Paltusotine
PALSONIFY
What it isAn oral, once-daily nonpeptide somatostatin-receptor-2 agonist for acromegaly.
Why this oneIt is the first oral nonpeptide somatostatin agonist, avoiding depot injections for suitable patients.
What limits itAbsorption is finicky — it is taken fasting — and bradycardia, hyperglycemia, GI effects, and gallstones can limit use; monitor biochemical control.
FDA-approved for
- acromegaly (2025)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acromegaly (see flags) | Adults | 40 mg QD (may temporarily reduce to 20 mg QD for tolerability, then resume 40 mg) | 60 mg QD if needed per IGF-1 after 2–4 wk | 60 mg QD |
Titration Wait 2–4 weeks on 40 mg QD before increasing to 60 mg QD, based on IGF-1 levels
Renal Undefined
Hepatic No adjustment needed
CYP3A4 inducers may require higher paltusotine dose: strong — up to 3× prior dose; moderate — up to 2× prior dose; cap 120 mg/day either way. PPI users may need a higher dose; avoid PPIs in patients already on 60 mg
Instructions
- Take once daily with water on an empty stomach — at least 6 h after a meal (e.g., after overnight fast) and at least 1 h before the next meal
Cautions
- Cholelithiasis and complications (cholecystitis, pancreatitis) — monitor periodically; discontinue if complications occur
- Hyperglycemia and hypoglycemia — monitor glucose at initiation and dose changes; adjust antidiabetics
- Bradycardia, sinus arrest, AV block, PR prolongation — may need dose adjustment of concomitant bradycardic drugs (e.g., beta-blockers)
- Hypothyroidism — periodic thyroid function tests
- Steatorrhea/fat malabsorption — evaluate for pancreatic exocrine insufficiency if new or worsening
- Vitamin B12 deficiency — monitor levels if indicated
Adverse reactions
- ≥5%: diarrhea, abdominal pain, nausea, decreased appetite, sinus bradycardia, hyperglycemia, palpitations, gastroenteritis
Pregnancy Insufficient human data; no malformations in animals at 3–11× human exposure at MRHD 60 mg QD
Lactation No human data; present in animal milk (2.4–3.8× plasma in rats), likely present in human milk; weigh benefit vs risk
NO BOXED WARNINGS
Classes and tags
Clinical profile
Mechanism of action: Paltusotine ballicule
