Related Experiment Video

Updated: Jun 20, 2025

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
14:20

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?

Published on: June 13, 2014

16.7K

Synthetic routes and clinical application of Small-Molecule HER2 inhibitors for cancer therapy

He-Nan Liu1, Ying Zhu2, Yuan Chi3

  • 1Department of Ophthalmology, Shengjing Hospital of China Medical University, Shenyang, China.

Bioorganic Chemistry
|July 18, 2024
PubMed

Insights

This review details small-molecule tyrosine kinase inhibitors (TKIs) targeting human epidermal growth factor receptor 2 (HER2) for cancer therapy. It covers synthesis, clinical uses of lapatinib, neratinib, and tucatinib, and future research directions.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Human epidermal growth factor receptor 2 (HER2) is a key driver in various cancers.
  • Small-molecule tyrosine kinase inhibitors (TKIs) offer targeted therapeutic strategies.
  • HER2-positive malignancies, including breast and gastric cancers, require effective treatment options.

Purpose of the Study:

  • To comprehensively review the synthesis and clinical applications of HER2-targeted small-molecule TKIs.
  • To highlight the advancements and challenges in developing these targeted therapies.
  • To provide insights for pharmaceutical scientists in the field of HER2-targeted drug development.

Main Methods:

  • Literature review focusing on small-molecule TKIs targeting HER2.
  • Analysis of synthesis strategies and structural complexities of key inhibitors.
  • Evaluation of clinical data for lapatinib, neratinib, and tucatinib in HER2-positive cancers.

Main Results:

  • Detailed examination of synthesis pathways for lapatinib, neratinib, and tucatinib.
  • Demonstrated clinical efficacy of these TKIs in HER2-positive breast and gastric cancers.
  • Tucatinib's ability to cross the blood-brain barrier offers new hope for metastatic disease.

Conclusions:

  • HER2 TKIs represent significant progress in cancer therapeutics, particularly for HER2-positive cancers.
  • Overcoming resistance mechanisms and off-target effects remains a critical area for ongoing research.
  • Development of next-generation HER2 TKIs is essential for improved patient outcomes.
Keywords:
ApplicationHER2Small-moleculeSynthetic routesTKIs

More Related Videos

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down08:59

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down

Published on: December 11, 2017

7.2K
Validated Immunochemical Assay for Comprehensive Determination of the Human Epidermal Growth Factor Receptor 2 Released from and Bound to Cells08:29

Validated Immunochemical Assay for Comprehensive Determination of the Human Epidermal Growth Factor Receptor 2 Released from and Bound to Cells

Published on: May 9, 2025

91

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.5K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
6.4K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
4.9K
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
697