lanreotide

Action and Spectrum

Lanreotide is a somatostatin analogue that primarily works by activating somatostatin receptors, especially types 2 and 5. This action suppresses growth hormone release in the brain and, in tumors, triggers cell cycle arrest or apoptosis. It also reduces the production of growth-promoting substances and angiogenesis, contributing to its anti-tumor effects. 

Drug Interaction

Adverse Reaction

Frequency defined: 

>10%: 

Bradycardia 

Headache 

Rash at injection site 

Weight loss 

Diarrhea 

Abdominal pain 

Vomiting 

Nausea 

Flatulence 

Anemia 

Gallbladder sludge 

Muscle pain  

1%-10% 

Sinus bradycardia 

Dizziness 

Loose stools 

Constipation 

Arthralgia 

Muscle spasm 

Dyspnea   

<1%: 

Abscess at the injection site 

Anaphylaxis 

Mitral valve insufficiency 

Steatorrhea 

Black Box Warning

There is no blackbox warnings 

Contraindication / Caution

Contraindication/Caution 

Contraindication 

Hypersensitivity 

Cautions 

Use lanreotide with caution due to several potential risks. It may reduce gallbladder motility, increasing the chance of gallstone formation and related complications such as cholecystitis or pancreatitis. The drug can inhibit insulin and glucagon secretion, affecting glucose control and leading to hyper- or hypoglycemia—regular monitoring and dose adjustments of antidiabetic medications are advised. Decreased thyroid function and gastrointestinal issues like steatorrhea and malabsorption may also occur. Lanreotide may affect the absorption and bioavailability of other drugs, such as cyclosporine, necessitating dose adjustments.  

Pregnancy / Lactation

Pregnancy consideration: insufficient information available regarding its effect on pregnancy to recommend its use.  

Lactation: excretion of lanreotide in breast milk is not known.  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology 

Lanreotide is a synthetic somatostatin analogue that mimics the action of natural somatostatin by inhibiting the release of various hormones such as growth hormone, thyroid-stimulating hormone (TSH), insulin, and glucagon. 

Pharmacokinetics 

Absorption 

Lanreotide is absorbed in two phases after subcutaneous injection. Initially, there is a rapid release of the unprecipitated drug, followed by a slow release from the injection site depot through passive diffusion. Absorption is not affected by body weight, gender, or dose. 

Distribution 

The estimated volume of distribution is 15.1 L. 

Metabolism 

Half-Life: 23-36 days 

Excretion: Urine (<5%); feces (<0.5%) 

Elimination/Excretion 

 Less than 5% of the drug is excreted in urine, and under 0.5% is eliminated unchanged in feces, indicating biliary excretion. 

Half-life: Approximately 22 days. 

Clearance: Estimated at 23.1 L/h.  

Pharmacodynamics 

Lanreotide works by suppressing cAMP and modulating ion currents like potassium and calcium, which causes membrane hyperpolarization and blocks calcium-dependent depolarization. It also exerts strong antiproliferative effects through both direct and indirect mechanisms. 

Adminstartion

Patient information leaflet  

Generic Name: Lanreotide 

Pronounced: LAN-ree-oh-tide 

Why do we use Lanreotide?  

Lanreotide is used to treat acromegaly and gastroenteropancreatic neuroendocrine tumors (GEP-NETs) that are unresectable, locally advanced, or metastatic, and are well- to moderately differentiated. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: Lanreotide 

Pronounced: lan-ree-tide 

Why do we use lanreotide? 

Lanreotide is a somatostatin analog class of antineoplastic drug. It is used to treat Cushing’s disease, acromegaly, and neuroendocrine tumor of the gastrointestinal tract or the pancreas.