• Symptomatic tenosynovial giant cell tumor associated with severe morbidity or functional limitations and not amenable to improvement with surgery.

Contraindicated in:

• Pre-existing liver enzyme elevations or active liver or biliary tract disease
• OB: Pregnancy (may cause fetal harm)
• Lactation: Lactation.

Use Cautiously in:

• Mild, moderate, or severe renal impairment (↓ dose)
• Moderate or severe hepatic impairment
• Rep: Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CNS: dysgeusia, amnesia, attention disturbances, confusion, memory impairment.

CV: hypertension, peripheral edema.

Derm: hair color changes, pruritus, rash, alopecia, skin pigmentation changes.

EENT: eye edema, blurred vision, diplopia, photophobia.

F and E: hypophosphatemia.

GI: HEPATOTOXICITY, constipation, vomiting, dry mouth, stomatitis.

GU: ↓fertility.

Hemat: NEUTROPENIA, anemia, lymphocytopenia, thrombocytopenia.

Metab: ↓appetite, hypercholesterolemia.

Neuro: peripheral neuropathy.

Misc: fatigue, fever.

Drug-Drug:

• Hepatotoxic drugs can ↑ risk of hepatotoxicity; avoid concurrent use.
• Strong CYP3A inhibitors may ↑ levels and risk of toxicity; avoid concurrent use; if concurrent use cannot be avoided, ↓ pexidartinib dose.
• Strong CYP3A inducers may ↓ levels and effectiveness; avoid concurrent use.
• UGT inhibitors may ↑ levels and risk of toxicity; avoid concurrent use; if concurrent use cannot be avoided, ↓ pexidartinib dose.
• Proton pump inhibitorsmay ↓ levels and effectiveness; avoid concurrent use; as alternative, administer pexidartinib 2 hr before or after taking an antacid or 2 hr before or 10 hr after taking an H₂ antagonist.

Drug-Natural Products:

• St. John's wort may ↓ levels and effectiveness; avoid concurrent use.

Drug-Food:

• Grapefruit or grapefruit juice may ↑ levels and risk of toxicity; if concurrent use cannot be avoided, ↓ pexidartinib dose.

• Capsules: 200 mg;

• PO (Adults): 400 mg twice daily until disease progression or unacceptable toxicity. Concurrent use of strong CYP3A inhibitor or UGT inhibitor — If originally taking pexidartinib 600 mg/day or 800 mg/day, ↓ dose to 200 mg twice daily; if originally taking pexidartinib 400 mg/day, ↓ dose to 200 mg once daily.

Turalio

• Acts as a tyrosine kinase inhibitor that selectively inhibits the colony-stimulating factor 1 receptor (CSF1R) which slows proliferation of tumor cells in the synovium.

• Reduction in tumor size and improvement in joint movement.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: High-fat food increases drug exposure by 100% and delays absorption.

Distribution: Extensively distributed to extravascular tissues.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized by CYP3A4 isoenzyme and through glucuronidation (via UGT1A4); inactive metabolite formed via glucuronidation. 65% excreted via feces (44% as unchanged drug), 27% excreted in urine as metabolites.

Half-life: 26.6 hr.

(plasma concentrations)

• Instruct patient to take pexidartinib on an empty stomach, as directed. If a dose is missed or patient vomits after dose, omit dose and take next dose at scheduled time. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• Inform patient of the Turalio REMS program and requirements.
• Caution patient to avoid grapefruit juice during therapy.
• Advise patient to take pexidartinib 2 hr before or 2 hr after antacids and at least 2 hr before or 10 hr after H₂antagonists.
• Advise patient to notify health care professional immediately if signs and symptoms of liver toxicity occur.
• Inform patient that pexidartinib may cause a change in hair color and a loss of taste or changes in the way things taste.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other Rx, OTC, herbal products, especially St. John's Wort.
• Rep: May be teratogenic. Advise women of reproductive potential to use effective nonhormonal contraception during and for 1 mo after last dose and to avoid breastfeeding during and for 1 wk after last dose. Advise males with female partners of reproductive potential to use effective nonhormonal contraception during and for 1 wk after last dose of pexidartinib. May impair male and female fertility.
• Emphasize the need for regular lab tests to monitor for side effects.

pex-i-DAR-ti-nib

NDC Code^*

• 65597- Daiichi Sankyo Inc.
  • 65597-402- Turalio
    • 65597-402-20- 1 BOTTLE in 1 CARTON (65597-402-20) > 120 CAPSULE in 1 BOTTLE

• 65597- Daiichi Sankyo Inc.
  • 65597-402- Turalio
    • 65597-402-28- 1 BOTTLE in 1 CARTON (65597-402-28) > 28 CAPSULE in 1 BOTTLE