Herceptin

HER2-overexpressing adjuvant breast cancer (as part of regimens containing doxorubicin, cyclophosphamide, and paclitaxel or docetaxel; with docetaxel and carboplatin; or as single agent following multi-modality anthracycline-based therapy); HER2-overexpressing metastatic breast cancer (with paclitaxel for first-line, or as single agent for ≥2 prior chemo regimens); HER2-overexpressing metastatic gastric or GEJ adenocarcinoma (with cisplatin and capecitabine or 5-FU, first-line)

Weekly: Initial 4 mg/kg IV over 90 min, then 2 mg/kg IV over 30 min weekly
Every 3 weeks: Initial 8 mg/kg IV over 90 min, then 6 mg/kg IV over 30-90 min q3w
Adjuvant treatment: 52 weeks total (sequential or concurrent with chemo)

For injection: 150 mg lyophilized powder in single-dose vial; 420 mg multi-dose vial

Refer to the complete prescribing information for contraindications. Herceptin prescribing should account for patient-specific factors including hypersensitivity to the active ingredient or any excipients.

• Cardiomyopathy: Incidence of cardiac dysfunction 7-28% depending on regimen. Evaluate LVEF prior to and during treatment.
• Infusion Reactions: Fatal reactions reported; premedicate and monitor.
• Pulmonary Toxicity: Including dyspnea, interstitial pneumonitis, pulmonary infiltrates, ARDS.
• Exacerbation of Chemotherapy-Induced Neutropenia

Headache (26%), diarrhea (25%), nausea (23%), chills (22%), infusion reactions (21%), infection (20%), cough (15%), rash (14%)

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

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.

Trastuzumab is a recombinant humanized IgG1 monoclonal antibody that selectively binds to the extracellular domain of HER2 (ErbB2). It inhibits HER2-mediated signaling, mediates antibody-dependent cellular cytotoxicity (ADCC), and inhibits proliferation of tumor cells that overexpress HER2.

Half-life: dose-dependent; mean 28.5 days at maintenance doses. Vd: 44 mL/kg. Clearance: 5.15 mL/kg/day (decreased over time). Steady-state by ~20 weeks with weekly dosing, ~16 weeks with q3w. Mean washout time: ~7 months.

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

• H0648g — Trastuzumab + chemotherapy vs. chemotherapy alone in HER2+ metastatic breast cancer. Phase III, n=469.
  🔬 NCT00005970 ↗ 📄 Primary Publication ↗
• HERA — Trastuzumab after adjuvant chemotherapy in HER2+ early breast cancer. Phase III, n=5102.
  🔬 NCT00045032 ↗ 📄 Primary Publication ↗

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