Signifor

Acromegaly is a rare, chronic disease characterized by hypersecretion of growth hormone (GH) from benign somatotrophic adenomas. Hypersecretion of GH, in turn, stimulates overproduction of insulin-like growth factor 1 (IGF-1) from the liver and systemic tissues.^1,2

The effects of increased levels of GH and IGF-1 on many organs result in the clinical manifestations of acromegaly that lead to a multisystem disease associated with physical disfigurement, comorbidities, and premature mortality. Patients with acromegaly may develop cardiovascular comorbidities such as hypertension and cardiomyopathy, insulin resistance, sleep apnea, and neoplasia such as colon polyps.¹

Classic signs and symptoms include prominent brow ridge, a widening of the space between the teeth, and soft-tissue changes. Patients may complain of excessive perspiration, soft-tissue swelling, large-joint osteoarthritis, and carpal tunnel syndrome.¹

Somatostatin receptors are expressed in many tissues including neuroendocrine tumors such as GH-secreting pituitary adenomas. There are 5 known human SST receptor subtypes: SST₁, SST₂, SST₃, SST₄, and SST₅. These receptor subtypes are expressed in different tissues under normal physiologic conditions. SST analogs bind to SST receptors with different potencies.³

SIGNIFOR LAR exerts its pharmacologic effect by binding to SST receptors. Of the 5 known human SST receptor subtypes, SIGNIFOR LAR binds with high affinity to four of the five. SIGNIFOR LAR binds with the highest affinity to SST₂ and SST₅ subtype receptors, which may be relevant for inhibition of GH secretion. In vivo studies show that SIGNIFOR LAR lowers GH and IGF-1 levels in patients with acromegaly.³

SIGNIFOR LAR for injectable suspension is administered by a trained healthcare professional, such as a physician or nurse, as an intramuscular injection into the right or left gluteal muscle. The long-acting formulation achieves 28 days of medication release with one injection, allowing SIGNIFOR LAR to be administered once every 4 weeks.³