Therapy Detail

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Therapy Name ASTX029
Synonyms
Therapy Description

ASTX029 is an ERK1/2 inhibitor that prevents MAPK/ERK pathway activation, which may result in growth inhibition and tumor regression (PMID: 34330842).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
ASTX029 ASTX-029|ASTX 029 ERK Inhibitor (pan) 18 ERK1 Inhibitor 2 ERK2 Inhibitor 2 ASTX029 is an ERK1/2 inhibitor that prevents MAPK/ERK pathway activation, which may result in growth inhibition and tumor regression (PMID: 34330842).

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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600D melanoma sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, ASTX029 treatment inhibited growth of a melanoma cell line harboring BRAF V600D in culture (PMID: 34330842). 34330842
BRAF V600E melanoma sensitive ASTX029 Preclinical - Cell line xenograft Actionable In a preclinical study, ASTX029 treatment reduced Erk and Rsk phosphorylation, induced cell-cycle arrest, and inhibited growth of a melanoma cell line harboring BRAF V600E in culture and inhibited tumor growth in cell line xenograft models, and was also effective against cells with acquired resistance to Zelboraf (vemurafenib) or Koselugo (selumetinib) (PMID: 34330842). 34330842
FLT3 exon 14 ins acute myeloid leukemia sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cell lines harboring FLT3-ITD mutations were sensitive to treatment with ASTX029 in culture (PMID: 34330842). 34330842
NRAS Q61K melanoma sensitive ASTX029 Preclinical - Pdx Actionable In a preclinical study, ASTX029 treatment inhibited growth of melanoma cell lines harboring NRAS Q61K in culture, and inhibited tumor growth in a patient-derived xenograft (PDX) model of melanoma harboring NRAS Q61K (PMID: 34330842). 34330842
NRAS G13D melanoma sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, ASTX029 treatment inhibited growth of a melanoma cell line harboring NRAS G13D in culture (PMID: 34330842). 34330842
NRAS G12D acute myeloid leukemia sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring NRAS G12D were sensitive to treatment with ASTX029 in culture (PMID: 34330842). 34330842
BRAF V600E NRAS Q61K melanoma sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, ASTX029 treatment reduced Erk and Rsk phosphorylation and inhibited growth of a melanoma cell line harboring BRAF V600E and expressing NRAS Q61K in culture (PMID: 34330842). 34330842
NRAS G12D melanoma sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, ASTX029 treatment inhibited growth of a melanoma cell line harboring NRAS G12D in culture (PMID: 34330842). 34330842
NRAS Q61L acute myeloid leukemia sensitive ASTX029 Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring NRAS Q61L were sensitive to treatment with ASTX029 in culture (PMID: 34330842). 34330842
BRAF V600E colorectal adenocarcinoma sensitive ASTX029 Preclinical - Cell line xenograft Actionable In a preclinical study, ASTX029 treatment reduced Erk and Rsk phosphorylation and inhibited growth of colorectal adenocarcinoma cell lines harboring BRAF V600E in culture, and inhibited tumor growth and induced tumor regression in cell line xenograft models (PMID: 34330842). 34330842
NRAS Q61R melanoma sensitive ASTX029 Preclinical - Cell line xenograft Actionable In a preclinical study, ASTX029 treatment inhibited growth of melanoma cell lines harboring NRAS Q61R in culture, and inhibited tumor growth in cell line xenograft models (PMID: 34330842). 34330842

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03520075 Phase Ib/II ASTX029 Study of ASTX029 in Subjects With Advanced Solid Tumors Recruiting USA | FRA | ESP 1


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