There are 3 main medical therapy classes for the treatment of acromegaly:
Acromegaly is characterized by excessive GH production by the pituitary gland, resulting in excessive tissue growth and dysfunction across multiple systems, including the metabolic, musculoskeletal, neurologic, cardiovascular, and pulmonary systems.
Somatostatin is a polypeptide hormone that inhibits hormone release, cell growth, and differentiation through binding to its 5 distinct receptors (SSTR).
Somatostatin receptor ligands or somatostatin analogs are synthetic molecules that bind to the same receptors as somatostatin. By inhibiting GH secretion, they reduce the production of insulin-like growth factor 1 (IGF-1) by liver cells. These agents are considered the primary medical therapy for acromegaly.
Octreotide is a synthetic octapeptide somatostatin analog that mimics natural somatostatin. By binding to SSTR2, it suppresses GH secretion and IGF-1 production.
Sandostatin is an injectable octreotide acetate indicated for patients with acromegaly with an inadequate response to or who are ineligible for surgical resection, pituitary irradiation, or bromocriptine mesylate at maximally tolerated doses. It was approved by the US Food and Drug Administration (FDA) in 1988. A long-acting release (LAR) formulation, Sandostatin® LAR Depot, may be used as an adjunct to surgery and radiotherapy.
Mycapssa is the first oral octreotide capsule, approved by the FDA in 2020 for the long term treatment of patients with acromegaly who previously responded to and tolerated injectable octreotide or lanreotide.
Somatuline Depot is an octapeptide analog of natural somatostatin that suppresses GH and IGF-1 production. Approved by the FDA in 2007, it is administered subcutaneously for the long term treatment of patients with acromegaly with an inadequate response to or who are unable to undergo surgery and/or radiotherapy.
Signifor is a somatostatin analog that binds to SSTR1, 2, 3, and 5, with the highest affinity for SSTR5. It potently suppresses GH, IGF-1, and adrenocorticotropic hormone secretion. A long-acting intramuscular injection formulation, Signifor® LAR, was approved by the FDA in 2012 for patients with acromegaly with an inadequate response to or who are not candidates for surgery.
Paltusotine (formerly CRN00808) is a nonpeptide selective agonist of SSTR2. It suppresses GH and IGF-1 levels and is designed for efficient intestinal absorption without the need for absorption enhancers. Developed by Crinetics, this first-in-class oral, once-daily treatment was approved by the FDA in 2025 under the brand name Palsonify™.
In patients with acromegaly who do not respond to somatostatin receptor ligands, GH receptor antagonists may be used. These agents bind to GH receptors on liver cells and inhibit the generation of peripheral IGF-1.
Somavert selectively binds to GH receptors, blocking endogenous GH binding and reducing IGF-1 levels and other GH-responsive serum proteins. It is administered subcutaneously and was approved by the FDA in 2003 for adults with acromegaly who do not respond adequately to or are not candidates for surgery or radiation.
Dopamine agonists bind to the dopamine D2 receptor and suppress GH secretion, though their clinical effectiveness in acromegaly is limited.
Bromocriptine inhibits GH release through tuberoinfundibular pathways, lowering circulating GH levels. Approved by the FDA in 1984 under the brand name Parlodel, it is available as an oral capsule and may be used as monotherapy or as an adjuvant to pituitary irradiation or surgery.
Dostinex is another dopamine agonist used off-label to treat acromegaly as monotherapy or add-on therapy to a somatostatin receptor ligand or Somavert to normalize IGF-1 levels.
Several novel therapies are being investigated for their efficacy in acromegaly, including CAM2028, a once-monthly subcutaneous self-administered octreotide formulation. Other experimental approaches involve the development of new somatostatin receptor ligands and formulations, as well as antisense oligonucleotides.
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Written by Özge Özkaya, MSc, PhD. Reviewed by Harshi Dhingra, MD, on 10/4/2025.
Özge’s background is in research; she holds a MSc. in Molecular Genetics from the University of Leicester and a PhD. in Developmental Biology from the University of London. Özge worked as a bench scientist for six years in the field of neuroscience before embarking on a career in science communication. She worked as the research communication officer at MDUK, a UK-based charity that supports people living with muscle-wasting conditions, and then a research columnist and the managing editor of resource pages at BioNews Services before joining Rare Disease Advisor.
