Palsonify

Drug overview for PALSONIFY (paltusotine hcl):

Generic name: PALTUSOTINE HCL (pal-TOO-soe-teen)
Drug class: Somatostatic Agents
Therapeutic class: Endocrine

Paltusotine is a somatostatin receptor agonist.

No enhanced Uses information available for this drug.

DRUG IMAGES

No Image Available

The following indications for PALSONIFY (paltusotine hcl) have been approved by the FDA:

Indications:
Acromegaly

Professional Synonyms:
Acromegalia
Marie's disease
Marie's syndrome

Dosing information for PALSONIFY
DRUG LABEL	DOSING TYPE	DOSING INSTRUCTIONS
PALSONIFY 20 MG TABLET	Maintenance	Adults take 2 tablets (40 mg) by oral route once daily
PALSONIFY 30 MG TABLET	Maintenance	Adults take 2 tablets (60 mg) by oral route once daily

The following drug interaction information is available for PALSONIFY (paltusotine hcl):

Contraindicated
Severe
Moderate

There are 0 contraindications.

There are 1 severe interactions. These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.

Drug Interaction	Drug Names
Gallium Ga 68 Dotatate; Gallium Ga 68 Dotatoc/Somatostatin analogs SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Both somatostatin analogs and gallium Ga 68 dotatate/ gallium Ga 68 dotatoc bind to the same somatostatin receptors, resulting in competitive inhibition.(1) CLINICAL EFFECTS: Concurrent use of gallium Ga 68 dotatate/ gallium Ga 68 dotatoc and somatostatin analogs may affect the results of the scan.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: In patients receiving somatostatin analogs, perform the image just prior to dosing with long-acting somatostatin analogs. Short acting somatostatin analogs can be used up to 24 hours before imaging with gallium Ga 68 dotatate or gallium Ga 68 dotatoc. (1) DISCUSSION: Both somatostatin analogs and gallium Ga 68 dotatate/ gallium Ga 68 dotatoc bind to the same somatostatin receptors, resulting in competitive inhibition, which can affect the results of the scan.(1)	GALLIUM GA-68 DOTATOC, NETSPOT

Drug Interaction

Drug Names

Gallium Ga 68 Dotatate; Gallium Ga 68 Dotatoc/Somatostatin analogs

SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.

MECHANISM OF ACTION: Both somatostatin analogs and gallium Ga 68 dotatate/ gallium Ga 68 dotatoc bind to the same somatostatin receptors, resulting in competitive inhibition.(1)

CLINICAL EFFECTS: Concurrent use of gallium Ga 68 dotatate/ gallium Ga 68 dotatoc and somatostatin analogs may affect the results of the scan.(1)

PREDISPOSING FACTORS: None determined.

PATIENT MANAGEMENT: In patients receiving somatostatin analogs, perform the image just prior to dosing with long-acting somatostatin analogs. Short acting somatostatin analogs can be used up to 24 hours before imaging with gallium Ga 68 dotatate or gallium Ga 68 dotatoc. (1)

DISCUSSION: Both somatostatin analogs and gallium Ga 68 dotatate/ gallium Ga 68 dotatoc bind to the same somatostatin receptors, resulting in competitive inhibition, which can affect the results of the scan.(1)

GALLIUM GA-68 DOTATOC, NETSPOT

There are 3 moderate interactions. The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.

