{"id":179,"date":"2014-06-14T08:10:32","date_gmt":"2014-06-14T12:10:32","guid":{"rendered":"http:\/\/blogs.shu.edu\/cancer\/?p=179"},"modified":"2021-07-02T08:52:01","modified_gmt":"2021-07-02T12:52:01","slug":"idh1-and-idh2-inhibitors","status":"publish","type":"post","link":"http:\/\/blogs.shu.edu\/cancer\/2014\/06\/14\/idh1-and-idh2-inhibitors\/","title":{"rendered":"IDH1 and IDH2 inhibitors"},"content":{"rendered":"

IDH1 and IDH2 are enzymes in the Krebs Cycle of glucose metabolism – IDH1 (AG-120) is active in the cyotplasm and IDH2 (AG-221) is active in the mitochondria. \u00a0Phase 1 clinical studies of these compounds are underway.<\/p>\n

Mutated forms of these enzymes are seen in hematological malignancies, and sold tumors, notably AML. \u00a0The metabolite produced by the mutated enzymes, 2HG (2-hydroxyglutarate), cause epigenetic changes that block the normal differentiation of cells, which prevents them from entering the post-mitotic state, which leads to cancer. \u00a0Thus, 2HG is an “oncometabolite.” \u00a0(See\u00a0http:\/\/www.agios.com\/pipeline-idh.php<\/a>)<\/p>\n

 <\/p>\n

\"IDH-graphic\"<\/a><\/p>\n

As reported at the 2014 ASCO meeting, 6 of 7 patients in the Phase 1 study of AG-221 had objective responses.<\/p>\n

Celgene, a leading oncology company with a robust portfolio and pipeline of cancer treatments, licensed the compounds. (see\u00a0http:\/\/www.marketwatch.com\/story\/agios-pharmaceuticals-announces-that-celgene-exercised-its-option-to-license-ag-221-under-global-strategic-collaboration-2014-06-13<\/a>)<\/p>\n","protected":false},"excerpt":{"rendered":"

IDH1 and IDH2 are enzymes in the Krebs Cycle of glucose metabolism – IDH1 (AG-120) is active in the cyotplasm and IDH2 (AG-221) is active in the mitochondria. \u00a0Phase 1 clinical studies of these compounds are underway.<\/p>\n","protected":false},"author":2252,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_monsterinsights_skip_tracking":false,"_monsterinsights_sitenote_active":false,"_monsterinsights_sitenote_note":"","_monsterinsights_sitenote_category":0,"footnotes":""},"categories":[428,25,24,1],"tags":[107,108,109,105,106,104],"class_list":["post-179","post","type-post","status-publish","format-standard","hentry","category-cellular-metabolism","category-epigenetic-regulation","category-mutations","category-uncategorized","tag-2hg","tag-agios","tag-differentiation","tag-idh1","tag-idh2","tag-oncometabolite"],"post_mailing_queue_ids":[],"_links":{"self":[{"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/posts\/179","targetHints":{"allow":["GET"]}}],"collection":[{"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/users\/2252"}],"replies":[{"embeddable":true,"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/comments?post=179"}],"version-history":[{"count":4,"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/posts\/179\/revisions"}],"predecessor-version":[{"id":5029,"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/posts\/179\/revisions\/5029"}],"wp:attachment":[{"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/media?parent=179"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/categories?post=179"},{"taxonomy":"post_tag","embeddable":true,"href":"http:\/\/blogs.shu.edu\/cancer\/wp-json\/wp\/v2\/tags?post=179"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}