Therapy Detail

Request Content

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@genomenon.com

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).

Filtering

Case insensitive filtering will display rows if any text in any cell matches the filter term
Use simple literal full or partial string matches
Separate multiple filter terms with a space. Any order may be used (i. e. 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 on a longer phrase with spaces (i.e. "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.

Filter rows:

Showing 1 to 1 of 1 entries

Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
ASTX029		ASTX-029\|ASTX 029	ERK Inhibitor (pan) 21 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).

Showing 1 to 1 of 1 entries

Filter rows:

Filtering

Case insensitive filtering will display rows if any text in any cell matches the filter term
Use simple literal full or partial string matches
Separate multiple filter terms with a space. Any order may be used (i. e. 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 on a longer phrase with spaces (i.e. "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.

Filter rows:

Showing 1 to 12 of 12 entries

Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
NRAS Q61K	ovary adenocarcinoma	predicted - sensitive	ASTX029	Case Reports/Case Series	Actionable	In a Phase II trial, ASTX029 treatment was well tolerated in patients with relapsed/refractory gynecological tumors harboring MAPK pathway alterations, and resulted in an objective response rate of 12.5% (4/32, all partial responses), a median duration of response of 8.5 months, and a median overall survival of 11.2 months, with a partial response in a patient with ovarian adenocarcinoma harboring NRAS Q61K who progressed on prior MEKi therapy (Ann Oncol (2024) 35 (Suppl_2): S591; NCT03520075).	detail...
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
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
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
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 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
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 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
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 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 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

Showing 1 to 12 of 12 entries

Filter rows:

Filtering

Case insensitive filtering will display rows if any text in any cell matches the filter term
Use simple literal full or partial string matches
Separate multiple filter terms with a space. Any order may be used (i. e. 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 on a longer phrase with spaces (i.e. "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.

Filter rows:

Showing 1 to 2 of 2 entries

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	Active, not recruiting	USA \| GBR \| FRA \| ESP	0
NCT06284460	Phase Ib/II	ASTX029 ASTX029 + Decitabine and Cedazuridine	Phase I/II Study of a Combination of Decitabine and Cedazuridine (ASTX727) and ASTX029, an ERK Inhibitor, for Patients With RAS Pathway Mutant Myelodysplastic Syndromes and Myelodysplastic/Myeloproliferative Neoplasms	Withdrawn	USA	0

Showing 1 to 2 of 2 entries

Filter rows:

Additional content available in CKB BOOST