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Glossary RAF inhibitors

block proteins involved in cell growth signaling pathways

RAF inhibitors, also known as RAF kinase inhibitors, are a class of drugs designed to block the activity of RAF kinases, which are proteins involved in cell signaling pathways that control cell growth and division. These inhibitors are particularly important in the treatment of certain cancers, such as melanoma, where mutations in the RAF gene (e.g., BRAF mutations) lead to uncontrolled cell proliferation. By inhibiting RAF kinases, these drugs can help to slow down or stop the growth of cancer cells.

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research Abstract 1677: Epithelial hyperplasia induced by a selective B-Raf inhibitor, WYE-130600

1 citations , April 2010 in “Cancer Research”

In preclinical studies, a B-Raf inhibitor called WYE-130600 caused dose-related skin effects in dogs and rats, suggesting potential similar responses might occur in humans.

Repurposing a Clinical Antimalarial for the Therapeutic Induction of Lethal ER Stress Targeting BRAF-Kinase Inhibitor-Resistant Malignant Melanoma

research 554 Repurposing a clinical antimalarial for the therapeutic induction of lethal ER stress targeting BRAF-kinase inhibitor-resistant malignant melanoma

April 2016 in “Journal of Investigative Dermatology”

This study identified mefloquine as a potent inducer of lethal ER stress that effectively eliminated vemurafenib-resistant and sensitive melanoma cells, suggesting its potential for repurposing as a melanoma treatment.

research BRAF Inhibitor Dabrafenib in Patients with Metastatic BRAF-Mutant Thyroid Cancer

188 citations , October 2014 in “Thyroid”

This study found that dabrafenib was well tolerated and led to durable responses in patients with BRAF-mutant differentiated thyroid carcinoma, with a median progression-free survival of 11.3 months.

research Cutaneous manifestations of dabrafenib (GSK2118436): a selective inhibitor of mutant BRAF in patients with metastatic melanoma

173 citations , July 2012 in “British Journal of Dermatology”

This study found that the administration of the mutant BRAF inhibitor dabrafenib in patients with metastatic melanoma was associated with various skin lesions, including keratinocytic proliferation that sometimes showed low-grade malignancy features.

research Cutaneous adverse effects of BRAF inhibitors in metastatic malignant melanoma, a prospective study in 20 patients.

31 citations , March 2014 in “Journal of the European Academy of Dermatology and Venereology”

In this study, multiple cutaneous adverse effects were observed in patients with metastatic malignant melanoma receiving BRAF inhibitors, but most were well managed with appropriate treatment.

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