Generic
Pertuzumab
2 brands available in the market
At a glance
Pertuzumab is a HER2/neu receptor antagonist used in combination with Trastuzumab and docetaxel for the treatment of HER2-positive metastatic breast cancer and HER2-positive locally advanced, inflammatory, or early stage breast cancer.
Description
Pertuzumab is a recombinant humanized monoclonal antibody that targets the extracellular dimerization domain (Subdomain II) of the human epidermal growth factor receptor 2 protein (HER2). It blocks ligand-dependent heterodimerization of HER2 with other HER family members, including EGFR, HER3, and HER4, inhibiting MAP kinase and PI3K signaling pathways, resulting in cell growth arrest and apoptosis. It also mediates antibody-dependent cell-mediated cytotoxicity.
Indications
- HER2-positive metastatic breast cancer (no prior anti-HER2 therapy or chemotherapy for metastatic disease)
- HER2-positive locally advanced, inflammatory, or early stage breast cancer (neoadjuvant treatment)
Therapeutic class
Targeted Cancer Therapy
Pharmacological class
HER2/neu Receptor Antagonist (Monoclonal Antibody)
Pharmacology
Pertuzumab is a recombinant humanized monoclonal antibody that targets the extracellular dimerization domain (Subdomain II) of HER2. It blocks HER2 heterodimerization with other HER family members, inhibiting MAP kinase and PI3K signaling, leading to cell growth arrest and apoptosis. It also mediates antibody-dependent cell-mediated cytotoxicity.
Mechanism of action
Binds to the extracellular dimerization domain of HER2 to block HER2 signaling pathways.
Dosage
Adult Dose (Intravenous):
- Initial (loading) dose: 840 mg (60-minute infusion)
- Subsequent doses (every 3 weeks): 420 mg (30-60 minute infusion)
- Metastatic breast cancer: With Trastuzumab and Docetaxel every 3 weeks
- Neoadjuvant: With Trastuzumab and Docetaxel every 3 weeks for 3-6 cycles
Pediatric Dose: Safety and efficacy not established.
Administration
- Intravenous infusion only; do not administer as IV push or bolus
- Do not use with other drugs
- Administered by doctor or nurse; do not self-administer
Missed dose
If you miss a dose, consult your doctor.
Side effects
Common Side Effects (>30%):
- Diarrhea
- Alopecia
- Neutropenia
- Nausea
- Fatigue
- Rash
- Peripheral neuropathy
- Vomiting
- Thrombocytopenia
- Anemia
Precautions & warnings
- Left Ventricular Dysfunction: May cause CHF and decreased LVEF; monitor cardiac function before and during treatment; discontinue for clinically significant decrease
- Embryo-fetal Toxicity: May cause embryo-fetal death and birth defects; oligohydramnios, delayed renal development; use effective contraception
- Infusion-Related Reactions: Monitor for signs and symptoms; slow/interrupt infusion if significant reaction occurs
- Hypersensitivity/Anaphylaxis: Discontinue immediately if severe reaction occurs
- Anthracyclines: Avoid for up to 7 months after stopping Pertuzumab (cardiac dysfunction risk)
Contraindications
- Known hypersensitivity to pertuzumab or any of its excipients
Drug interactions
- Anthracyclines: Avoid anthracycline-based therapy for up to 7 months after stopping Pertuzumab; if used, monitor cardiac function carefully
Food interactions
It is not known whether it is safe to consume alcohol with Pertuzumab; consult your doctor.
Use in pregnancy
Use in Pregnancy: Pregnancy Category D; risk to the fetus; if pregnancy occurs during treatment or within 7 months of last dose, apprise of potential hazard.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Human IgG is excreted in human milk; unknown if Pertuzumab is excreted; decide whether to discontinue nursing or the drug.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
No dose adjustment required in elderly patients.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment required.
Hepatic Impairment: Limited information on use in liver disease; consult your doctor.
Overdose effects
No overdose information available; consult your doctor if overused.
Storage conditions
Store at 2-8°C in the refrigerator; keep in outer carton to protect from light; do not freeze.
Chemical structure
Pertuzumab