Pharmacokinetic profile of Somatuline Depot (lanreotide) Injection
Therapeutic levels are achieved in 24 hours and maintained for 28 days10
Mean serum lanreotide concentration increases following a single dose of Somatuline® Depot (lanreotide) Injection10*
The steady-state values of Cmin, Cmax, and AUCt increase in a dose-dependent, linear manner10
Lanreotide has a high affinity for the somatostatin receptor subtypes (SSTR) 2 and 51,12
Clinical studies show similar potency and selectivity for SSTR 2 and SSTR 5 between lanreotide and octreotide.5
Activity at SSTR 2 and SSTR 5 is the primary mechanism believed responsible for GH inhibition.1
* From a phase II, randomized, double-blind study, during which 18 patients with acromegaly underwent a washout period of up to six weeks and then received Somatuline® Depot (lanreotide) Injection 60 mg, 90 mg, or 120 mg for four fixed injections at 28-day intervals. Chart adapted from Bronstein M, et al.10
Affinity measured as Ki (nM), where Ki is an inhibitory constant, a measure of affinity. The lower the number, the higher the affinity.
Indication and Important Safety Information
Somatuline® Depot (lanreotide) Injection is a somatostatin analog indicated for the long-term treatment of patients with acromegaly who have had an inadequate response to or cannot be treated with surgery and/or radiotherapy.
Lanreotide may reduce gallbladder motility and lead to gallstone formation. Periodic monitoring may be needed. Patients treated with Somatuline Depot may experience hypoglycemia or hyperglycemia. Glucose level monitoring is recommended and antidiabetic treatment adjusted accordingly. Lanreotide may lead to a decrease in heart rate. Use with caution in at-risk patients.
Patients with moderate and severe renal impairment or moderate and severe hepatic impairment should begin treatment with Somatuline Depot 60 mg.
There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human responses, Somatuline Depot should be used during pregnancy only if the potential benefit justifies risk to the fetus.
A decision should be made whether to discontinue nursing or discontinue the drug taking into account the importance of the drug to the mother.
Somatuline Depot may decrease the bioavailability of cyclosporine. Cyclosporine dose may need to be adjusted to maintain levels.
Patients receiving beta-blockers, calcium channel blockers, or other drugs that affect heart rate may need dose adjustments. Somatuline Depot may reduce the intestinal absorption of coadministered drugs. Caution should be used.
The most common adverse reactions (incidence >5%) are diarrhea (37%), cholelithiasis (20%), abdominal pain (19%), nausea (11%), injection-site reaction (9%), flatulence (7%), arthralgia (7%), and loose stools (6%).
For Full Prescribing Information, click here.
