A long-acting somatostatin receptor analogue known as lanreotide (Somatuiline) is used to treat acromegaly, carcinoid disease, and neuroendocrine tumours in individuals.

Lanreotide (Somatuiline) Indications:

• Acromegaly:

  • It is recommended for the treatment of acromegaly patients who do not respond well to surgery or radiotherapy or for whom those treatments are not an option.
  • The goal of treatment for these patients is to lower their levels of insulin-like growth factor-1 and growth hormone.
  • The Endocrine Society advises the use of somatostatin analogues to lessen perioperative surgical risks and as early adjuvant therapy in patients with moderate to severe signs and symptoms of growth hormone excess following surgery without mass consequences.
  • In patients with modest illness, other medicines may be administered postoperatively.

• Carcinoid syndrome:

  • In order to lessen the frequency of somatostatin analogue rescue therapy, it is approved for the treatment of adult carcinoid syndrome.

• Gastroenteropancreatic neuroendocrine tumours:

  • It is recommended for individuals with well- or moderately-differentiated GEP-NETs (gastroenteropancreatic neuroendocrine tumours) that are locally progressed or metastatic and unresectable by surgery.
  • The aim of therapy in these patients is to improve progression-free survival.

Lanreotide (Somatuiline) Dose in Adults:

Lanreotide dose in the treatment of Acromegaly:

• 90 mg subQ for the first three months, once every four weeks.
• Depending on the clinical and biochemical response (levels of growth hormone and IGF-1) after the first three months, you may need to adjust the dose as follows:

• GH ≤1 ng/mL, IGF-1 normal, symptoms stable:

  • 60 mg administered once every four weeks is the new dose.
  • The extended-release formulation regimen of 120 mg may be used every 6 to 8 weeks once the patient is established on the decreased dose given four times per week.

• GH >1 to 2.5 ng/mL, IGF-1 normal, symptoms stable:

  • Keep taking 90 mg four times each week at the same dose.
  • The extended-interval regimen (120 mg subQ delivered once every 6–8 weeks) may be considered if the patient is stabilised on 90 mg once every four weeks.

• GH >2.5 ng/mL, IGF-1 elevated and/or uncontrolled symptoms:

  • Once every four weeks, increase the dosage from 90 mg to 120 mg subQ.
  • Patients who respond only partially may be advised 180 mg once every four weeks or 120 mg once every three weeks.

Note:

If despite the maximum dose, the clinical and biochemical response is inadequate, combination therapy with pegvisomant or a dopamine agonist like cabergoline may be used.

Lanreotide Dose in the treatment of Carcinoid syndrome:

• 120 mg subQ once every four weeks
• Additional doses should not be administered if the patient is already receiving lanreotide for GEP-NETs (Gastroenteropancreatic-neuroendocrine tumours)

GEP-NETs ((Gastroenteropancreatic-neuroendocrine tumors):

• 120 mg SubQ once every 4 weeks until toxicity occurs or the disease progresses.

Use in children:

Children aged 16 years or more: Refer to adult dosing.

Pregnancy Risk Category: C

• Limited data are available on the pregnancy effects of lanreotide.
• For the treatment of acromegaly or worsening symptoms like headaches, alternative agents may be used during pregnancy.
• Because of the possible misinterpretation of maternal serum levels of IGF-1 and growth hormone, they are not recommended for routine use.
• Effective contraception is advised for women who are pregnant.
• Normalization of growth hormones with therapy can restore fertility, leading to an unplanned pregnancy.
• The Endocrine Society recommends that long-acting somatostatin analogues be stopped at least two months before a planned pregnancy
• Short-term somatostatin analogues can be used in these cases.

Lanreotide use during breastfeeding:

• It is unknown if the drug will be excreted into breast milk.
• Due to potential side effects on babies, it is not advised to breastfeed during therapy or for at least six months following the final dose (bradycardia, altered glucose metabolism).

Lanreotide (Somatuiline) dose in Renal impairment:

• Acromegaly:

  • CrCl ≥60 mL/minute:

    • Adjustment in the dose is not necessary.

  • CrCl <60 mL/minute:

    • 60 mg subQ initially once every 4 weeks for three months.
    • Then, based on the clinical and biochemical response, the dose is modified (growth hormone and insulin-like growth factor-1 levels).
    • Exercise caution when using 120 mg once every 6 to 8 weeks in extended-release formulations.

• Carcinoid syndrome or gastroenteropancreatic neuroendocrine tumours (GEP-NETs):

  • CrCl ≥30 mL/minute:

    • The manufacturer has not recommended any adjustments in the dose, however, the total clearance of the drug is least likely to be affected.

  • CrCl <30 mL/minute:

    • The manufacturer has not recommended any adjustments in the dose as it has not been studied in these patients.

Lanreotide (Somatuiline) dose in Liver disease:

• Acromegaly:

  • Mild impairment (Child-Pugh class A):

    • Adjustment in the dose is not necessary.

  • Moderate to severe impairment (Child-Pugh classes B and C):

    • The initial dosage of 60 mg subQ, given every four weeks for three months.
    • The dose is then adjusted based on the clinical and biochemical response (growth hormone levels and IGF-1 levels.
    • The use of extended-interval formulations every 6 - 8 weeks should be done with caution.

• Carcinoid syndrome or gastroenteropancreatic neuroendocrine tumours (GEP-NETs):

  • It has not been studied in patients with GEP-NETs.
  • The manufacturer has not recommended any adjustments in the dose in these patients.

