Related Experiment Videos

Trametinib (GSK1120212)

Robert Zeiser1, Hana Andrlová2, Frank Meiss3

  • 1Department of Hematology, Oncology and Stem Cell Transplantation, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Hugstetterstr. 55, 79106, Freiburg, Germany. robert.zeiser@uniklinik-freiburg.de.

Recent Results in Cancer Research. Fortschritte Der Krebsforschung. Progres Dans Les Recherches Sur Le Cancer
|August 3, 2018
PubMed

Insights

Trametinib, a MEK inhibitor (mitogen-activated protein kinase/ERK kinase), shows promise in treating metastatic melanoma. Further trials will explore its role in other solid tumors, potentially combined with BRAF inhibitors.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Mitogen-activated protein kinase (MEK) signaling pathways regulate crucial cellular functions like proliferation and survival.
  • MEK inhibition is a validated strategy for antineoplastic (anti-cancer) therapy.
  • Trametinib is a selective oral inhibitor of MEK1 and MEK2.

Purpose of the Study:

  • To review preclinical and clinical data for trametinib.
  • To present the mechanisms of action of trametinib.
  • To discuss the potential of trametinib in treating various solid tumors.

Main Methods:

  • Review of in vitro studies.
  • Analysis of preclinical data.
  • Evaluation of findings from clinical studies.

Main Results:

  • Trametinib is FDA-approved for metastatic melanoma in combination with a BRAF inhibitor.
  • Preclinical and clinical data support trametinib's efficacy.
  • Trametinib targets MEK1 and MEK2, key components of the MAPK/ERK pathway.

Conclusions:

  • Trametinib is an effective targeted therapy for certain cancers.
  • Future clinical trials are necessary to define trametinib's role in other solid tumors.
  • Combination therapy, particularly with BRAF inhibitors, may enhance trametinib's therapeutic potential.
Keywords:
Kinase inhibitionMAPK/ERK Kinase (MEK)Small moleculesTrametinib

Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
375
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...
8.5K