Therapy Detail
Contact
Missing content? – Request curation!
Request curation for specific Genes, Variants, or PubMed publications.
Have questions, comments, or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
| Therapy Name | RAF265 |
| Synonyms | |
| Therapy Description |
RAF265 inhibits the activities of several intracellular kinases, including BRAF(V600E), BRAF(wild type), c-RAF (RAF1), VEGF receptor 2 (VEGFR2/KDR), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF)1R, RET and c-KIT, SRC, STE20, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death (PMID: 22351689, PMID: 28719152). |
Filtering
- Case insensitive filtering will display rows if any text in any cell matches the filter term
- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
- Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.
| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| RAF265 | CHIR-265|NVP-RAF265 | BRAF Inhibitor 25 CRAF Inhibitor 12 VEGFR2 Inhibitor 37 | RAF265 inhibits the activities of several intracellular kinases, including BRAF(V600E), BRAF(wild type), c-RAF (RAF1), VEGF receptor 2 (VEGFR2/KDR), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF)1R, RET and c-KIT, SRC, STE20, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death (PMID: 22351689, PMID: 28719152). |
Filtering
- Case insensitive filtering will display rows if any text in any cell matches the filter term
- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
- Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF T529M BRAF V600E | Advanced Solid Tumor | predicted - sensitive | RAF265 | Preclinical | Actionable | In a preclinical study, RAF265 inhibited kinase activity in vitro, and downstream Erk phosphorylation in cells expressing BRAF V600E and the gatekeeper mutation BRAF T529M to a similar degree as transformed cells expressing BRAF V600E in culture (PMID: 20538618). | 20538618 |
| BRAF T529I BRAF V600E | Advanced Solid Tumor | predicted - sensitive | RAF265 | Preclinical | Actionable | In a preclinical study, RAF265 inhibited kinase activity in vitro, and downstream Erk phosphorylation in cells expressing BRAF V600E and the gatekeeper mutation BRAF T529I to a similar degree as transformed cells expressing BRAF V600E in culture (PMID: 20538618). | 20538618 |
| NRAS Q61L | urinary bladder cancer | sensitive | RAF265 | Preclinical - Cell culture | Actionable | In a preclinical study, RAF265 treatment decreased colony formation of a bladder cancer cell line harboring NRAS Q61L in culture (PMID: 34554931). | 34554931 |
| NRAS Q61R | urinary bladder cancer | sensitive | RAF265 | Preclinical - Cell culture | Actionable | In a preclinical study, RAF265 treatment decreased viability of a bladder cancer cell line harboring NRAS Q61R in culture (PMID: 34554931). | 34554931 |
| BRAF wild-type | melanoma | predicted - sensitive | RAF265 | Preclinical | Actionable | In a preclinical study, RAF265 inhibited the growth of melanoma tumors orthotopically implanted in mice, including tumors wild-type for BRAF (PMID: 22351689). | 22351689 |
| BRAF wild-type | melanoma | predicted - sensitive | RAF265 | Phase I | Actionable | In a Phase I trial, treatment with RAF265 in melanoma patients resulted in an objective response rate of 12.1% (8/66), including a partial response in four patients harboring BRAF V600E, two partial responses and one complete response in patients with wild-type BRAF, and one complete response in a patient with unknown mutational status (PMID: 28719152). | 28719152 |
| BRAF T529N BRAF V600E | Advanced Solid Tumor | resistant | RAF265 | Preclinical | Actionable | In a preclinical study, transformed cells expressing BRAF V600E and the gatepkeeper mutation BRAF T529N were insensitive to RAF265 in culture (PMID: 20538618). | 20538618 |
| BRAF V600E | melanoma | predicted - sensitive | RAF265 | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with RAF265 in melanoma patients resulted in an objective response rate of 12.1% (8/66), including a partial response in four patients harboring BRAF V600E, two partial responses and one complete response in patients with wild-type BRAF, and one complete response in a patient with unknown mutational status (PMID: 28719152). | 28719152 |
| BRAF V600E | Advanced Solid Tumor | sensitive | RAF265 | Preclinical | Actionable | In a preclinical study, RAF265 inhibited Erk phosphorylation and cell proliferation in BRAF V600E expressing cells in culture (PMID: 20538618). | 20538618 |
| HRAS G12V | urinary bladder cancer | sensitive | RAF265 | Preclinical - Cell culture | Actionable | In a preclinical study, RAF265 treatment decreased viability and colony formation of a bladder cancer cell line harboring HRAS G12V in culture (PMID: 34554931). | 34554931 |
Filtering
- Case insensitive filtering will display rows if any text in any cell matches the filter term
- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
- Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.
| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
CKB BOOST