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 | CI-1040 |
| Synonyms | |
| Therapy Description |
CI-1040 (PD184352) binds and inhibits Mek1 and Mek2, which may inhibit the activation of downstream signaling targets and reduce tumor cell proliferation (PMID: 14613031). |
Filtering
- Case insensitive filtering will display rows where any text in any cell matches the filter term
- Simple literal full or partial string matches
- Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "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 |
|---|---|---|---|---|
| CI-1040 | PD184352|PD-184352 | MEK inhibitor (Pan) 22 MEK1 Inhibitor 20 MEK2 Inhibitor 18 | CI-1040 (PD184352) binds and inhibits Mek1 and Mek2, which may inhibit the activation of downstream signaling targets and reduce tumor cell proliferation (PMID: 14613031, PMID: 16009947). |
Filtering
- Case insensitive filtering will display rows where any text in any cell matches the filter term
- Simple literal full or partial string matches
- Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "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 |
|---|---|---|---|---|---|---|---|
| ERBB2 T798M | breast cancer | resistant | CI-1040 | Preclinical | Actionable | In a preclinical study, breast cancer cells expressing ERBB2 T798M demonstrated resistance to CI-1040 (PMID: 23948973). | 23948973 |
| MAP2K1 F53S | Advanced Solid Tumor | sensitive | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, CI-1040 (PD184352) inhibited kinase activity of Map2k1 F53S expressed in transformed human kidney cells (PMID: 12370306). | 12370306 |
| BRAF T529M BRAF V600E | Advanced Solid Tumor | predicted - sensitive | CI-1040 | Preclinical | Actionable | In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation in transformed cells expressing BRAF V600E and the gatekeeper mutation BRAF T529M in culture (PMID: 20538618). | 20538618 |
| MAP2K1 L115A | Advanced Solid Tumor | decreased response | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, CI-1040 (PD184352) partially inhibited kinase activity of Map2k1 L115A expressed in transformed human kidney cells (PMID: 12370306). | 12370306 |
| BRAF T529N BRAF V600E | Advanced Solid Tumor | sensitive | CI-1040 | Preclinical | Actionable | In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation and growth of transformed cells expressing BRAF V600E and the gatekeeper mutation BRAF T529N in culture (PMID: 20538618). | 20538618 |
| MAP2K1 I103N | Advanced Solid Tumor | decreased response | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, CI-1040 (PD184352) partially inhibited kinase activity of Map2k1 I103N expressed in transformed human kidney cells (PMID: 12370306). | 12370306 |
| Unknown unknown | Advanced Solid Tumor | not applicable | CI-1040 | Phase I | Actionable | In a Phase I trial, CI-1040 treatment resulted in median stable disease for 5.5 months in 28% (19/66) of patients with advanced solid tumors (including colorectal, non-small-cell lung, pancreatic, melanoma, and kidney) and partial response in 1 pancreatic cancer patient (PMID: 16009947). | 16009947 |
| MAP2K1 L115P | melanoma | resistant | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, CI-1040 (PD184352) did not inhibit proliferation of melanoma cells expressing Map2k1 L115P (PMID: 19915144). | 19915144 |
| HRAS G12V | melanoma | sensitive | CI-1040 | Preclinical | Actionable | In a preclinical study CI-1040 (PD-184352) inhibited melanoma progression in a transgenic zebrafish model of melanoma expressing HRAS G12V (PMID: 26267534). | 26267534 |
| BRAF V600E MAP2K1 V211D | melanoma | resistant | CI-1040 | Preclinical | Actionable | In a preclinical study, melanoma cells harboring BRAF V600E and expressing MAP2K V211D demonstrated resistance to growth inhibition by CI-1040 in cell culture (PMID: 19915144). | 19915144 |
| BRAF V600E | Advanced Solid Tumor | sensitive | CI-1040 | Preclinical | Actionable | In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation and growth of transformed cells expressing BRAF V600E in culture (PMID: 20538618). | 20538618 |
| STK11 inact mut | Advanced Solid Tumor | sensitive | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, the presence an STK11 loss expression signature, which correlates with STK11 inactivating mutations, was associated with increased sensitivity to CI-1040 (PD184352) in human tumor cell lines in culture (PMID: 27821489). | 27821489 |
| MAP2K1 L115P | Advanced Solid Tumor | resistant | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of Map2k1 L115P expressed in transformed human kidney cells (PMID: 12370306). | 12370306 |
| BRAF T529I BRAF V600E | Advanced Solid Tumor | sensitive | CI-1040 | Preclinical | Actionable | In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation in transformed cells expressing BRAF V600E and the gatekeeper mutation BRAF T529I in culture (PMID: 20538618). | 20538618 |
| BRAF V600E | ovarian cancer | sensitive | CI-1040 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CI-1040 inhibited growth of a human ovarian cancer cell line harboring BRAF V600E in culture, and inhibited tumor growth in xenograft models (PMID: 19018267). | 19018267 |
| MAP2K1 I103N | melanoma | resistant | CI-1040 | Preclinical - Cell culture | Actionable | In a preclinical study, CI-1040 (PD184352) did not inhibit proliferation of melanoma cells expressing Map2k1 I103N (PMID: 19915144). | 19915144 |
Filtering
- Case insensitive filtering will display rows where any text in any cell matches the filter term
- Simple literal full or partial string matches
- Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "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 |
|---|
CKB BOOST