{"id":"https://openalex.org/W4307776249","doi":"https://doi.org/10.5582/ddt.2022.01085","title":"Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma","display_name":"Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma","publication_year":2022,"publication_date":"2022-10-27","ids":{"openalex":"https://openalex.org/W4307776249","doi":"https://doi.org/10.5582/ddt.2022.01085","pmid":"https://pubmed.ncbi.nlm.nih.gov/36310058"},"language":"en","primary_location":{"id":"doi:10.5582/ddt.2022.01085","doi":"https://doi.org/10.5582/ddt.2022.01085","is_oa":true,"landing_page_url":"https://doi.org/10.5582/ddt.2022.01085","pdf_url":"https://www.jstage.jst.go.jp/article/ddt/16/6/16_2022.01085/_pdf","source":{"id":"https://openalex.org/S2764561415","display_name":"Drug Discoveries & Therapeutics","issn_l":"1881-7831","issn":["1881-7831","1881-784X"],"is_oa":true,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","medline","poland-70","russia-white-list-2"],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Drug Discoveries &amp; Therapeutics","raw_type":"journal-article"},"volume":null,"type":"article","indexed_in":["crossref","pubmed"],"open_access":{"is_oa":true,"oa_status":"diamond","oa_url":"https://www.jstage.jst.go.jp/article/ddt/16/6/16_2022.01085/_pdf","any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5051706504","display_name":"Fangzhou Dou","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I108688024","display_name":"Qingdao University","ror":"https://ror.org/021cj6z65","country_code":"CN","type":"education","lineage":["https://openalex.org/I108688024"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Fangzhou Dou","raw_affiliation_strings":["Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China","institution_ids":["https://openalex.org/I108688024"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5074463034","display_name":"Zhenxue Tian","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210119987","display_name":"Qingdao Municipal Hospital","ror":"https://ror.org/02jqapy19","country_code":"CN","type":"healthcare","lineage":["https://openalex.org/I4210119987"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Zhenxue Tian","raw_affiliation_strings":["Department of Pharmacy, Qingdao Municipal Hospital, Qingdao, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Pharmacy, Qingdao Municipal Hospital, Qingdao, China","institution_ids":["https://openalex.org/I4210119987"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5104110494","display_name":"Xu Yang","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210119987","display_name":"Qingdao Municipal Hospital","ror":"https://ror.org/02jqapy19","country_code":"CN","type":"healthcare","lineage":["https://openalex.org/I4210119987"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Xu Yang","raw_affiliation_strings":["Department of Pharmacy, Qingdao Municipal Hospital, Qingdao, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Pharmacy, Qingdao Municipal Hospital, Qingdao, China","institution_ids":["https://openalex.org/I4210119987"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100336950","display_name":"Jing Li","orcid":"https://orcid.org/0000-0002-5748-3934","observed_orcids":["https://orcid.org/0000-0002-5748-3934"]},"institutions":[{"id":"https://openalex.org/I108688024","display_name":"Qingdao University","ror":"https://ror.org/021cj6z65","country_code":"CN","type":"education","lineage":["https://openalex.org/I108688024"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Jing Li","raw_affiliation_strings":["Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China","institution_ids":["https://openalex.org/I108688024"]}]},{"author_position":"middle","author":{"id":null,"display_name":"Ruquan Wang","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I108688024","display_name":"Qingdao University","ror":"https://ror.org/021cj6z65","country_code":"CN","type":"education","lineage":["https://openalex.org/I108688024"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Ruquan Wang","raw_affiliation_strings":["Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China","institution_ids":["https://openalex.org/I108688024"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5069915515","display_name":"Jianjun Gao","orcid":"https://orcid.org/0000-0001-6138-4472","observed_orcids":["https://orcid.org/0000-0001-6138-4472"]},"institutions":[{"id":"https://openalex.org/I108688024","display_name":"Qingdao University","ror":"https://ror.org/021cj6z65","country_code":"CN","type":"education","lineage":["https://openalex.org/I108688024"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Jianjun