmarketing experience. If complications of cholelithiasis suspected, discontinue therapy and initiate appropriate medical therapy.

Endocrine Effects

Hypoglycemia or hyperglycemia can occur as a result of inhibition of insulin and glucagon secretion. Monitor blood glucose concentrations when lanreotide therapy is initiated or dosage adjusted in patients with diabetes mellitus. Adjust dose of antidiabetic agents as necessary.

Slight decreases in thyroid function possible; hypothyroidism reported rarely. Assess thyroid function when indicated.

Cardiovascular Effects

Sinus bradycardia, bradycardia, and hypertension reported. Exercise care when initiating therapy in patients with bradycardia. If symptomatic bradycardia occurs, initiate appropriate therapy.

Patient Monitoring

Monitoring and dosage adjustments in patients with acromegaly are based on GH and IGF-I concentrations.

Steatorrhea and Malabsorption of Dietary Fats

New onset steatorrhea, stool discoloration, and loose stools reported. If new occurrence or worsening of these symptoms, evaluate patients for potential pancreatic exocrine insufficiency and manage accordingly.

Immunogenicity

Potential for immunogenicity with use of therapeutic proteins, such as lanreotide.

Specific Populations

Pregnancy

No adequate and well-controlled studies using lanreotide in pregnant women. In animal studies, embryofetal toxicity (e.g., decreased embryofetal survival, fetal skeletal/soft tissue abnormalities) observed.

Lactation

Not known whether lanreotide is distributed into milk, affects milk production, or has any effects on breast-fed infants. Discontinue nursing during therapy and for 6 months after the last dose.

Females and Males of Reproductive Potential

May impair fertility in females of reproductive potential based on animal data.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults with acromegaly, but increased sensitivity cannot be ruled out.

Insufficient number of patients ≥65 years of age with neuroendocrine tumors to determine whether they respond differently than younger patients.

Hepatic Impairment

Patients with acromegaly: Clearance is decreased in patients with moderate to severe hepatic impairment. Dosage adjustment recommended for such patients.

Patients with GEP-NETs: Effect of hepatic impairment on pharmacokinetics of lanreotide not established.

Renal Impairment

Patients with acromegaly: Clearance may be decreased and half-life and AUC may be increased in patients with end-stage renal function on dialysis. Dosage adjustment recommended for patients with moderate to severe renal impairment (Cl_cr < 60 mL/minute).

Patients with GEP-NETs: Pharmacokinetics of lanreotide not substantially altered in patients with mild to moderate renal impairment (Cl_cr 30–89 mL/minute). Effect of severe renal impairment (Cl_cr <30 mL/minute) on pharmacokinetics of lanreotide not established.

Common Adverse Effects

Acromegaly (>5%): diarrhea, abdominal pain, nausea, injection site reactions.

GEP-NET (>10%): abdominal pain, musculoskeletal pain, vomiting, headache, injection site reaction, hyperglycemia, hypertension, cholelithiasis.

Carcinoid syndrome (≥5% and at least 5% greater than placebo): headache, dizziness, muscle spasm.

Drug Interactions

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP isoenzymes: Potential pharmacokinetic interaction (decreased substrate clearance). Caution advised if used concomitantly with CYP3A4 substrates with a low therapeutic index.

Drugs Associated with Bradycardia

Possible additive effect on heart rate reduction; dosage adjustment of the concomitantly administered drug may be necessary.

Specific Drugs

Lanreotide Acetate Pharmacokinetics

Absorption

Bioavailability

Mean bioavailability was 73.4, 69, and 78.4% following sub-Q administration of single 60-, 90-, and 120-mg dosages, respectively. A drug depot is formed at the injection site allowing for sustained release.

Peak levels obtained during the first day following sub-Q administration.

Duration

Serum concentrations slowly decline over 28 days with low peak to trough fluctuation noted at steady state.

Distribution

Extent

Not known whether lanreotide is distributed into human milk.

Elimination

Elimination Route

<5% excreted in urine; <0.5% recovered unchanged in feces, indicating some biliary excretion.

Half-life

23–30 days following single-dose administration to healthy subjects.

Special Populations

In healthy geriatric individuals, half-life was increased by 85%.

End-stage renal disease requiring dialysis decreases clearance twofold and increases half-life and AUC twofold.

Moderate to severe hepatic impairment reduces clearance by 30%.

Stability

Storage

Parenteral

Injection

2–8°C in original package; protect from light.

If left in sealed pouch at room temperature (not to exceed 40°C) for up to 72 hours, may return to refrigerator for continued storage and later use.

Actions

• Decreases the concentration of GH and IGF-1.

• Inhibits basal secretion of several gastric enzymes (e.g., motilin, gastric inhibitory peptide, pancreatic polypeptide) and postprandial secretion of pancreatic polypeptide, gastrin, and cholecystokinin.

• Has high affinity for somatostatin receptors (SSTR) 2 and 5 in the anterior pituitary and pancreas.

Advice to Patients

• Advise patient to read manufacturer’s patient information.

• Risk of cholelithiasis or complications of gallstones. Stress importance of patients contacting a clinician immediately if they experience sudden abdominal or shoulder pain, fever, chills, nausea, or yellowing of eyes or skin.

• Risk of bradycardia. Stress importance of patients contacting a clinician immediately if they experience bradycardia.

• Risk of hyperglycemia or hypoglycemia. Stress importance of monitoring for signs and symptoms of hyperglycemia (e.g., excessive thirst, increased appetite with weight loss, high urine output, fatigue) or hypoglycemia (e.g., dizziness, confusion, headache, hunger, shakiness). Stress importance of monitoring blood glucose concentration during therapy.

• Risk of thyroid function abnormalities. Advise patients to contact a clinician immediately if they experience signs and symptoms of hypothyroidism (chest pain, shortness of breath, weakness, dizziness, or fainting.

• Risk of hypersensitivity reactions. Inform patients to immediately contact a clinician if a serious hypersensitivity reaction (e.g., angioedema, anaphylaxis) occurs.

• Stress importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Stress importance of patients informing clinicians if they are or plan to become pregnant.

• Advise women to discontinue nursing during therapy and for 6 months after the last dose.

• Advise women that lanreotide may reduce fertility.

• Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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