Zepzelca

— THERAPEUTIC CATEGORIES —
  • Respiratory and thoracic cancers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Zepzelca Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Lurbinectedin 4mg; per vial; lyophilized pwd for IV infusion after reconstitution and dilution; preservative-free.

    Pharmacological Class

    Alkylating agent.

    How Supplied

    Single-dose vial—1

    Manufacturer

    Jazz Pharmaceuticals plc

    Generic Availability

    NO

    Mechanism of Action

    Lurbinectedin binds to guanine residues in the minor groove of DNA, forming adducts and resulting in a bending of the DNA helix towards the major groove. Adduct formation triggers a cascade of events that can affect the subsequent activity of DNA binding proteins, including some transcription factors, and DNA repair pathways, resulting in perturbation of the cell cycle and eventual cell death.

    Zepzelca Indications

    Indications

    Metastatic small cell lung cancer (SCLC) in adults with disease progression on or after platinum-based chemotherapy.

    Zepzelca Dosage and Administration

    Adult

    Consider premedication with corticosteroids, serontonin antagonists. Initiate only if ANC is ≥1500cells/mm3 and platelet count is ≥100000/mm3. Give by IV infusion over 60mins. 3.2mg/m2 every 21 days until disease progression or unacceptable toxicity. Concomitant strong CYP3A inhibitors, if unavoidable: reduce Zepzelca dose by 50%. Dose modifications for adverse reactions: see full labeling.

    Children

    Not established.

    Zepzelca Contraindications

    Not Applicable

    Zepzelca Boxed Warnings

    Not Applicable

    Zepzelca Warnings/Precautions

    Warnings/Precautions

    Risk of myelosuppression, hepatotoxicity, rhabdomyolysis. Monitor blood counts with neutrophils, platelets prior to initiation. If neutrophils <500cells/mm3 or any value less than LLN: give G-CSF. Monitor LFTs, creatinine phosphokinase prior to and during therapy as clinically indicated. Withhold, reduce dose, or permanently discontinue based on severity. Extravasation resulting in tissue necrosis; monitor during infusion. Discontinue immediately if extravasation occurs. Moderate or severe hepatic impairment. Elderly. Embryo-fetal toxicity. Advise to use effective contraception during and for 6 months (females of reproductive potential) or 4 months (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after the last dose).

    Zepzelca Pharmacokinetics

    Absorption

    Mean maximum plasma concentration: 107 μg/L. Mean AUC0-inf: 551 μg•h/L.

    Distribution

    Volume of distribution at steady-state: 504 L. Plasma protein bound: ~99% to both albumin and α-1-acid glycoprotein.

    Metabolism

    CYP3A4. 

    Elimination

    Fecal (89%), renal (6%). Half-life: 51 hours.

    Zepzelca Interactions

    Interactions

    Potentiated by strong or moderate CYP3A inhibitors (eg, grapefruit, Seville oranges); avoid concomitant use. If concomitant strong CYP3A inhibitors unavoidable; reduce Zepzelca dose (see Adult dose). If concomitant moderate CYP3A inhibitors unavoidable; consider Zepzelca dose reduction, if needed. Antagonized by strong CYP3A inducers; avoid concomitant use.

    Zepzelca Adverse Reactions

    Adverse Reactions

    Leukopenia, lymphopenia, fatigue, anemia, neutropenia, increased creatinine, increased alanine aminotransferase, increased glucose, thrombocytopenia, nausea, decreased appetite, musculoskeletal pain, decreased albumin, constipation, dyspnea, decreased sodium, increased aspartate aminotransferase, vomiting, cough, decreased magnesium, diarrhea.

    Zepzelca Clinical Trials

    See Literature

    Zepzelca Note

    Not Applicable

    Zepzelca Patient Counseling

    See Literature

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