HERCEPTIN
Herceptin is a HER2/neu receptor antagonist indicated for the treatment of adults with HER2-overexpressing breast cancer and metastatic gastric or gastroesophageal junction adenocarcinoma. In the adjuvant breast cancer setting, it is administered as part of multi-drug chemotherapy regimens or as a single agent following anthracycline-based therapy. For metastatic disease, the drug is used either as a single agent or in combination with specific chemotherapy agents such as paclitaxel, cisplatin, and fluoropyrimidines. Patient selection for all indications requires the use of an FDA-approved companion diagnostic to confirm HER2 overexpression.
How HERCEPTIN Works
Herceptin targets the HER2 proto-oncogene, which encodes a 185 kDa transmembrane receptor protein related to the epidermal growth factor receptor. By binding to this receptor, the drug inhibits the proliferation of human tumor cells that overexpress HER2. Additionally, Herceptin functions as a mediator of antibody-dependent cellular cytotoxicity (ADCC), a process that preferentially exerts its effects on cancer cells that overexpress HER2 compared to those that do not.
Details
- Status
- Prescription
- First Approved
- 1998-09-25
- Routes
- INTRAVENOUS
- Dosage Forms
- VIAL
HERCEPTIN Approval History
What HERCEPTIN Treats
3 indicationsHERCEPTIN is approved for 3 conditions since its original approval in 1998. These indications span multiple therapeutic areas including oncology, immunology, and more.
- HER2-overexpressing adjuvant breast cancer
- HER2-overexpressing metastatic breast cancer
- HER2-overexpressing metastatic gastric or gastroesophageal junction adenocarcinoma
HERCEPTIN Boxed Warning
CARDIOMYOPATHY, INFUSION REACTIONS, EMBRYO-FETAL TOXICITY, and PULMONARY TOXICITY WARNING: CARDIOMYOPATHY, INFUSION REACTIONS, EMBRYO-FETAL TOXICITY, and PULMONARY TOXICITY See full prescribing information for complete boxed warning Cardiomyopathy: Herceptin can result in subclinical and clinical cardiac failure manifesting as CHF, and decreased LVEF, with greatest risk when administered concurrently with anthracyclines. Evaluate cardiac function prior to and during treatment. Discontinue Hercep...
WARNING: CARDIOMYOPATHY, INFUSION REACTIONS, EMBRYO-FETAL TOXICITY, and PULMONARY TOXICITY WARNING: CARDIOMYOPATHY, INFUSION REACTIONS, EMBRYO-FETAL TOXICITY, and PULMONARY TOXICITY See full prescribing information for complete boxed warning Cardiomyopathy: Herceptin can result in subclinical and clinical cardiac failure manifesting as CHF, and decreased LVEF, with greatest risk when administered concurrently with anthracyclines. Evaluate cardiac function prior to and during treatment. Discontinue Herceptin for cardiomyopathy. ( 2.5 , 5.1 ) Infusion Reactions, Pulmonary Toxicity: Discontinue Herceptin for anaphylaxis, angioedema, interstitial pneumonitis, or acute respiratory distress syndrome. ( 5.2 , 5.4 ) Embryo-Fetal Toxicity: Exposure to Herceptin during pregnancy can result in oligohydramnios, in some cases complicated by pulmonary hypoplasia and neonatal death. Advise patients of these risks and the need for effective contraception. ( 5.3 , 8.1 , 8.3 ) Cardiomyopathy Herceptin administration can result in sub - clinical and clinical cardiac failure. The incidence and severity was highest in patients receiving Herceptin with anthracycline - containing chemotherapy regimens. Evaluate left ventricular function in all patients prior to and during treatment with Herceptin. Discontinue Herceptin treatment in patients receiving adjuvant therapy and withhold Herceptin in patients with metastatic disease for clinically significant decrease in left ventricular function [see Dosage and Administration (2.5) and Warnings and Precautions (5.1)] . Infusion Reactions; Pulmonary Toxicity Herceptin administration can result in serious and fatal infusion reactions and pulmonary toxicity. Symptoms usually occur during or within 24 hours of Herceptin administration. Interrupt Herceptin infusion for dyspnea or clinically significant hypotension. Monitor patients until symptoms completely resolve. Discontinue Herceptin for anaphylaxis, angioedema, interstitial pneumonitis, or acute
HERCEPTIN Target & Pathway
ProTarget
A receptor tyrosine kinase that promotes cell growth and division. Approximately 20% of breast cancers overexpress HER2, leading to aggressive tumor growth. Targeting HER2 blocks these growth signals and can trigger immune-mediated destruction of cancer cells.
Pathway Context
HER2 forms dimers with other HER family members to activate growth signaling
A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.
HERCEPTIN Biosimilars
6 FDA-approvedThese 6 alternatives require prescriber approval to substitute for HERCEPTIN.
What are biosimilars? Lower-cost alternatives to HERCEPTIN with no clinically meaningful differences.
Auto-substitute OK = FDA "interchangeable" designation — pharmacist can switch without calling the doctor.
HERCEPTIN Competitors
Pro10 other drugs also target HER2. Compare mechanisms, indications, and trial activity.
Competitors share the same molecular target (HER2). Earlier expiry dates signal biosimilar/generic opportunities.
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
HERCEPTIN FDA Label Details
ProIndications & Usage
FDA Label (PDF)Herceptin is a HER2/neu receptor antagonist indicated in adults for: The treatment of HER2-overexpressing breast cancer. The treatment of HER2-overexpressing metastatic gastric or gastroesophageal junction adenocarcinoma. Select patients for therapy based on an FDA-approved companion diagnostic for Herceptin . 1.1 Adjuvant Breast Cancer Herceptin is indicated in adults for adjuvant treatment of HER2 overexpressing node positive or node negative (ER/PR negative or with one high risk feature [see Clinical Studies ] ) breast cancer as part of a treatment regimen consisting of doxorubicin, cycloph...
WARNING: CARDIOMYOPATHY, INFUSION REACTIONS, EMBRYO-FETAL TOXICITY, and PULMONARY TOXICITY WARNING: CARDIOMYOPATHY, INFUSION REACTIONS, EMBRYO-FETAL TOXICITY, and PULMONARY TOXICITY See full prescribing information for complete boxed warning Cardiomyopathy: Herceptin can result in subclinical and cl...
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.