Therapy Detail

Therapy Name PD-0325901
Synonym
Therapy Description

PD-0325901, a derivative of CI-1040, is a pan-MEK inhibitor, which inhibits activation of MAPK/ERK resulting in decreased tumor cell proliferation (PMID: 18952427).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
PD-0325901 PD0325901|PD-901 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 PD-0325901, a derivative of CI-1040, is a pan-MEK inhibitor, which inhibits activation of MAPK/ERK resulting in decreased tumor cell proliferation (PMID: 18952427).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown melanoma not applicable PD-0325901 Phase I Actionable In a Phase I trial, PD-0325901 demonstrated some efficacy in previously treated melanoma patients, however, there was significant toxicity above 10 mg BID (PMID: 21516509). 21516509
KRAS G12C pancreatic adenocarcinoma sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, a pancreatic adenocarcinoma cell line harboring KRAS G12C demonstrated sensitivity to growth inhibition by MEK inhibitors, including PD-0325901, in culture (PMID: 28957417). 28957417
BRAF V600E melanoma conflicting PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, a melanoma cell line xenograft model harboring BRAF V600E treated with PD-0325901 demonstrated stable tumor growth, but by day 44, growth ensued and thus, demonstrated no benefit (PMID: 27488531). 27488531
BRAF V600E melanoma conflicting PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, PD-0325901 inhibited growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 26267534). 26267534
MAP2K1 Q56P lung adenocarcinoma sensitive PD-0325901 Preclinical Actionable In a preclinical study, a lung adenocarcinoma cell line harboring MAP2K1 Q56P demonstrated sensitivity to PD-0325901, resulting in decreased cell viability (PMID: 26582713). 26582713
KIT W557_K558del gastrointestinal stromal tumor sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, PD-0325901 treatment inhibited Erk phosphorylation and decreased expression of ETV1 and CXCR4 in gastrointestinal stromal tumor cells harboring KIT W557_K558del (PMID: 26936919). 26936919
Unknown unknown Advanced Solid Tumor not applicable PD-0325901 Phase I Actionable In a Phase I clinical trial, PD-0325901 demonstrated preliminary clinical activity in patients with advanced solid tumors, however late-onset dose-limiting toxicities were encountered (PMID: 20215549). 20215549
KRAS G12S lung cancer decreased response PD-0325901 Preclinical Actionable In a preclinical study, a lung cancer cell line harboring KRAS G12S demonstrated a decreased response when treated with PD-0325901 in culture (PMID: 26582713). 26582713
BRAF V600E colon cancer sensitive PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, PD-0325901 demonstrated antitumor activity against BRAF V600E colon cancer cell line xenografts (PMID: 16273091). 16273091
BRAF V600E MAP2K1 I103N melanoma resistant PD-0325901 Preclinical Actionable In a preclinical study, over expression of MAPK21 I103N in melanoma cells harboring BRAF V600E resulted in insensitivity to growth inhibition by PD-0325901 in cell culture (PMID: 26267534). 26267534
KRAS G12X Advanced Solid Tumor sensitive PD-0325901 Preclinical Actionable In a preclinical study, transformed cell lines with various KRAS codon 12 mutations displayed differential inhibition by PD-0325901 (PMID: 26037647). 23934108 26037647
KRAS A146T colorectal cancer sensitive PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, PD-0325901 inhibited growth of colorectal cancer cell lines harboring KRAS A146T in culture and in cell line xenograft models (PMID: 20570890). 20570890
STK11 inact mut Advanced Solid Tumor sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, the presence of an STK11 loss expression signature, which correlates with STK11 inactivating mutations, was associated with increased sensitivity to PD-0325901 in human tumor cell lines in culture (PMID: 27821489). 27821489
BRAF V600E colorectal cancer sensitive PD-0325901 Preclinical Actionable In a preclinical study, PD-0325901 inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 26267534). 26267534
BRAF V600E MAP2K1 L115P melanoma resistant PD-0325901 Preclinical Actionable In a preclinical study, over expression of MAPK21 L115P in melanoma cells harboring BRAF V600E resulted in insensitivity to growth inhibition by PD-0325901 in cell culture (PMID: 26267534). 26267534
NRAS mutant melanoma no benefit PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, PD-0325901 treatment resulted in stable tumor growth in melanoma cell line xenograft models harboring an NRAS mutation, however, growth later ensued and thus, demonstrates a lack of benefit (PMID: 27488531). 27488531
KRAS G12D lung adenocarcinoma sensitive PD-0325901 Preclinical Actionable In a preclinical study, PD-0325901 inhibited growth of lung adenocarcinomas in mouse models expressing Kras G12D (PMID: 22684718). 22684718
BRAF V600E KRAS mutant colorectal cancer resistant PD-0325901 Preclinical Actionable In a preclinical study, over expression of BRAF V600E in KRAS-mutant colorectal cancer cells resulted in resistance to growth inhibition by PD-0325901 in cell culture (PMID: 26267534). 26267534
Unknown unknown colorectal cancer not applicable PD-0325901 Phase I Actionable In a Phase I study, PD-325901 demonstrated efficacy but toxicity at current dose was unacceptable (PMID: 21516509). 21516509
BRAF V600E glioblastoma multiforme decreased response PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, a glioblastoma cell line harboring BRAF V600E demonstrated a decreased response to treatment with PD-0325901, demonstrating increased viability of CD133 positive cells in culture (PMID: 26573800). 26573800
Unknown unknown breast cancer not applicable PD-0325901 Phase I Actionable In a Phase I trial, PD-0325901 demonstrated some efficacy, however, the dose administered resulted in a significant degree of toxicity (PMID: 21516509). 21516509
Clinical Trial Phase Therapies Title Recruitment Status
NCT02096471 Phase II PD-0325901 MEK Inhibitor PD-0325901 Trial in Adolescents and Adults With NF1 Completed
NCT01347866 Phase I Gedatolisib PD-0325901 Irinotecan Clinical Study Of PI3K/mTOR Inhibitors In Combination With An Oral MEK Inhibitor Or Irinotecan In Patients With Advanced Cancer Terminated