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Therapy Name PD-0325901
Synonyms
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, PMID: 32147669).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
PD-0325901 PD0325901|PD 0325901|PD-901|Mirdametinib MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 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, PMID: 32147669).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
NRAS Q61L acute myeloid leukemia predicted - sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, PD-0325901 treatment induced apoptosis and inhibited proliferation of an acute myeloid leukemia cell line harboring NRAS Q61L in culture (PMID: 28923853). 28923853
BRAF V600E melanoma conflicting PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, PD-0325901 treatment induced cell cycle arrest and inhibited growth of melanoma cells harboring BRAF V600E in culture (PMID: 25422890). 25422890
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
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
BRAF N486_P490del melanoma sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, a melanoma cell line harboring BRAF N486_P490del demonstrated sensitivity to PD-0325901, resulting in decreased cell viability in culture (PMID: 26996308). 26996308
NRAS G75_E76insDSAMRDQYMRTG myelodysplastic/myeloproliferative neoplasm sensitive PD-0325901 Preclinical Actionable In a preclinical study, PD-0325901 decreased the accumulation of immature myeloid cells in a zebrafish model of myelodysplastic/myeloproliferative neoplasm harboring NRAS G75_E76insDSAMRDQYMRTG (PMID: 38522505). 38522505
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 glioblastoma conflicting PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, PD-0325901 inhibited growth of glioblastoma cell lines harboring BRAF V600E in culture (PMID: 38714355). 38714355
BRAF V600E glioblastoma conflicting 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
BRAF N486_P490del ovarian cancer sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, an ovarian cancer cell line harboring BRAF N486_P490del demonstrated sensitivity to PD-0325901, resulting in decreased cell viability in culture (PMID: 26996308). 26996308
BRAF V600E MAP2K1 L115P melanoma resistant PD-0325901 Preclinical Actionable In a preclinical study, overexpression of MAP2K1 L115P in melanoma cells harboring BRAF V600E resulted in insensitivity to growth inhibition by PD-0325901 in cell culture (PMID: 26267534). 26267534
NRAS Q61R melanoma sensitive PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, PD-0325901 treatment induced cell cycle arrest and inhibited growth of melanoma cells harboring NRAS Q61R in culture (PMID: 25422890). 25422890
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
BRAF V600E MAP2K1 I103N melanoma resistant PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, overexpression of MAP2K1 I103N in melanoma cells harboring BRAF V600E resulted in insensitivity to growth inhibition by PD-0325901 in cell culture (PMID: 26267534). 26267534
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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
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 USA | ITA | ESP | CAN 0
NCT03962543 Phase II PD-0325901 MEK Inhibitor Mirdametinib (PD-0325901) in Patients With Neurofibromatosis Type 1 Associated Plexiform Neurofibromas (ReNeu) Active, not recruiting USA 0
NCT04923126 Phase Ib/II PD-0325901 SJ901: Evaluation of Mirdametinib in Children, Adolescents, and Young Adults With Low-Grade Glioma Recruiting USA 0
NCT02096471 Phase II PD-0325901 MEK Inhibitor PD-0325901 Trial in Adolescents and Adults With NF1 Completed USA 0


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