Related Experiment Video

Updated: Aug 13, 2026

Drug-Induced Senescence in Liver Cells Promotes M2 Macrophage Polarization: Implications for Tyrosine Kinase Inhibitor-Associated Hepatotoxicity
09:32

Drug-Induced Senescence in Liver Cells Promotes M2 Macrophage Polarization: Implications for Tyrosine Kinase Inhibitor-Associated Hepatotoxicity

Published on: October 17, 2025

Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors

Michael H Nelson1, Christian R Dolder

  • 1School of Pharmacy, Wingate University, Wingate, NC 28174-0159, USA. mnelson@wingate.edu

The Annals of Pharmacotherapy
|January 19, 2006
PubMed
Abstract

Insights

Lapatinib is a dual tyrosine kinase inhibitor showing activity in solid tumors, particularly advanced breast cancer. This targeted therapy has a manageable side effect profile, with diarrhea and rash being most common.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Tyrosine kinase inhibitors (TKIs) represent a targeted approach to cancer therapy.
  • Understanding tumor cell biology has enabled the development of novel therapeutics.
  • Lapatinib targets key signaling pathways in solid tumors.

Purpose of the Study:

  • To review the pharmacology, pharmacokinetics, clinical trials, adverse effects, and drug interactions of lapatinib.
  • To assess the efficacy and safety of lapatinib in solid tumors.
  • To provide a comprehensive overview of lapatinib for clinical application.

Main Methods:

  • A comprehensive literature search was conducted using PubMed and other sources.
  • Included preclinical and clinical trials evaluating lapatinib in various models and human subjects.
  • Focused on pivotal in vitro and all published in vivo data.

Main Results:

  • Lapatinib is a dual tyrosine kinase inhibitor targeting EGFR and HER2, suppressing tumor proliferation.
  • Demonstrated clinical activity in solid tumors, notably advanced or metastatic breast cancer, including trastuzumab-refractory cases.
  • Exhibited a mild adverse effect profile, with diarrhea and rash as the most frequent events.

Conclusions:

  • Lapatinib possesses novel dual tyrosine kinase inhibitory properties targeting overexpressed factors in solid tumors.
  • Preclinical and Phase I/II trials suggest efficacy in solid tumors, especially advanced breast cancer.
  • Further evaluation in ongoing Phase III trials is expected to support regulatory approval.

More Related Videos

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

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 specific...
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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...
lncRNA - Long Non-coding RNAs02:39

lncRNA - Long Non-coding RNAs

In humans, more than 80% of the genome gets transcribed. However, only around 2% of the genome codes for proteins. The remaining part produces non-coding RNAs which includes ribosomal RNAs, transfer RNAs, telomerase RNAs, and regulatory RNAs, among other types. A large number of regulatory non-coding RNAs have been classified into two groups depending upon their length – small non-coding RNAs, such as microRNA, which are less than 200 nucleotides in length, and long non-coding RNA (lncRNA)...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...