Paltusotine

Brand Names: Palsonify

Drug Class: General Prescription

Overview

11 DESCRIPTION PALSONIFY tablets contain paltusotine hydrochloride, a somatostatin receptor agonist. Paltusotine is known chemically as 3-[4-(4-Amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxybenzonitrile hydrochloride. The molecular weight of paltusotine hydrochloride is 492.95 g/mol (C 27 H 22 F 2 N 4 O·HCl).

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Similar to the natural hormone somatostatin, paltusotine suppresses growth hormone (GH) and insulin-like growth factor-1 (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 (EC 50 ) of 0.25 nM. 12.2 Pharmacodynamics In patients with acromegaly, there was a dose-dependent reduction in IGF-1 levels over the therapeutic dose range of 20 to 60 mg.

Indications

  • 1 INDICATIONS AND USAGE PALSONIFY 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. PALSONIFY is a somatostatin receptor agonist indicated for the treatment of adults with acromegaly who had an inadequate response to surgery and/or for whom surgery is not an option ( 1 ).

Common Doses

  • 40 mg
  • 20 mg
  • 60 mg
  • 120 mg

Dosage

2 DOSAGE AND ADMINISTRATION Take orally once daily with water on an empty stomach (at least 6 hours after a meal) and at least 1 hour before the next meal ( 2.1 ). Recommended initial dosage is 40 mg once daily. During initiation, PALSONIFY may be temporarily reduced to 20 mg once daily if needed, based on tolerability. Once adverse reactions have resolved, resume PALSONIFY 40 mg once daily ( 2.2 ). After 2 to 4 weeks, based on IGF-1 levels, titrate to 60 mg once daily ( 2.2 ). 2.

Contraindications

  • 4 CONTRAINDICATIONS None. None ( 4 )

Side Effects

  • 6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Cholelithiasis and Complications of Cholelithiasis [see Warnings and Precautions ( 5.1 )] Hyperglycemia and Hypoglycemia [see Warnings and Precautions ( 5.2 )] Cardiovascular Abnormalities [see Warnings and Precautions ( 5.3 )] Thyroid Function Abnormalities [see Warnings and Precautions ( 5.4 )] Steatorrhea and Malabsorption of Dietary Fats [see Warnings and Precautions ( 5.5 )] Changes in Vitamin B 12 Levels [see Warnings and Precautions ( 5.

Interactions

  • 7 DRUG INTERACTIONS Strong CYP3A4 Inducers: may decrease paltusotine exposure. May require PALSONIFY dosage increase ( 2.3 , 7.1 ). Moderate CYP3A4 Inducers: may decrease paltusotine exposure. May require PALSONIFY dosage increase ( 2.3 , 7.1 ). Proton Pump Inhibitors: may decrease paltusotine exposure. May require PALSONIFY dosage increase ( 2.3 , 7.1 ) Cyclosporine: may decrease cyclosporine exposure. May require cyclosporine dosage adjustment ( 7.2 ). 7.1 Effect of Other Drugs on PALSONIFY Table 3.