Doxil

Ovarian cancer — patients whose disease has progressed or recurred after platinum-based chemotherapy; AIDS-related Kaposi's sarcoma — after failure of prior systemic chemotherapy or intolerance; Multiple myeloma — in combination with bortezomib, in patients who have not previously received bortezomib and have received at least one prior therapy

Ovarian cancer: 50 mg/m² IV every 4 weeks at minimum
AIDS-related KS: 20 mg/m² IV every 3 weeks
Multiple myeloma (with bortezomib): 30 mg/m² IV on Day 4 following bortezomib (which is given at 1.3 mg/m² Days 1, 4, 8, 11) in a 21-day cycle
Initial infusion rate: 1 mg/min; if no reaction, increase to complete in 1 hour
NOT interchangeable with conventional doxorubicin

Injection: 2 mg/mL doxorubicin HCl in 10 mL (20 mg) and 25 mL (50 mg) single-dose vials

Nursing mothers. NOT substitutable with other doxorubicin formulations.

• Cardiotoxicity: Cumulative dose-related cardiomyopathy. Monitor LVEF. Risk increases with prior mediastinal radiation, prior/concurrent cyclophosphamide, cumulative dose >550 mg/m².
• Infusion Reactions: In up to 11%. Serious including back pain, flushing, tightness in chest/throat, dyspnea, hypotension. Slow infusion rate for initial dose.
• Hand-Foot Syndrome (PPE): Up to 50% in ovarian cancer. May be severe.
• Myelosuppression: Monitor CBCs including neutrophils, platelets frequently.
• Secondary Oral Neoplasms: Reported in long-term survivors.

PPE/hand-foot syndrome (50%), stomatitis (41%), nausea (37%), fatigue (23%), vomiting (21%), rash (22%), diarrhea (18%), constipation (13%), neutropenia (12%), anemia (6%)

Hand-foot syndrome (PPE) in 48-51% (Grade 3 in 17-20%). Dose-modify for Grade 2+ PPE. Cardiotoxicity risk increases with cumulative dose (max lifetime 550 mg/m² or less with prior anthracyclines).

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

Hand-foot syndrome (PPE) in 48-51% (Grade 3 in 17-20%). Dose-modify for Grade 2+ PPE. Cardiotoxicity risk increases with cumulative dose (max lifetime 550 mg/m² or less with prior anthracyclines).

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.

Doxil is a liposomal formulation of doxorubicin encapsulated in STEALTH liposomes (polyethylene glycol-coated). The PEG coating creates a protective layer that allows prolonged circulation time, and the small size (100 nm) enables accumulation in tumors through the enhanced permeability and retention (EPR) effect. Once internalized, doxorubicin intercalates DNA base pairs, inhibits topoisomerase II, and generates free radicals, leading to cell death.

Half-life: approximately 55 hours at 50 mg/m². Plasma clearance: 0.041 L/h. Vd: 2.7 L. PEGylated liposomal formulation reduces RES clearance. Mostly confined to vascular space. Metabolized via doxorubicinol formation.

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

• CAELYX/Doxil OC — PLD vs. topotecan in recurrent ovarian cancer. Phase III, n=474.
  🔬 NCT00003656 ↗ 📄 Primary Publication ↗

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