Common Side Effects of Lanreotide (Somatuiline):

• Cardiovascular:

  • Bradycardia
  • Hypertension

• Central Nervous System:

  • Headache

• Dermatologic:

  • Injection Site Pruritus
  • Rash At Injection Site

• Endocrine & Metabolic:

  • Diabetes Mellitus
  • Hyperglycemia
  • Hypoglycemia
  • Weight Loss

• Gastrointestinal:

  • Diarrhea
  • Abdominal Pain
  • Cholelithiasis
  • Vomiting
  • Flatulence
  • Nausea

• Hematologic & Oncologic:

  • Anemia

• Hepatic:

  • Gallbladder Sludge

• Immunologic:

  • Antibody Development

• Local:

  • Inflammation At the Injection Site
  • Injection Site Reaction
  • Pain At the Injection Site
  • Residual Mass At Injection Site
  • Induration At the Injection Site
  • Injection Site Nodule
  • Bleeding At the Injection Site
  • Discomfort At the Injection Site
  • Hematoma At Injection Site
  • Injection Site Extravasation
  • Injection Site Granuloma
  • Swelling At the Injection Site

• Neuromuscular & Skeletal:

  • Musculoskeletal Pain

Less Common Side Effects of Lanreotide (Somatuiline):

• Cardiovascular:

  • Sinus bradycardia

• Central nervous system:

  • Dizziness
  • Depression

• Gastrointestinal:

  • Loose stools
  • Constipation

• Neuromuscular & skeletal:

  • Arthralgia
  • Muscle spasm

• Respiratory:

  • Dyspnea

Contraindication to Lanreotide (Somatuiline):

• You may have severe allergic reactions to any ingredient of the drug.
• Allergies to somatostatin and related peptides
• Biliary tract and complicated gallbladder stones

Warnings and precautions

• Cholelithiasis

  • Gallbladder disease may manifest as gall stones, gall stones, cholecystitis or cholangitis. It can also cause gallbladder dysfunction.
  • It is necessary to monitor the situation periodically.
  • Gallbladder disease patients should stop taking medication and be treated appropriately.

• Gastrointestinal effects:

  • It is possible to experience abdominal pain and diarrhea, which can affect the intestinal absorption of concomitant medication.

• Effect on blood glucose:

  • Hyperglycemia or hypoglycemia can occur due to insulin secretion and glucagon secretion.
  • At treatment initiation and during dose adjustments, it is important to monitor blood glucose.
  • After treatment initiation, dose adjustment and dosage adjustments, diabetic patients may require dose adjustments to their anti-diabetic medication.

• Hypersensitivity

  • The treatment may cause severe hypersensitivity reactions, such as anaphylaxis or angioedema. Allergy reactions should be closely monitored.

• Thyroid disorders:

  • Therapy has been successful in reducing thyroid function abnormalities, but it is uncommon for clinically significant hypothyroidism.
  • If clinically indicated, thyroid function tests should always be performed.

• Cardiac disorders:

  • Patients with preexisting heart conditions and patients on heart rate-reducing medications for treatment-associated bradycardia or hypertension should not use it.
  • Bradycardia, a decrease in heart rate, may also occur in patients with no pre-existing heart disease.
  • Patients with heart disease should have their heart rate monitored. If symptomatic bradycardia develops, the appropriate treatment should be started.

• Hepatic impairment

  • The drug should not be used in patients suffering from acromegalic hepatic impairment.
  • Patients with elevated systemic exposure should receive lower doses of treatment.
  • Patients with neuroendocrine tumours and hepatic impairment have not had lanreotide studied.

• Renal impairment

  • Patients with severe or moderate renal impairment should be treated with caution and in lower doses at first.

Monitor:

• Monitor the serum growth hormone and insulin-like growth factor 1 levels at baseline and at three months after treatment initiation in patients with acromegaly.
• When switching to the extended-interval dosing, growth hormone levels should be measured after 6 weeks of therapy.
• Monitor blood glucose periodically. Diabetic patients should have their glycemic control assessed frequently and the dose should be adjusted periodically and especially following dose adjustment.
• Monitor thyroid function as clinically indicated
• Heart rate
• Monitor for gallbladder disease. Routine ultrasound is not necessary, however, if the patient develops right hypochondria symptoms should be assessed with hepatobiliary functions and an ultrasound scan.

How to administer Lanreotide (Somatuiline)?

• It is intended for subQ use only.
• Avoid other methods of administration (such as intravenous, intradermal, and intramuscular administration).
• The sealed pouch is removed from the refrigerator at least 30 minutes prior to administration and allowed to reach room temperature.
• While it is kept at room temperature, the seal should not be removed until just prior to administration.
• It is administered into the superior outer quadrant of the buttock as a deep subQ injection. The site of the injection should be rotated between alternate buttocks.

Mechanism of action of Lanreotide (Somatuiline):

• Lanreotide, a synthetic analogue to the natural somatostatin, reduces the production of insulin-like growth factors and growth hormones.
• It reduces the production of multiple endocrine and neuroendocrine peptides, hormones, and exocrine metabolically activated peptides.
• It has a stronger affinity for somatostatin types 2 (SSTR2), and 5 (SSTR5) receptors.
• These receptors are primarily located in the pituitary (especially the growth hormone secreting tumors of pituitary) and the pancreas. It is less attracted to somatostatin receptors 1, 3 and 4.

It is bioavailable at a rate of69% to 78%, and the half-life elimination Between 23 and 30 days Time to get there peak plasma concentration It takes between 7 and 12 hours. Excretion: Urine (5% unchanged drug); feces 0.5% unchanged drug

International Brands of Lanreotide:

• Somatuline Depot
• Ipstyl
• Somatuiline
• Somatulin
• Somatulina
• Somatuline
• Somatuline Autogel
• Somatuline Depot
• Somatuline LA
• Somatuline LP
• Somatuline

Lanreotide Brand Names in Pakistan:

No Brands Available in Pakistan.