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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.

The Cutaneous Side Effects of Selective BRAF Inhibitors and Anti-CTLA4 Agents: The Growing Role of the Dermatologist in the Management of Patients with Metastatic Melanoma

research The Cutaneous Side Effects of Selective BRAF Inhibitors and Anti-CTLA4 Agents: the Growing Role of the Dermatologist in the Management of Patients with Metastatic Melanoma

6 citations , April 2013 in “Current Dermatology Reports”

This review discusses the cutaneous side effects associated with vemurafenib and ipilimumab in metastatic melanoma treatment and emphasizes the importance of dermatologists in managing these skin eruptions; it reports no new clinical results.

research Wound healing with topical BRAF inhibitor therapy in a diabetic model suggests tissue regenerative effects

3 citations , June 2021 in “PLOS ONE”

This study found that topical application of the BRAF inhibitor vemurafenib improved wound healing and promoted hair follicle regeneration in a diabetic murine model.

research Melanotic pigmentation in excisional scar of melanoma patient who received BRAF and MEK inhibitors

1 citations , August 2018 in “Journal of The American Academy of Dermatology”

Patients with melanoma who saw dermatologists and were from higher-income areas were more likely to have follow-up visits, which was linked to lower mortality.

research 696 MEK and BRAF inhibitors augment the production and accumulation of sebum in hamster sebocytes

April 2016 in “Journal of Investigative Dermatology”

This study found that trametinib and vemurafenib increased sebum production and gene expression related to lipid accumulation in hamster sebocytes, which may help explain certain side effects in patients.

research Network pharmacology and molecular docking analysis on potential molecular targets and mechanism of action of BRAF inhibitors for application in wound healing

11 citations , June 2023 in “Journal of Cellular Biochemistry”

This study suggests that BRAF inhibitors, particularly Encorafenib and Dabrafenib, may have potential applications in wound healing by targeting specific proteins involved in the healing process in murine models.

research Inhibition of mitochondrial respiration prevents BRAF-mutant melanoma brain metastasis

29 citations , April 2019 in “Acta neuropathologica communications”

This study found that β-sitosterol, a brain-penetrable phytosterol, reduced melanoma cell growth and brain metastasis formation by interfering with mitochondrial respiration, suggesting its potential as an adjuvant therapy to BRAF inhibitors for patients with melanoma brain metastases.

research Alopecia due to chemotherapeutics, hedgehog inhibitors, targeted antibody therapies and immune checkpoint inhibitors

May 2024 in “Deleted Journal”

This study reports that chemotherapy-induced hair loss affects up to 65% of patients, typically within 1 to 3 weeks of treatment, while scalp cooling may help prevent severe hair loss with taxane-based therapies.

research The risk of dermatological toxicities of combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma patients: a systematic review and meta-analysis

9 citations , December 2018 in “Cutaneous and Ocular Toxicology”

This meta-analysis found that combined BRAF and MEK inhibitor treatment in melanoma patients is linked to increased all-grade rash but reduced risks of several other dermatological toxicities compared to BRAF inhibition alone.

research Toxic Side Effects of Targeted Therapies and Immunotherapies Affecting the Skin, Oral Mucosa, Hair, and Nails

179 citations , October 2018 in “American Journal of Clinical Dermatology”

This review outlines various dermatologic adverse events associated with targeted therapies and immunotherapies, emphasizing the need for collaboration between dermatologists and oncologists to manage these effects effectively; it reports no new clinical findings.

research Cutaneous reactions to chemotherapeutic drugs and targeted therapy for cancer

88 citations , July 2014 in “Journal of the American Academy of Dermatology”

This review discusses common cutaneous reactions to targeted cancer drugs such as tyrosine kinase inhibitors and reports no new clinical results.

research Cutaneous Drug Eruptions Associated with the Use of New Oncological Drugs

29 citations , January 2012 in “Chemical immunology/Fortschritte der Allergielehre/Progress in allergy/Chemical immunology and allergy”

This review discusses the various skin, mucosa, and adnexa side effects associated with different chemotherapeutic agents and provides insights into their clinical presentation and management; it reports no new results.

research Dermatologic adverse events associated with chemotherapy and targeted anticancer therapy

4 citations , January 2016 in “Dermatology Review”

