Drug intelligence / Profile preview

octreotide + cabergoline

Development stage
Unknown
Lead developer
Novartis
Modality
Peptides, Small Molecules
Administration
Subcutaneous, Intramuscular, Intravenous, Oral
01

Overview

Octreotide + cabergoline is a combination therapy used primarily in the management of acromegaly and certain pituitary tumors, particularly when monotherapy with either agent is insufficient. Octreotide is a synthetic peptide analog of somatostatin that binds to somatostatin receptors, inhibiting the secretion of growth hormone (GH) and other hormones. Cabergoline is an ergot-derived dopamine receptor agonist that acts mainly on dopamine D2 receptors to suppress prolactin secretion and can also reduce GH levels. The combination has been shown to improve biochemical control in patients with acromegaly who are inadequately controlled with monotherapy, as well as in cases of dopamine-agonist resistant macroprolactinoma[2][4][6]. This approach leverages complementary mechanisms—octreotide’s inhibition via somatostatin receptors and cabergoline’s suppression via dopamine D2 receptor agonism—to achieve better hormonal regulation.

02

Targets

DRD4 (Dopamine D4 Receptor)DRD1 (Dopamine D1 Receptor)SSTR1 (Somatostatin Receptor Type 1)SSTR5 (Somatostatin receptor 5)SSTR2 (Somatostatin receptor type 2)DRD3 (Dopamine receptor D3)SSTR4 (Somatostatin receptor 4)DRD2 (Dopamine D2 Receptor)SSTR3 (Somatostatin receptor 3)

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