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lurbinectedin (Zepzelca)
Indications:
- metastatic small cell lung cancer with disease progression on or after platinum-based chemotherapy
Dosage:
- 3.2 mg/m2 every 21 days, intravenous infusion over 60 minutes
- consider premedication with glucocorticoid & serotonin antagonist
4 mg injection
Pharmacokinetics:
- volume of distribution - 504 L
- terminal 1/2life is 51 hours
- plasma clearance of lurbinectedin is 11 L/h (50%)
- metabolized by CYP3A4, in vitro
- 89% recovered in feces (< 0.2% unchanged); 6% in urine (1% unchanged)
Adverse effects:
- leukopenia, lymphopenia, anemia, neutropenia, thrombocytopenia
- increased serum creatinine, hyperglycemia, hyponatremia, hypomagnesemia
- nausea/vomiting, constipation, diarrhea fatigue
- decreased appetite, musculoskeletal pain
- dyspnea, cough
- hepatotoxicity: increased serum transaminases, decreased serum albumin
* effect on ECG QTc < 20 msec
Drug interactions:
- strong or moderate CYP3A inhibitors: avoid coadministration
- strong or moderate CYP3A inducers: avoid coadministration
Mechanism of action:
- alkylating agent
- binds guanine residues in the minor groove of DNA bending DNA helix towards the major groove
- affects activity of DNA binding proteins, including some transcription factors, & DNA repair pathways
- perturbs cell cycle, causes eventual cell death
- inhibits human monocyte activity in vitro Lurbinectedin inhibited human monocyte activity in vitr
Interactions
drug adverse effects of alkylating agents
General
alkylating agent
Database Correlations
PUBCHEM correlations
References
- Highlights of Prescribing Information
Zepzelca (lurbinectedin) for injection, for intravenous use
https://pp.jazzpharma.com/pi/zepzelca.en.USPI.pdf