Lutetium Lu 177 Dotatate (Mechanism of Action)

In this article, we will discuss Lutetium Lu 177 Dotatate (Mechanism of Action). So, let’s get started.

Mechanism of Action

Lutetium Lu 177 dotatate binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSRT2). Upon binding to somatostatin receptor expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized. The beta emission from Lu 177
induces cellular damage by formation of free radicals in somatostatin receptor-positive cells and in neighboring cells.

Pharmacodynamics

Lutetium Lu 177 exposure-response relationships and the time course of pharmacodynamics response are unknown.

Cardiac Electrophysiology
The ability of Lutetium Lu 177 dotatate to prolong the QTc interval at the therapeutic dose was assessed in an open label study in 20 patients with somatostatin receptor-positive midgut carcinoid tumors. No large changes in the mean QTc interval (i.e., >20 ms) were detected.

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