Last reviewed · How we verify
Trastuzumab and neratinib
Trastuzumab and neratinib together block HER2 signaling through complementary mechanisms: trastuzumab is a monoclonal antibody that binds HER2 extracellularly, while neratinib is a tyrosine kinase inhibitor that irreversibly blocks HER2 and other ErbB family kinases intracellularly.
Trastuzumab and neratinib together block HER2 signaling through complementary mechanisms: trastuzumab is a monoclonal antibody that binds HER2 extracellularly, while neratinib is a tyrosine kinase inhibitor that irreversibly blocks HER2 and other ErbB family kinases intracellularly. Used for HER2-positive breast cancer (early-stage or metastatic).
At a glance
| Generic name | Trastuzumab and neratinib |
|---|---|
| Sponsor | Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University |
| Drug class | HER2-targeted combination therapy (monoclonal antibody + tyrosine kinase inhibitor) |
| Target | HER2 (human epidermal growth factor receptor 2) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
This combination targets HER2-positive cancers by dual inhibition of the HER2 pathway. Trastuzumab provides antibody-mediated cellular cytotoxicity and blocks ligand-independent signaling, while neratinib provides irreversible kinase inhibition to prevent compensatory signaling and overcome resistance. The complementary mechanisms aim to achieve more complete HER2 pathway suppression than either agent alone.
Approved indications
- HER2-positive breast cancer (early-stage or metastatic)
Common side effects
- Diarrhea
- Nausea
- Vomiting
- Fatigue
- Rash
- Left ventricular dysfunction
- Hepatotoxicity
Key clinical trials
- Testing the Safety and Tolerability of the Anti-cancer Drugs Trastuzumab Deruxtecan and Neratinib for Cancers With Changes in the HER2 Gene (PHASE1)
- I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer (PHASE2)
- Trial of Pre-operative Neratinib and Endocrine Therapy With Trastuzumab in ER-Positive, HER-2 Positive Breast Cancers (PHASE2)
- Neratinib and Paclitaxel With or Without Pertuzumab and Trastuzumab Before Combination Chemotherapy in Treating Patients With Metastatic or Locally Advanced Breast Cancer (PHASE1, PHASE2)
- Neratinib In Combination With Chemotherapy/Trastuzumab/Pembrolizumab In HER2 Gastroesophageal Cancer (PHASE2)
- Pilot Study of [68Ga]Ga-ABY-025 Imaging in Patients Undergoing Treatment With HER2-targeted Therapy (EARLY_PHASE1)
- HKI-272 for HER2-Positive Breast Cancer and Brain Metastases (PHASE2)
- Neratinib Combined With Fulvestrant and Eribulin in the Treatment ofHR+/HER2+ Advanced Breast Cancer (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape: