Lanreotide: long acting somatostatin analogue as deep depot
Lanreotide (brand name Somatuline Autogel) is a synthetic octapeptide somatostatin analogue with markedly prolonged action compared with native somatostatin. Introduced in 1989, lanreotide is now an established treatment option in acromegaly and neuroendocrine tumours. It is characteristically available as a deep depot Autogel given subcutaneously once a month.
Compared with the related agent octreotide, lanreotide Autogel offers longer duration and easier administration through prefilled syringes that can also be used at home by trained patients or relatives.
Mechanism of action
Lanreotide selectively binds the somatostatin receptors SSTR2 and SSTR5 with high affinity. These receptors are present on numerous endocrine and neuroendocrine cells and on many tumour cells. Activation leads to:
- Inhibition of growth hormone secretion from the pituitary
- Reduction of plasma IGF 1 levels
- Inhibition of secretion of glucagon, insulin, gastrin, VIP and other gastrointestinal hormones
- Antiproliferative effect on neuroendocrine tumours expressing SSTR
- Splanchnic vasoconstriction (reduction of portal venous pressure)
The antitumour effect has two components: symptom control in hormone secreting tumours (carcinoid syndrome) and antiproliferative action with stabilisation of tumour growth.
Indications
- Acromegaly: in patients with insufficient control after surgery or radiotherapy or as bridging therapy
- Gastroenteropancreatic neuroendocrine tumours (GEP NET): symptom control in carcinoid syndrome (flushing, diarrhoea) and antiproliferative therapy in well to moderately differentiated tumours
- Pituitary tumours with TSH secretion (TSHoma): in selected cases
- Variceal bleeding in hepatic disease: off label, octreotide is more usual here
Dosing and administration
Acromegaly and GEP NET: 60, 90 or 120 mg subcutaneously every 4 weeks, individually titrated against IGF 1, growth hormone and clinical symptoms. With a progressive course the interval can be shortened to 14 days.
Administration: deep subcutaneous injection in the upper gluteal region. The prefilled syringe is brought to room temperature for about 30 minutes before use. After thorough skin disinfection inject perpendicularly into a skin fold.
After training patients or relatives can perform self injection at home. If there is uncertainty administration in the practice remains an option.
Treatment success: assessment via IGF 1 and growth hormone (acromegaly), tumour markers and clinical symptoms (NET). Imaging every 6 to 12 months.
Adverse effects
Very common: diarrhoea, soft stools, abdominal pain, nausea, cholelithiasis (gallstones, often asymptomatic), injection site reactions.
Common: hypoglycaemia or hyperglycaemia (because of simultaneous inhibition of glucagon and insulin), raised liver transaminases, pancreatitis, bradycardia, fatigue, rash.
Uncommon: gallstone complications with cholecystitis, glucose disorders, thyroid dysfunction, hair loss, allergic reactions.
Rare: acute pancreatitis, cardiomyopathy, severe allergic reactions.
Important points:
- Cholelithiasis is very common, mostly asymptomatic; ultrasound on symptoms
- Monitor glucose regularly, particularly in diabetes
- ECG check for bradycardia
- Injection site reactions are mostly mild and transient
Interactions
- Antidiabetics: changes in glucose metabolism, adjust insulin or oral antidiabetic doses
- Bradycardia inducing substances (beta blockers, calcium channel blockers, digoxin): additive bradycardia, caution
- Cyclosporin: reduced cyclosporin levels, adjustment as needed
- Bromocriptine: raised bromocriptine levels
Special considerations
Pregnancy: limited data, individual evaluation. Possible with clear indication and careful observation.
Breastfeeding: limited data, small amounts may pass into milk.
Diabetes mellitus: close glucose monitoring, since lanreotide can trigger both hyper and hypoglycaemia.
Cholelithiasis: ultrasound of the gallbladder at therapy start and on symptoms. Asymptomatic stones do not require treatment.
Thyroid function: already monitored regularly in acromegaly, also useful during therapy.
Follow up: after 3 to 6 months reassess efficacy via IGF 1, growth hormone, clinical symptoms and imaging. In NET also tumour markers (chromogranin A, 5 HIAA) and imaging.
Patient communication: the monthly injection requires a reliable routine. After training self injection at home is possible, improving comfort and adherence. Information about typical adverse events such as diarrhoea and gallstones supports disease management.
Related substances
- Octreotide, related somatostatin analogue
- Aflibercept, VEGF trap as ophthalmic and oncological therapy
- Regorafenib, multikinase inhibitor
- Sotorasib, KRAS G12C inhibitor
Frequently asked questions
Who is suitable for lanreotide?
Patients with acromegaly in whom adequate biochemical control was not achieved after surgery or radiotherapy. Also in gastroenteropancreatic neuroendocrine tumours (GEP NET) for symptom control and antiproliferative therapy. Expression of somatostatin receptors, demonstrable on imaging with octreoscan or DOTATATE PET CT, is required.
What is the difference from octreotide?
Both are somatostatin analogues with similar profiles. Lanreotide Autogel is given once monthly deep subcutaneously into the gluteal region, octreotide LAR intramuscularly. Lanreotide can be self administered at home after training, which is less common with octreotide.
Why do I often have diarrhoea?
Somatostatin analogues reduce gastrointestinal hormone secretion and affect motility and absorption. Diarrhoea and soft stools are common at the start and often improve over time. Dietary changes and possibly loperamide may relieve symptoms. Persistent severe diarrhoea needs medical evaluation.
Do I need to watch my gallbladder?
Yes. Somatostatin analogues reduce gallbladder motility, which can lead to gallstone formation. Ultrasound at therapy start and on symptoms is sensible. Asymptomatic stones generally do not require treatment; symptoms or complications may require cholecystectomy.
Sources
- EMA Somatuline Autogel (lanreotide) EPAR
- BfArM German Federal Institute for Drugs and Medical Devices
- AWMF guidelines acromegaly and neuroendocrine tumours
- Gelbe Liste lanreotide monograph
Legal notice and disclaimer
The information on this page is provided for general information only and does not constitute medical advice, diagnosis or treatment recommendation. It does not replace advice from a qualified physician or pharmacist. Medicines should only be used on prescription or after dispensing by a pharmacist. All information is based on the product information available at the time of writing and on recognised scientific sources; the manufacturer's current product information always prevails. Sanoliste assumes no liability for completeness, timeliness or accuracy of the information presented. In a medical emergency call the European emergency number 112.