olutasidenib   Click here for help

GtoPdb Ligand ID: 10319

Synonyms: example 26 [US9834539B2] | FT-2102 | FT2102 | Rezlidhia®
Approved drug PDB Ligand
olutasidenib is an approved drug (FDA (2022))
Compound class: Synthetic organic
Comment: Olutasidenib (FT-2102) is an orally available and brain penetrant inhibitor of mutant IDH1 that is being developed by Forma Therapeutics for antineoplastic potential [1]. Activating mutations in IDH1 (e.g. IDH1R132H) drive cancer initiation and growth by enhancing the formation of the oncometabolite 2-hydroxyglutarate (2HG) [4]. Pharmacological inhibition of mutant IDH1 blocks 2HG production as a means to restore normal cellular differentiation. This is the same mechanism of action as ivosidenib (Tibsovo®) that was FDA approved in 2018.
FT-2102 is claimed as example 26 (I-14) in Forma Tm2's patent US9834539B2 [3].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 2
Hydrogen bond donors 2
Rotatable bonds 3
Topological polar surface area 90.68
Molecular weight 354.09
XLogP 4.41
No. Lipinski's rules broken 0
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Canonical SMILES N#Cc1ccc(c(=O)n1C)NC(c1cc2cc(Cl)ccc2[nH]c1=O)C
Isomeric SMILES N#Cc1ccc(c(=O)n1C)N[C@H](c1cc2cc(Cl)ccc2[nH]c1=O)C
InChI InChI=1S/C18H15ClN4O2/c1-10(21-16-6-4-13(9-20)23(2)18(16)25)14-8-11-7-12(19)3-5-15(11)22-17(14)24/h3-8,10,21H,1-2H3,(H,22,24)/t10-/m0/s1
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Summary of Clinical Use Click here for help
FT-2102 was evaluated in clinical trials as a monotherapy or in conjunction with other chemotherapeutics (e.g. azacitidine or cytarabine), in patients with solid or liquid tumours that carry IDH1 mutations. It has been estimated that IDH1 mutations are present in 6-8% of patients with AML, and in approximately 80% of patients with grade 2 and 3 gliomas and secondary glioblastoma. Click here to link to ClinicalTrials.gov's full list of FT-2102 trials. First FDA approval was granted in December 2022 [2], for the treatment of relapsed/refractory IDH1 mutation-positive acute myeloid leukemia (AML).
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03684811 A Study of FT 2102 in Participants With Advanced Solid Tumors and Gliomas With an IDH1 Mutation Phase 1/Phase 2 Interventional Forma Therapeutics, Inc.
NCT02719574 Open-label Study of FT-2102 With or Without Azacitidine or Cytarabine in Patients With AML or MDS With an IDH1 Mutation Phase 1/Phase 2 Interventional Forma Therapeutics, Inc. 5