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HKI-272
HKI-272 is a small molecule inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase.
HKI-272 is a small molecule inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase. Used for Metastatic breast cancer, HER2 positive, Locally advanced or metastatic breast cancer, HER2 positive.
At a glance
| Generic name | HKI-272 |
|---|---|
| Also known as | neratinib, Neratinib |
| Sponsor | Puma Biotechnology, Inc. |
| Drug class | HER2 inhibitor |
| Target | HER2 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 2 |
Mechanism of action
By inhibiting the HER2 tyrosine kinase, HKI-272 prevents the activation of downstream signaling pathways that promote cell proliferation and survival, thereby exerting its anti-tumor effects.
Approved indications
- Metastatic breast cancer, HER2 positive
- Locally advanced or metastatic breast cancer, HER2 positive
Common side effects
- Fatigue
- Nausea
- Diarrhea
- Vomiting
- Rash
Key clinical trials
- Testing the Use of Neratinib or the Combination of Neratinib and Palbociclib Targeted Treatment for HER2+ Solid Tumors (A ComboMATCH Treatment Trial) (PHASE2)
- Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
- Testing the Safety and Tolerability of the Anti-cancer Drugs Trastuzumab Deruxtecan and Neratinib for Cancers With Changes in the HER2 Gene (PHASE1)
- Neratinib and Paclitaxel With or Without Pertuzumab and Trastuzumab Before Combination Chemotherapy in Treating Patients With Metastatic or Locally Advanced Breast Cancer (PHASE1, PHASE2)
- HKI-272 for HER2-Positive Breast Cancer and Brain Metastases (PHASE2)
- Neratinib and Everolimus, Palbociclib, or Trametinib in Treating Participants With Refractory and Advanced or Metastatic Solid Tumors With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation (PHASE1)
- Neratinib in Extended Adjuvant Treatment for HER2+ Early Breast Cancer With pCR But High-Risk Features: A Hebei Multi-Center Real-World Study
- Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial (PHASE1)
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 |