Gao","raw_affiliation_strings":["Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China","institution_ids":["https://openalex.org/I108688024"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":2,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":1.7163,"has_fulltext":true,"cited_by_count":24,"citation_normalized_percentile":{"value":0.84669004,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":99},"biblio":{"volume":"16","issue":"6","first_page":"297","last_page":"299"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T12159","display_name":"T-cell and Retrovirus Studies","score":0.8511000275611877,"subfield":{"id":"https://openalex.org/subfields/2403","display_name":"Immunology"},"field":{"id":"https://openalex.org/fields/24","display_name":"Immunology and Microbiology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T12159","display_name":"T-cell and Retrovirus Studies","score":0.8511000275611877,"subfield":{"id":"https://openalex.org/subfields/2403","display_name":"Immunology"},"field":{"id":"https://openalex.org/fields/24","display_name":"Immunology and Microbiology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10269","display_name":"Epigenetics and DNA Methylation","score":0.07800000160932541,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T13157","display_name":"Cancer-related gene regulation","score":0.005200000014156103,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/valemetostat","display_name":"valemetostat","score":0.9990000128746033},{"id":"https://openalex.org/keywords/adult-t-cell-leukemia-lymphoma","display_name":"adult T-cell leukemia/lymphoma","score":0.996999979019165},{"id":"https://openalex.org/keywords/h3k27me3","display_name":"H3K27me3","score":0.8450000286102295},{"id":"https://openalex.org/keywords/histone-methyltransferase-inhibitors","display_name":"histone methyltransferase inhibitors","score":0.8709999918937683},{"id":"https://openalex.org/keywords/drug-approval","display_name":"drug approval","score":0.5239999890327454},{"id":"https://openalex.org/keywords/hematologic-malignancies","display_name":"hematologic malignancies","score":0.6970000267028809},{"id":"https://openalex.org/keywords/solid-tumors","display_name":"solid tumors","score":0.6110000014305115}],"concepts":[{"id":"https://openalex.org/C50171091","wikidata":"https://www.wikidata.org/wiki/Q17917770","display_name":"EZH2","level":4,"score":0.8111171722412109},{"id":"https://openalex.org/C502942594","wikidata":"https://www.wikidata.org/wiki/Q3421914","display_name":"Cancer research","level":1,"score":0.622173547744751},{"id":"https://openalex.org/C2779338263","wikidata":"https://www.wikidata.org/wiki/Q208414","display_name":"Lymphoma","level":2,"score":0.5488149523735046},{"id":"https://openalex.org/C111936080","wikidata":"https://www.wikidata.org/wiki/Q913367","display_name":"Enhancer","level":4,"score":0.4815388321876526},{"id":"https://openalex.org/C2778461978","wikidata":"https://www.wikidata.org/wiki/Q29496","display_name":"Leukemia","level":2,"score":0.4334338307380676},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.3968013525009155},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.3124554753303528},{"id":"https://openalex.org/C203014093","wikidata":"https://www.wikidata.org/wiki/Q101929","display_name":"Immunology","level":1,"score":0.20544034242630005},{"id":"https://openalex.org/C64927066","wikidata":"https://www.wikidata.org/wiki/Q36293","display_name":"Histone","level":3,"score":0.19782117009162903},{"id":"https://openalex.org/C86339819","wikidata":"https://www.wikidata.org/wiki/Q407384","display_name":"Transcription factor","level":3,"score":0.07478025555610657},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.06934070587158203},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.0}],"mesh":[{"descriptor_ui":"D000328","descriptor_name":"Adult","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000627","qualifier_name":"therapeutic use","is_major_topic":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008223","descriptor_name":"Lymphoma","qualifier_ui":null,"qualifier_name":null,"is_major_topic":true},{"descriptor_ui":"D015459","descriptor_name":"Leukemia-Lymphoma, Adult T-Cell","qualifier_ui":"Q000188","qualifier_name":"drug therapy","is_major_topic":true},{"descriptor_ui":"D063151","descriptor_name":"Polycomb Repressive Complex 