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Extracellular signal-regulated kinase (ERK) inhibitors in oncology clinical trials

1 Rice University, Denver, CO, USA
2 University of Colorado – Denver, Denver, CO, USA
3 Sarah Cannon Research Institute at HealthONE, Denver, CO, USA

Correspondence Address:
Gerald S Falchook,
Sarah Cannon Research Institute at HealthONE, 1800 Williams Street, Suite 300, Denver, CO 80218
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/JIPO.JIPO_17_18

The mitogen-activated protein kinase (MAPK) pathway consists of the series of protein kinases RAS-RAF-MEK- Extracellular signal-regulated kinase (ERK), and its function is important to cell proliferation, differentiation, motility, and survival. Certain mutations in the pathway, such as KRAS or BRAF V600 mutations are associated with cancer. Inhibitors of this pathway, including some MEK and BRAF inhibitors, are already being used in the clinic, but a variety of selective ERK inhibitors are still being tested in clinical studies. To date, common adverse events associated with ERK inhibitors include diarrhea, nausea, fatigue, and rash. ERK inhibitors have demonstrated preliminary antitumor activity and may be most effective against cancers with RAS, RAF, or MAPK pathway alterations. This review discusses the MAPK pathway, the biological rationale for ERK inhibitors, and clinical trials involving ERK inhibitors.

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