Paltusotine is a somatostatin receptor agonist used to treat acromegaly in adults whose surgery is not an option or has not been effective. Paltusotine is a selective somatostatin receptor agonist: It mimics the biological actions of endogenous somatostatin, which activates the somatostatin 2 receptor (SST2) to block the secretion of growth hormone (GH) and decreases the production of...
- Mechanism
- Curator reviewed · 5 references
Acromegaly is a hormonal disorder associated with excessive secretion of growth hormone (GH) and subsequent increase in the production of insulin-like growth factor I (IGF-I). Similar to the natural hormone somatostatin, paltusotine suppresses GH and IGF-1 secretion. Paltusotine exerts its pharmacological activity via selective agonism (>4000-fold) at somatostatin receptor 2 (SSTR2) and exhibits little or no affinity for other SST receptor subtypes. Paltusotine inhibited cyclic adenosine monophosphate accumulation via human SSTR2 activation with an average drug (agonist) concentration that results in half-maximal response (EC50) of 0.25 nM.
- Primary indication
- Paltusotine is indicated for the treatment of adults with acromegaly who had an inadequate response to surgery and/or for whom surgery is not an option.Curator reviewed · 1 structured indication
- Formula / weight
- C27H22F2N4O · 456.497 g/mol (avg)
- First approval
- United States, 2025
- Code names
- CRN-00808
- Brand names
Resolves to
GHILNKWBALQPDP-UHFFFAOYSA-NSMILESNC1CCN(CC1)C1=C(C=NC2=CC=C(C=C12)C1=C(O)C(=CC=C1)C#N)C1=CC(F)=CC(F)=C1What you can answer from here — as of September 12, 2026
Which drugs share a target with Paltusotine, and which of those have an active Phase 3 trial?
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