This review focuses on the various skin toxicities caused by chemotherapeutic and targeted tumor therapy drugs, including rashes, keratoacanthoma, and more severe conditions like Stevens-Johnson syndrome, without presenting new clinical results.

research Diseases of the Canine Prostate Gland

1 citations , August 2022 in “Veterinary medicine and science”

This review discusses various diagnostic and treatment strategies for canine prostate diseases, including pharmacological options and advanced procedures, but reports no new clinical results.

research The Influence of Flightless I: Regeneration versus Wound Healing

1 citations , March 2011 in “Journal of Investigative Dermatology”

This study found that Flightless I (Flii) positively influences hair follicle regeneration in rodents, contrasting with its known negative effect on wound healing.

research Tombo em João Pessoa dá força a Memorial da Arquitetura Paraibana

January 2008 in “Projeto: revista mensal de arquitetura”

This article reviews the cutaneous reactions associated with targeted cancer therapies and highlights the importance of dermatologists recognizing these reactions to provide effective care but reports no clinical results.

research Cutaneous toxicities of new treatments for melanoma

25 citations , May 2018 in “Clinical & Translational Oncology”

This review summarizes common skin-related side effects of BRAF inhibitors and immunotherapy in advanced melanoma treatment, reporting no new clinical findings, and emphasizes consensus management to improve patient outcomes.

research The spectrum of cutaneous adverse events during encorafenib and binimetinib treatment in B‐rapidly accelerated fibrosarcoma‐mutated advanced melanoma

21 citations , November 2018 in “Journal of the European Academy of Dermatology and Venereology”

In this study, encorafenib combined with binimetinib was well tolerated in melanoma patients, resulting in relatively few cutaneous adverse events compared to other BRAF and MEK inhibitors.

research Management of Dermatologic Toxicities

12 citations , May 2015 in “Journal of the National Comprehensive Cancer Network”

This article provides a narrative on managing dermatologic side effects from cancer therapies and suggests strategies that oncologists could adopt, but it reports no new clinical findings.

research Adverse Hair Reactions to New Targeted Therapies for Cancer

1 citations , March 2019 in “Actas Dermo-Sifiliográficas”

This review discusses the adverse effects on hair associated with targeted cancer therapies and reports no new clinical results; it emphasizes the need for comprehensive documentation of these effects.

research RASopathic Skin Eruptions during Vemurafenib Therapy

82 citations , March 2013 in “PLoS ONE”

In this study, vemurafenib was associated with a wide range of cutaneous side effects in patients with advanced melanoma, including photosensitivity and various skin and hair changes, necessitating regular dermatological management.

research Is knowledge about the genetic and epigenetic alterations in melanoma a basis for targeted therapy?

September 2006 in “Experimental Dermatology”

This review discusses the genetic pathways involved in melanoma and suggests that targeting these pathways with pharmacological inhibitors may provide a new therapeutic approach, though clinical results have been disappointing so far.

research Hair and nail adverse events during treatment with targeted therapies for metastatic melanoma

32 citations , May 2016 in “European journal of dermatology/EJD. European journal of dermatology”

In this study, researchers found that targeted therapies for metastatic melanoma often cause hair and nail side effects, with hair changes more common in patients treated with BRAF inhibitors like vemurafenib.

research Hair(y) Matters in Melanoma Biology

7 citations , May 2020 in “Trends in molecular medicine”

This study explored the immune environment of the hair follicle's bulge region and suggested that its unique signaling may prevent melanoma formation by lacking necessary proinflammatory signals for full oncogenic transformation, indicating potential strategies for melanoma prevention by replicating this immune-privileged environment.

research Targeted therapy in melanoma

21 citations , February 2013 in “Clinics in Dermatology”

This review discusses recent developments in targeted melanoma therapies, including BRAF/MEK/ERK pathway inhibitors and challenges like resistance and skin toxicities, but reports no new clinical results.

research Progress in Dermatology and Venereology in 2023 as reflected in the Journal of the European Academy of Dermatology and Venereology

December 2023 in “JEADV. Journal of the European Academy of Dermatology and Venereology/Journal of the European Academy of Dermatology and Venereology”

This study found that among melanoma patients in a real-world setting, adjuvant anti-PD-1 antibodies and BRAF/MEK inhibitors were associated with a recurrence-free survival of 78.1% and 86.5% respectively after 12 months.