2","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.5582/ddt.2022.01085","doi":"https://doi.org/10.5582/ddt.2022.01085","is_oa":true,"landing_page_url":"https://doi.org/10.5582/ddt.2022.01085","pdf_url":"https://www.jstage.jst.go.jp/article/ddt/16/6/16_2022.01085/_pdf","source":{"id":"https://openalex.org/S2764561415","display_name":"Drug Discoveries & Therapeutics","issn_l":"1881-7831","issn":["1881-7831","1881-784X"],"is_oa":true,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","medline","poland-70","russia-white-list-2"],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Drug Discoveries &amp; Therapeutics","raw_type":"journal-article"},{"id":"pmid:36310058","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/36310058","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Drug discoveries & therapeutics","raw_type":"Journal Article"}],"best_oa_location":{"id":"doi:10.5582/ddt.2022.01085","doi":"https://doi.org/10.5582/ddt.2022.01085","is_oa":true,"landing_page_url":"https://doi.org/10.5582/ddt.2022.01085","pdf_url":"https://www.jstage.jst.go.jp/article/ddt/16/6/16_2022.01085/_pdf","source":{"id":"https://openalex.org/S2764561415","display_name":"Drug Discoveries & Therapeutics","issn_l":"1881-7831","issn":["1881-7831","1881-784X"],"is_oa":true,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","medline","poland-70","russia-white-list-2"],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Drug Discoveries &amp; Therapeutics","raw_type":"journal-article"},"sustainable_development_goals":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.9763000011444092}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":true,"grobid_xml":true},"content_urls":{"pdf":"https://content.openalex.org/works/W4307776249.pdf","grobid_xml":"https://content.openalex.org/works/W4307776249.grobid-xml"},"referenced_works_count":19,"referenced_works":["https://openalex.org/W2042093631","https://openalex.org/W2134170049","https://openalex.org/W2310558276","https://openalex.org/W2316418663","https://openalex.org/W2317684406","https://openalex.org/W2550825807","https://openalex.org/W2738573788","https://openalex.org/W2782727153","https://openalex.org/W2985567193","https://openalex.org/W2991638976","https://openalex.org/W2995760187","https://openalex.org/W2999309243","https://openalex.org/W3045753156","https://openalex.org/W3089190403","https://openalex.org/W3176651739","https://openalex.org/W3179009923","https://openalex.org/W4281719344","https://openalex.org/W4282927137","https://openalex.org/W4296848301"],"related_works":["https://openalex.org/W2983431477","https://openalex.org/W3211957689","https://openalex.org/W4310113833","https://openalex.org/W4409632168","https://openalex.org/W4309107837","https://openalex.org/W3214025529","https://openalex.org/W3211922817","https://openalex.org/W4406069068","https://openalex.org/W4296848301","https://openalex.org/W4389233718"],"abstract_inverted_index":{"Adult":[0],"T-cell":[1,7],"leukemia/lymphoma":[2],"(ATL)":[3],"is":[4,62,72],"a":[5,10,63],"mature":[6],"lymphoma":[8],"with":[9],"poor":[11],"prognosis.":[12],"Accumulating":[13],"trimethylation":[14],"of":[15,25,28,44,51,81],"histone":[16],"H3":[17],"lysine":[18],"27":[19],"(H3K27me3)":[20],"caused":[21],"by":[22],"upregulated":[23],"function":[24],"either":[26],"enhancer":[27],"zeste":[29],"homologue":[30],"2":[31],"(EZH2)":[32],"or":[33],"its":[34],"homolog":[35],"EZH1":[36,56],"plays":[37],"an":[38],"essential":[39],"role":[40],"in":[41,47,66,84,86,104,116],"the":[42,73],"maintenance":[43],"transcriptional":[45],"repression":[46],"ATL.":[48],"Selective":[49],"inhibition":[50],"EZH2":[52],"may":[53,111],"complementarily":[54],"induce":[55],"activation,":[57],"so":[58],"dual":[59,75,91],"targeting":[60,109],"EZH1/2":[61,76,92,110],"rational":[64],"strategy":[65],"developing":[67],"potent":[68],"antitumor":[69,114],"agents.":[70],"Valemetostat":[71],"first":[74],"inhibitor":[77],"approved":[78],"for":[79],"treatment":[80],"aggressive":[82],"ATL":[83],"Japan":[85],"September":[87],"2022.":[88],"Several":[89],"other":[90],"inhibitors":[93],"such":[94],"as":[95],"HH2853,":[96],"HM97594,":[97],"and":[98,119],"HM97662":[99],"have":[100,112],"also":[101],"demonstrated":[102],"potential":[103],"treating":[105],"malignant":[106],"tumors.":[107,121],"Dual":[108],"promising":[113],"action":[115],"hematological":[117],"malignancies":[118],"solid":[120]},"counts_by_year":[{"year":2026,"cited_by_count":6},{"year":2025,"cited_by_count":5},{"year":2024,"cited_by_count":7},{"year":2023,"cited_by_count":5},{"year":2022,"cited_by_count":1}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2022-11-05T00:00:00"}