Drug Interaction	Drug Names
Paltusotine/Strong CYP3A4 Inducers SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Strong CYP3A4 inducers may induce the metabolism of paltusotine.(1) CLINICAL EFFECTS: Concurrent or recent use of strong CYP3A4 inducers may alter the clinical effectiveness of paltusotine.(1) PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks. PATIENT MANAGEMENT: Patients taking strong CYP3A4 inducers may require an increased dosage of paltusotine.(1) The manufacturer of paltusotine states do not exceed three-fold the paltusotine dosage prior to concomitant use or 120 mg daily, whichever is less.(1) Monitor patients receiving concurrent therapy for reduced efficacy. DISCUSSION: Paltusotine is metabolized by CYP3A4.(1) In an interaction study, paltusotine concentration maximum (Cmax) and area-under-curve (AUC) decreased by 44% and 70%, respectively, following concomitant administration of carbamazepine (strong CYP3A inducer).(1) Strong CYP3A4 inducers linked to this monograph include: apalutamide, barbiturates, carbamazepine, encorafenib, enzalutamide, fosphenytoin, ivosidenib, lumacaftor, mitotane, phenobarbital, phenytoin, primidone, rifampin, rifapentine and St John's Wort.(2,3)	ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, BRAFTOVI, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTALBITAL, BUTALBITAL-ACETAMINOPHEN, BUTALBITAL-ACETAMINOPHEN-CAFFE, BUTALBITAL-ASPIRIN-CAFFEINE, CARBAMAZEPINE, CARBAMAZEPINE ER, CARBATROL, CEREBYX, DILANTIN, DILANTIN-125, DONNATAL, EQUETRO, ERLEADA, FIORICET, FOSPHENYTOIN SODIUM, LYSODREN, MITOTANE, MYSOLINE, ORKAMBI, PENTOBARBITAL SODIUM, PHENOBARBITAL, PHENOBARBITAL SODIUM, PHENOBARBITAL-BELLADONNA, PHENOBARBITAL-HYOSC-ATROP-SCOP, PHENOHYTRO, PHENYTEK, PHENYTOIN, PHENYTOIN SODIUM, PHENYTOIN SODIUM EXTENDED, PRIFTIN, PRIMIDONE, RIFADIN, RIFAMPIN, SEZABY, TEGRETOL, TEGRETOL XR, TENCON, TIBSOVO, XTANDI
Paltusotine/Moderate CYP3A4 Inducers SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Moderate CYP3A4 inducers may induce the metabolism of paltusotine.(1) CLINICAL EFFECTS: Concurrent or recent use of moderate CYP3A4 inducers may alter the clinical effectiveness of paltusotine.(1) PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks. PATIENT MANAGEMENT: Patients taking moderate CYP3A4 inducers may require an increased dosage of paltusotine.(1) The manufacturer of paltusotine states do not exceed two-fold the paltusotine dosage prior to concomitant use or 120 mg daily, whichever is less.(1) Monitor patients receiving concurrent therapy for reduced efficacy. DISCUSSION: Paltusotine is metabolized by CYP3A4.(1) Moderate CYP3A4 inducers such as efavirenz are predicted to decrease concentration maximum (Cmax) and area-under-curve (AUC) of paltusotine approximately 5% and 30%, respectively.(1) In an interaction study, paltusotine concentration maximum (Cmax) and area-under-curve (AUC) decreased by 44% and 70%, respectively, following concomitant administration of carbamazepine (strong CYP3A inducer).(1) Moderate inducers of CYP3A4 include: belzutifan, bosentan, cenobamate, dabrafenib, dipyrone, efavirenz, elagolix, etravirine, lesinurad, lorlatinib, mavacamten, mitapivat, modafinil, nafcillin, pacritinib, pexidartinib, repotrectinib, rifabutin, sotorasib, telotristat, thioridazine, and tovorafenib.(2,3)	AQVESME, AUGTYRO, BOSENTAN, CAMZYOS, EFAVIRENZ, EFAVIRENZ-EMTRIC-TENOFOV DISOP, EFAVIRENZ-LAMIVU-TENOFOV DISOP, ETRAVIRINE, INTELENCE, LORBRENA, LUMAKRAS, MODAFINIL, NAFCILLIN, NAFCILLIN SODIUM, OJEMDA, ORIAHNN, ORILISSA, PROVIGIL, PYRUKYND, RIFABUTIN, SYMFI, TAFINLAR, TALICIA, THIORIDAZINE HCL, THIORIDAZINE HYDROCHLORIDE, TRACLEER, TURALIO, VONJO, WELIREG, XCOPRI, XERMELO
Paltusotine (Less Than 60 mg)/Proton Pump Inhibitors SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: The aqueous solubility of paltusotine is pH dependent. Higher gastric pH leads to lower solubility which may reduce paltusotine absorption.(1) CLINICAL EFFECTS: Coadministration of proton pump inhibitors (PPIs) may reduce the bioavailability of paltusotine, leading to decreased systemic levels and effectiveness.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturer of paltusotine states that concomitant use of paltusotine with PPIs may require an increased dosage of paltusotine. Patients who are already on paltusotine 60 mg daily should avoid concomitant use with PPIs.(1) DISCUSSION: In an interaction study, paltusotine area-under-the-curve (AUC) was decreased by 21% with 20 mg dose and 42% with 60 mg dose levels.(1)	ACIPHEX, ACIPHEX SPRINKLE, DEXILANT, DEXLANSOPRAZOLE DR, ESOMEPRAZOLE MAGNESIUM, ESOMEPRAZOLE SODIUM, KONVOMEP, LANSOPRAZOL-AMOXICIL-CLARITHRO, LANSOPRAZOLE, NAPROXEN-ESOMEPRAZOLE MAG, NEXIUM, OMECLAMOX-PAK, OMEPRAZOLE, OMEPRAZOLE-SODIUM BICARBONATE, PANTOPRAZOLE SODIUM, PANTOPRAZOLE SODIUM-0.9% NACL, PREVACID, PRILOSEC, PROTONIX, PROTONIX IV, RABEPRAZOLE SODIUM, TALICIA, VOQUEZNA, VOQUEZNA DUAL PAK, VOQUEZNA TRIPLE PAK, YOSPRALA

Moderate List
Bradycardia
Diabetes mellitus
Exocrine pancreatic insufficiency
Hypothyroidism
Vitamin b12 deficiency

The following adverse reaction information is available for PALSONIFY (paltusotine hcl):

Overview
Severe
Less Severe

Adverse reaction overview.

Most common adverse reactions (>=5%) of paltusotine are diarrhea, abdominal pain, nausea, decreased appetite, sinus bradycardia, hyperglycemia, palpitations, and gastroenteritis.

There are 0 severe adverse reactions.

There are 10 less severe adverse reactions.

More Frequent	Less Frequent
Acute abdominal pain Diarrhea	Anorexia Biliary calculus Gastroenteritis Hyperglycemia Nausea Palpitations Sinus bradycardia

Rare/Very Rare
Vitamin b12 deficiency

The following precautions are available for PALSONIFY (paltusotine hcl):

Pediatric
Pregnant
Lactation
Geriatric

The safety and efficacy of paltusotine have not been established in pediatric patients.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

Data in pregnant patients are insufficient to determine whether paltusotine poses risks for birth defects or pregnancy loss. Animal studies in rats and rabbits showed no malformations at exposures up to 11- and 3-times the human exposure at the maximum recommended dose.

The presence of paltusotine in human milk and its effects on infants or milk production are unknown. Because paltusotine is found in animal milk at higher levels than in plasma, transfer into human milk is possible. The benefits of breastfeeding should be weighed against the mother's clinical need for paltusotine and any potential risks to the infant.

In phase 3 trials, 20.2% of paltusotine-treated patients were >=65 years of age. No safety or efficacy differences were observed between older and younger adults, and no age-based dose adjustments are needed.

Acromegaly
E22.0	Acromegaly and pituitary gigantism