Names and pronunciation
(pral′se′ti′nib) Gavreto
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Drug reference
(pral′se′ti′nib) Gavreto
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Func. class.: Antineoplastic Chem class.: RET kinase inhibitor
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ACTION: Inhibits wild-type RET, oncogenic RET fusions, and RET mutations; antitumor activity occurs in cells harboring oncogenic RET fusions or mutations
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USES: Treatment of non-small cell lung cancer (NSCLC), thyroid cancer
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CONTRAINDICATIONS: Hypersensitivity Precautions: Breastfeeding, children, chronic lung P disease, contraception requirements, growth inhibition, hepatic disease, hypertension, impaired wound healing, infertility, interstitial lung disease, male- mediated teratogenicity, pneumonitis, pregnancy, renal impairment, surgery, tumor lysis syndrome
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SIDE EFFECTS CNS: Fatigue GI: Constipation, diarrhea, xerostomia, increased LFTs, hepatotoxicity CV: Edema, hypertension META: Hypocalcaemia, hyponatremia, hyper-hypophosphatemia HEMA: Decreased HB, neutropenia, lym- phocytopenia, thrombocytopenia, hemor- rhage MS: MS pain GU: Increased serum creatinine, UTI RESP: Cough, pneumonia, pneumonitis MISC: Fever, sepsis
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INTERACTIONS Decrease: Pralsetinib effect—CYP3A4 inducers, depending if moderate or strong, monitor or alter dose Increase: Pralsetinib effect—Strong CYP3A4 Inhibitors, avoid using together NURSING CONSIDERATIONS
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DOSAGE AND ROUTES NSCLC/thyroid cancer Adult: PO 400 mg daily until disease progression/unacceptable toxicity.
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Available forms: Capsule 100 mg
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Administer: • On empty stomach ≥1 hr before or ≥2 hr after food • Store at room temperature
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Assess: • Lung cancer: Obtain RET gene fusion status, hepatitis B surface antigen (HB- sAg), hepatitis B core antibody (anti- HBc), total Ig or IgG before starting treat- ment, treatment may start before results • Bone marrow suppression: Moni- tor CBC with differential, platelets; ane- mia, lymphocytopenia, neutropenia, thrombocytopenia may occur • Bleeding/hemorrhage: Monitor for bleeding/hemorrhage, permanently dis- continue if severe • Hepatotoxicity: Monitor LFTs base- line, q2wk × 3 months, then monthly; if elevated dosage modification or discon- tinuation may be needed, evaluate RET gene status • Hypertension: Monitor B/P baseline, after 1 wk and monthly thereafter; do not use in uncontrolled hypertension • Interstitial lung disease/pulmo nary toxicity: Monitor for dyspnea, cough, fever, fatigue; withhold pralsetinib, evaluate for interstitial lung disease • Poor wound healing: Withhold ≥5 days before elective surgery; do not use ≥2 wk after major surgery and until after adequate wound healing. • Identify if propylene glycol is present in product used: monitor for toxicity if large amounts are present in the product (lactic acidosis, respiratory changes, sei- zures) • Pregnancy/breastfeeding: Obtain pregnancy testing before use in fe- males of reproductive potential, do not use in pregnancy or breastfeeding; nonhormonal contraceptive should be used during and for ≥2 wk after last dose; males should use contraception during and for ≥1 wk after last dose in those with partners of reproductive po- tential
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Evaluate: • Therapeutic response : decreasing tu- mor growth in lung cancer
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Patient and caregiver information: • To report immediately poor wound healing after surgery, increased trouble breathing, bloody sputum, other bleed- ing, cough, fever • Take 1 hr before or 2 hr after food; do not crush, chew, open capsule; take whole • Liver dysfunction: To report yellow skin/sclera, clay-colored stools, dark urine • If a dose is missed, take on the same day; resume the regular dosing next day; do not take another dose if vomiting oc- curs • Identify if pregnancy is planned or suspected, not to breastfeed, discuss needed contraception
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PHARMACOKINETICS Onset unknown, peak 2-4 hr, duration unknown, half-life 22 hr, protein binding 97%
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