• Respiratory and thoracic cancers

Zepzelca Generic Name & Formulations

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

Generic Availability


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


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

Zepzelca Dosage and Administration


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.


Not established.

Zepzelca Contraindications

Not Applicable

Zepzelca Boxed Warnings

Not Applicable

Zepzelca 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


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


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




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

Zepzelca 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