Paltusotine

PALSONIFY

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Pronunciation: pal-TOO-soe-teen (pal-SAHN-i-fye)

Paltusotine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Paltusotine ballicule

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.

Paltusotine molecular structure (skeletal formula) — Molecular structure: Paltusotine

FDA-approved for

acromegaly (2025)

FDA label

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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

Available strengths

tab 20, 30 mg

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

Cost

Paltusotine (PALSONIFY)

Strength		#/mo	generic $/mo	CostPlus
20 mg	tab	30 qd		not offered
30 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Paltusotine is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskCholelithiasis; hyperglycemia or hypoglycemia

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryN/A (post-2015 labeling)

Defining liabilityGallstones, glycemic disturbance and cardiac conduction abnormalities

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