Paltusotine

Paltusotine is a prescription medication indicated for the treatment of adults with acromegaly who had an inadequate response to surgery and/or for whom surgery is not an option.

• Paltusotine is available under the following different brand names: Palsonify

Common side effects of Paltusotine include:

• nausea
• diarrhea 
• abdominal pain 
• bradycardia
• hyperglycemia
• palpitations
• decreased appetite
• gastroenteritis

Serious side effects of Paltusotine include:

• cholelithiasis and its complications
• hyperglycemia and hypoglycemia
• cardiovascular abnormalities
• thyroid function abnormalities
• steatorrhea and malabsorption of dietary fats
• vitamin B12 deficiency

Rare side effects of Paltusotine include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 20 mg
• 30 mg

Acromegaly

Adult dosage

• Initial dose: 40 mg orally daily
• May temporarily reduce dose to 20 mg daily if needed during initiation period, based on tolerability; once adverse reactions are resolved, resume 40 mg daily
• After 2-4 weeks on 40 mg daily, based on IGF-1 levels, titrate to 60 mg daily

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

Drug interaction overview

• CYP3A4 substrate
• Strong CYP3A4 inducers
  • Modify dose
  • May require an increased paltusotine dose; not to exceed 3-fold dosage before concomitant use or 120 mg daily, whichever is less
• Moderate CYP3A4 inducers
  • Modify dose
  • May require an increased paltusotine dose; not to exceed 2-fold dosage before concomitant use or 120 mg daily, whichever is less
• Proton pump inhibitors (PPIs)
  • Avoid/modify dose
  • May require an increased paltusotine dose
  • Avoid coadministration of PPIs if already taking paltusotine 60 mg daily
• Cyclosporine
  • Modify dose
  • Coadministration may decrease cyclosporine bioavailability
  • May need to adjust cyclosporine dose to maintain therapeutic levels
  • Follow recommended therapeutic drug monitoring for cyclosporine

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Paltusotine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Paltusotine?”

Cautions

• Cholelithiasis
  • May inhibit gallbladder contractility and decrease bile secretion, which may lead to gallbladder stones or sludge
  • Cholelithiasis reported in clinical trials
  • Complications of cholelithiasis (e.g., acute cholecystitis, pancreatitis) have also been reported
  • Monitor patients periodically
  • Discontinue if complications of cholelithiasis occur and treat appropriately
• Hyperglycemia and hypoglycemia
  • May alter the balance between counter-regulatory hormones, insulin, glucagon, and growth hormone, which may result in hypoglycemia, hyperglycemia, or diabetes mellitus
  • Hyperglycemia reported in clinical trials
  • Monitor blood glucose levels when initiating or altering the dose of Paltusotine
  • Adjust antidiabetic treatment as needed
• Cardiovascular abnormalities
  • Cardiac conduction abnormalities and other ECG changes (e.g., PR interval prolongation) reported
  • Bradycardia, sinus arrest, and atrioventricular block reported in clinical trials
  • These ECG changes may occur in patients with acromegaly
  • Dosage adjustments of concomitantly used drugs that have bradycardia effects (e.g., beta-blockers) may be necessary
• Thyroid function abnormalities
  • Somatostatin analogs may suppress thyroid-stimulating hormone (TSH) secretion, which may result in hypothyroidism
  • Periodically assess thyroid function (TSH, total, and/or free T4) during treatment
• Steatorrhea and malabsorption of dietary fats
  • New onset steatorrhea, stool discoloration, and loose stools were reported in patients receiving somatostatin analogs
  • Somatostatin analogs reversibly inhibit the secretion of pancreatic enzymes and bile acids, which may result in malabsorption of dietary fats and subsequent symptoms of steatorrhea, loose stools, abdominal bloating, and weight loss
  • If new occurrences or worsening of these symptoms are reported, evaluate for potential pancreatic exocrine insufficiency and manage accordingly
• Vitamin B12 deficiency
  • Decreased vitamin B12 levels observed in patients treated with somatostatin analogs
  • Monitor vitamin B12 levels during treatment if clinically indicated

Pregnancy and Lactation

• Available data are insufficient to identify a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes
• Lactation
  • There is no information available on the presence of the drug in human milk, its effects on breastfed infants, or on milk production