Effect of octreotide LAR dose and weight on octreotide blood levels in patients with neuroendocrine tumors.

Objectives: Octreotide long acting repeatable (LAR) is widely used for the control of symptoms of functional neuroendocrine tumors. At doses of 30 mg/mo, up to 40% of patients require subcutaneous octreotide "rescue" and up to 40% of patients are given more than 30 mg of LAR/mo. Octreotide acetate binds to the sst2 receptor with an affinity (Kd) of approximately 1 x 10(-9) mol/L (approximately equal to 1000 pg/mL), but higher (approximately equal to 10,000 pg/mL) concentrations of octreotide are required to completely saturate this receptor.