Therapy Detail

Therapy Name CI-1040
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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
CI-1040 PD184352|PD-184352 MEK inhibitor (Pan) 20 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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 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
KRAS mutant 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 a KRAS mutation in culture, and inhibited tumor growth in xenograft models (PMID: 19018267). 19018267
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
KRAS mutant colorectal cancer sensitive CI-1040 Preclinical Actionable In a preclinical study, colorectal cancer cells harboring KRAS mutations demonstrated sensitivity to CI-1040 in culture (PMID: 19372556). 19372556
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 BRAF T529N 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
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 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
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
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
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 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
BRAF V600E BRAF T529M 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
BRAF V600E BRAF T529I 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 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
Clinical Trial Phase Therapies Title Recruitment Status