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Pills that block mutant IDH1 or IDH2 enzymes, which flood cells with a metabolite that blocks maturation; approved in leukaemia, bile duct cancer and low-grade glioma.
Mutations in isocitrate dehydrogenase 1 and 2 produce the oncometabolite 2-hydroxyglutarate, which blocks cell differentiation through epigenetic enzymes. Enasidenib (IDH2, 2017) and ivosidenib (IDH1, 2018) were approved in acute myeloid leukaemia, ivosidenib later in cholangiocarcinoma, olutasidenib in AML, and vorasidenib, which penetrates the brain, delayed progression of IDH-mutant low-grade glioma and was approved in 2024. Differentiation syndrome and resistance through second-site mutations are the class issues.
Allosteric inhibitors lock the mutant enzyme in an inactive state, lowering 2-hydroxyglutarate and restoring differentiation.
Enasidenib is the IDH2 counterpart of ivosidenib, approved in the US for relapsed disease but never approved in Europe after it failed to extend survival in a confirmatory trial.
The first drug to block a mutant metabolic enzyme in cancer. With azacitidine it tripled survival in IDH1-mutated AML that could not take intensive chemotherapy.
Olutasidenib is a second IDH1 inhibitor for relapsed AML, with a higher response rate in its pivotal cohort than ivosidenib had in its own.
The first targeted therapy for low-grade brain tumours, delaying the need for radiation and chemotherapy by years.
Query for this technology: (TITLE:"IDH inhibitors" OR ABSTRACT:"IDH inhibitors") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about IDH inhibitors, not a curated reading list.
Shares INDIGO, Olutasidenib, Enasidenib, Vorasidenib.
Shares An Early Access Study of Ivosidenib in Patients With a Pretreated Locally Advanced or Metastatic Cholangiocarcinoma, Ivosidenib in Participants With Locally Advanced or Metastatic Conventional Chondrosarcoma Untreated or Previously Treated With 1 Systemic Treatment Regimen, An Open-label Phase 3b Study of Ivosidenib in Combination With Azacitidine in Adult Patients Newly Diagnosed With IDH1m Acute Myeloid Leukemia (AML) Ineligible for Intensive Induction Chemotherapy., INDIGO.
Shares ClarIDHy, INDIGO, Olutasidenib, AGILE.
Shares Olutasidenib, Vorasidenib, Ivosidenib, Biliary tract cancer (cholangiocarcinoma).
Shares Study of Olutasidenib and Temozolomide in HGG, Olutasidenib, Acute myeloid leukaemia.
Shares Olutasidenib, AGILE, Enasidenib, Ivosidenib.
Shares INDIGO, Vorasidenib, Glioma & glioblastoma.
Shares INDIGO, Vorasidenib, Glioma & glioblastoma.