Vitrakvi Oral Solution

— THERAPEUTIC CATEGORIES —
  • Solid tumors
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Vitrakvi Oral Solution Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Larotrectinib 20mg/mL.

    Pharmacological Class

    Kinase inhibitor.

    See Also

    How Supplied

    Caps—60; Oral soln—2×50mL, 1×100mL

    Manufacturer

    Bayer Corporation

    Generic Availability

    NO

    Mechanism of Action

    Larotrectinib is an inhibitor of the tropomyosin receptor kinases (TRK), TRKA, TRKB, and TRKC. In in vitro and in vivo tumor models, larotrectinib demonstrated anti-tumor activity in cells with constitutive activation of TRK proteins resulting from gene fusions, deletion of a protein regulatory domain, or in cells with TRK protein overexpression. Larotrectinib had minimal activity in cell lines with point mutations in the TRKA kinase domain, including the clinically identified acquired resistance mutation, G595R. Point mutations in the TRKC kinase domain with clinically identified acquired resistance to larotrectinib include G623R, G696A, and F617L.

    Vitrakvi Oral Solution Indications

    Indications

    Solid tumors that have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have no satisfactory alternative treatments or that have progressed following treatment.

    Vitrakvi Oral Solution Dosage and Administration

    Adults and Children

    Confirm presence of a NTRK gene fusion in tumor specimens. Caps and oral soln are interchangeable. Swallow caps whole. Body surface area (BSA) <1.0m2: 100mg/m2 twice daily; BSA ≥1.0m2: 100mg twice daily. Both: continue until disease progression or unacceptable toxicity. Avoid concomitant strong CYP3A4 inhibitors, if unavoidable, reduce Vitrakvi dose by 50%. Avoid concomitant strong CYP3A4 inducers; if unavoidable, double Vitrakvi dose. Concomitant moderate CYP3A4 inducers: double Vitrakvi dose. Moderate to severe hepatic impairment: reduce initial dose by 50%. Dose modifications for adverse reactions: see full labeling.

    Vitrakvi Oral Solution Contraindications

    Not Applicable

    Vitrakvi Oral Solution Boxed Warnings

    Not Applicable

    Vitrakvi Oral Solution Warnings/Precautions

    Warnings/Precautions

    Risk of CNS effects (including cognitive impairment, mood disorders, dizziness, sleep disturbances), hepatotoxicity; withhold or permanently discontinue based on severity; adjust dose when resumed. Obtain LFTs prior to initiation, every 2 weeks during the first 2 months, then monthly thereafter, or more frequently following Grade ≥2 AST/ALT elevation. Evaluate if signs of potential skeletal fractures occur. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).

    Vitrakvi Oral Solution Pharmacokinetics

    Absorption

    Mean absolute bioavailability: 34%.

    Distribution

    Mean volume of distribution: 48 L. Plasma protein bound: 70%.

    Metabolism

    CYP3A4.

    Elimination

    Fecal (58%), renal (39%). Half-life: 2.9 hours. Mean clearance: 98 L/h.

    Vitrakvi Oral Solution Interactions

    Interactions

    Potentiated by strong CYP3A4 inhibitors (eg, itraconazole, grapefruit, or grapefruit juice); adjust dose (see Adults and Children). Potentiated by moderate CYP3A4 inhibitors; monitor more frequently and reduce dose based on severity of adverse reactions. Antagonized by strong or moderate CYP3A4 inducers (eg, rifampin, St. John's wort); adjust dose (see Adults and Children). Potentiates sensitive CYP3A4 substrates (eg, midazolam); if unavoidable, monitor for adverse reactions.

    Vitrakvi Oral Solution Adverse Reactions

    Adverse Reactions

    Increased AST/ALT, anemia, musculoskeletal pain, fatigue, hypoalbuminemia, neutropenia, increased alkaline phosphatase, cough, leukopenia, constipation, diarrhea, dizziness, hypocalcemia, nausea, vomiting, pyrexia, lymphopenia, abdominal pain.

    Vitrakvi Oral Solution Clinical Trials

    See Literature

    Vitrakvi Oral Solution Note

    Not Applicable

    Vitrakvi Oral Solution Patient Counseling

    See Literature

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