loading...| Preferred Name |
vemurafenib |
|
| Synonyms |
BRAF(V600E) Kinase Inhibitor RO5185426 BRAF(V600E) kinase inhibitor RO5185426 RO5185426 Zelboraf PLX4032 RG7204 |
|
| Definitions |
An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C64768" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C64768" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000528954 |
|
| altLabel |
BRAF(V600E) Kinase Inhibitor RO5185426 BRAF(V600E) kinase inhibitor RO5185426 RO5185426 Zelboraf PLX4032 RG7204 |
|
| cui |
C1832009 C3192263 C3192267 C4083042 C4083043 |
|
| DATE FIRST PUBLISHED |
2007-01-05 |
|
| Date last modified |
2011-08-17 |
|
| definition |
An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C64768" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C64768" NCI Thesaurus) |
|
| LT |
TRD |
|
| NCI ID |
C64768 |
|
| notation |
CDR0000528954 |
|
| ORIG STY |
Drug/agent |
|
| prefLabel |
vemurafenib |
|
| tui |
T109 T121 |