The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence
Historically, patients with advanced cutaneous melanoma have a poor prognosis and limited treatment options. The discovery of selective v-raf murine sarcoma viral oncogene homolog B1 (BRAF) V600 mutation as an oncogenic mutation in cutaneous melanoma and the importance of the mitogen-activated prote...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
| Published: |
SAGE Publishing
2012-03-01
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| Series: | Therapeutic Advances in Medical Oncology |
| Online Access: | https://doi.org/10.1177/1758834011432949 |
| _version_ | 1828308823969890304 |
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| author | Charlotte Lemech Jeffrey Infante Hendrik-Tobias Arkenau |
| author_facet | Charlotte Lemech Jeffrey Infante Hendrik-Tobias Arkenau |
| author_sort | Charlotte Lemech |
| collection | DOAJ |
| description | Historically, patients with advanced cutaneous melanoma have a poor prognosis and limited treatment options. The discovery of selective v-raf murine sarcoma viral oncogene homolog B1 (BRAF) V600 mutation as an oncogenic mutation in cutaneous melanoma and the importance of the mitogen-activated protein kinase (MAPK) pathway in its tumourigenesis have changed the treatment paradigm for melanoma. Selective BRAF inhibitors and now MEK inhibitors have demonstrated response rates far higher than standard chemotherapeutic options and we review the phase I–III results for these agents in this article. The understanding of mechanisms of resistance that may occur upstream, downstream, at the BRAF level or bypassing the MAPK pathway provides a platform for rational drug development and combination therapies. |
| first_indexed | 2024-04-13T15:19:10Z |
| format | Article |
| id | doaj.art-aeb52944b9a34e078ce0263377eedafe |
| institution | Directory Open Access Journal |
| issn | 1758-8340 1758-8359 |
| language | English |
| last_indexed | 2024-04-13T15:19:10Z |
| publishDate | 2012-03-01 |
| publisher | SAGE Publishing |
| record_format | Article |
| series | Therapeutic Advances in Medical Oncology |
| spelling | doaj.art-aeb52944b9a34e078ce0263377eedafe2022-12-22T02:41:43ZengSAGE PublishingTherapeutic Advances in Medical Oncology1758-83401758-83592012-03-01410.1177/1758834011432949The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidenceCharlotte LemechJeffrey InfanteHendrik-Tobias ArkenauHistorically, patients with advanced cutaneous melanoma have a poor prognosis and limited treatment options. The discovery of selective v-raf murine sarcoma viral oncogene homolog B1 (BRAF) V600 mutation as an oncogenic mutation in cutaneous melanoma and the importance of the mitogen-activated protein kinase (MAPK) pathway in its tumourigenesis have changed the treatment paradigm for melanoma. Selective BRAF inhibitors and now MEK inhibitors have demonstrated response rates far higher than standard chemotherapeutic options and we review the phase I–III results for these agents in this article. The understanding of mechanisms of resistance that may occur upstream, downstream, at the BRAF level or bypassing the MAPK pathway provides a platform for rational drug development and combination therapies.https://doi.org/10.1177/1758834011432949 |
| spellingShingle | Charlotte Lemech Jeffrey Infante Hendrik-Tobias Arkenau The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence Therapeutic Advances in Medical Oncology |
| title | The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence |
| title_full | The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence |
| title_fullStr | The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence |
| title_full_unstemmed | The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence |
| title_short | The potential for BRAF V600 inhibitors in advanced cutaneous melanoma: rationale and latest evidence |
| title_sort | potential for braf v600 inhibitors in advanced cutaneous melanoma rationale and latest evidence |
| url | https://doi.org/10.1177/1758834011432949 |
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