General
Preferred name
Olutasidenib
Synonyms
FT-2102 ()
Olutasidenib (FT-2102) ()
Rezlidhia ()
P&D ID
PD098094
CAS
1887014-12-1
Tags
available
drug
Approved by
FDA
First approval
2022
Drug Status
approved
investigational
Max Phase
4.0
Drug indication
Myelodysplastic syndrome
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1][2].
PRICE 216
DESCRIPTION Olutasidenib (FT-2102) is an orally available and brain penetrant inhibitor of mutant IDH1 that is being developed by Forma Therapeutics for antineoplastic potential . Activating mutations in IDH1 (e.g. IDH1R132H) drive cancer initiation and growth by enhancing the formation of the oncometabolite 2-hydroxyglutarate (2HG) . Pharmacological inhibition of mutant IDH1 blocks 2HG production as a means to restore normal cellular differentiation. This is the same mechanism of action as (Tibsovo®) that was FDA approved in 2018.
FT-2102 is claimed as example 26 (I-14) in Forma Tm2's patent US9834539B2 . (GtoPdb)
DESCRIPTION Olutasidenib is a mutant isocitrate dehydrogenase 1 (IDH1) inhibitor used to treat acute myeloid leukemia. (BOC Sciences Bioactive Compounds)
DESCRIPTION Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively). (TargetMol Bioactive Compound Library)
Compound Sets
12
BOC Sciences Bioactive Compounds
olutasidenib-cas-1887014-12-1-373144
Cayman Chemical Bioactives
30370
ChEMBL Approved Drugs
CHEMBL4297610
ChEMBL Drugs
CHEMBL4297610
DrugBank
DB16267
DrugBank Approved Drugs
DB16267
DrugCentral
5693
DrugCentral Approved Drugs
5693
Guide to Pharmacology
10319
MedChem Express Bioactive Compound Library
HY-114226
Selleckchem Bioactive Compound Library
olutasidenib-ft-2102
TargetMol Bioactive Compound Library
T16384
External IDs
18
Properties
(calculated by RDKit )
Molecular Weight
354.09
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
3
cLogP
2.92
TPSA
90.68
Fraction CSP3
0.17
Chiral centers
1.0
Largest ring
6.0
QED
0.76
QED
0.76
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Isocitrate Dehydrogenase (IDH)
Dehydrogenase
R132C-IDH1
R132H-IDH1
Pathway
Metabolism
Metabolic Enzyme/Protease
Solubility
Soluble in DMSO
Source data