Lurbinectedin

Small cell lung cancer (SCLC) — metastatic, with disease progression on or after platinum-based chemotherapy

3.2 mg/m² IV every 21 days until disease progression or unacceptable toxicity
Infuse over 60 minutes via central venous catheter
Pre-medication: Antiemetics and corticosteroids before each infusion
Dose reduction: 2.6 mg/m², then 2.0 mg/m²

For injection: 4 mg lyophilized powder in single-dose vial

None listed.

• Myelosuppression: Neutropenia 46% (Grade 3-4: 28%), anemia 93% (Grade 3-4: 9%), thrombocytopenia 40% (Grade 3-4: 7%). Monitor CBC prior to each dose and periodically. Withhold for ANC <500 or platelets <100K.
• Hepatotoxicity: ALT elevation 35%, bilirubin elevation 10%. Monitor LFTs prior to each dose.
• Embryo-Fetal Toxicity

Fatigue (47%), nausea (37%), decreased appetite (28%), musculoskeletal pain (26%), constipation (24%), dyspnea (20%), vomiting (18%), cough (14%), diarrhea (11%), anemia (93%), neutropenia (46%), leukopenia (40%), thrombocytopenia (40%), creatinine increase (42%), ALT increase (35%)

Grade 3-4 myelosuppression: neutropenia (46%), anemia (9%), thrombocytopenia (7%). Febrile neutropenia in 5%. G-CSF recommended. Grade 3+ hepatotoxicity in 5%.

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Grade 3-4 myelosuppression: neutropenia (46%), anemia (9%), thrombocytopenia (7%). Febrile neutropenia in 5%. G-CSF recommended. Grade 3+ hepatotoxicity in 5%.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Lurbinectedin is a synthetic alkaloid analogue of trabectedin that covalently binds to the minor groove of DNA. It selectively inhibits oncogenic transcription by binding to CG-rich sequences near gene promoters, trapping RNA polymerase II complexes on DNA, and inducing their degradation. This leads to a cascade of events including DNA double-strand breaks and apoptosis. Lurbinectedin also modulates the tumor microenvironment by depleting tumor-associated macrophages.

Half-life: approximately 51 hours (terminal). Clearance: 17 L/h. Vd: 851 L (extensive tissue distribution). Protein binding: 99%. Metabolized primarily by CYP3A4. Excreted in feces (88%) and urine (6%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• PM1183-B-005-14 — Lurbinectedin in relapsed SCLC after platinum-based chemotherapy. Phase II, n=105.
  🔬 NCT02454972 ↗ 📄 Primary Publication ↗

Lurbinectedin has FDA-approved indications across the following cancer types covered on PipelineEvidence: