Product Overview
Olutasidenib is a selective, orally active isocitrate dehydrogenase-1 (IDH1) inhibitor developed for targeted treatment of acute myeloid leukemia (AML) associated with susceptible IDH1 mutations.
Olutasidenib is also known by its development code FT-2102. It is marketed as an oral pharmaceutical product for adult patients with relapsed or refractory AML carrying a susceptible IDH1 mutation. The FDA approved olutasidenib in December 2022.
Olutasidenib is a small-molecule pharmaceutical compound with the molecular formula C18H15ClN4O2 and molecular weight 354.79 g/mol. It is described as a white to off-white to brown powder and is practically insoluble in aqueous solutions between pH 1.2 and 7.4.
Chemical Information
- Product Name: Olutasidenib
- Development Code: FT-2102
- CAS Number: 1887014-12-1
- UNII: 0T4IMT8S5Z
- Molecular Formula: C18H15ClN4O2
- Molecular Weight: 354.79 g/mol
- Chemical Class: Small-molecule IDH1 inhibitor
- Therapeutic Class: Antineoplastic agent
- Stereochemical Form: S-enantiomer
- Physical Form: White to off-white to brown powder
- Solubility: Practically insoluble in aqueous solutions between pH 1.2 and 7.4
- Development Name: FT-2102
The FDA GSRS database identifies olutasidenib under CAS 1887014-12-1 and confirms its molecular formula and stereochemical identity.
Mechanism of Action
Olutasidenib works by selectively inhibiting susceptible mutant forms of IDH1.
- Mutations in IDH1 can cause abnormal production of the oncometabolite 2-hydroxyglutarate (2-HG).
- Increased 2-HG can interfere with normal cellular differentiation.
- Olutasidenib inhibits susceptible mutant IDH1 enzymes.
- This reduces abnormal 2-HG production.
- Reduction of 2-HG can promote differentiation of leukemic cells.
- In vitro studies demonstrated inhibition of IDH1 R132H, R132L, R132S, R132G and R132C variants.
- Wild-type IDH1 and mutant IDH2 were not inhibited in the FDA-described studies.
Key Features
- Selective mutant IDH1 inhibitor
- Small-molecule oncology API
- Development code FT-2102
- CAS No. 1887014-12-1
- Molecular formula C18H15ClN4O2
- Molecular weight 354.79 g/mol
- S-enantiomerically defined pharmaceutical compound
- Developed for IDH1-mutated AML
- Practically insoluble in aqueous solutions between pH 1.2 and 7.4
- Suitable for HPLC, LC-MS, NMR and IR characterization
- Chiral analytical testing is relevant because of the defined stereochemical configuration
- Solid-state characterization is relevant for pharmaceutical development
Pharmaceutical Applications
Olutasidenib is primarily associated with:
- Acute myeloid leukemia treatment
- IDH1-mutated AML therapy
- Targeted oncology drug development
- IDH1 inhibitor research
- Pharmaceutical formulation development
- Analytical reference-standard development
- Related-substance and degradation-product studies
- Stability-indicating analytical method development
The FDA-approved indication is for adult patients with relapsed or refractory AML with a susceptible IDH1 mutation detected using an FDA-approved diagnostic test.
Physicochemical Properties
- Appearance: White to off-white to brown powder
- Molecular Weight: 354.79 g/mol
- Molecular Formula: C18H15ClN4O2
- Aqueous Solubility: Practically insoluble
- pH Solubility Range: pH 1.2–7.4
- Stereochemistry: S configuration
- CAS: 1887014-12-1
- Solid State: Crystalline pharmaceutical solid forms have been reported
The aqueous solubility description and physical appearance are directly reported in the current FDA/DailyMed product information.
Analytical Characterization
Olutasidenib can be characterized using several analytical techniques:
- HPLC
- LC-MS
- NMR spectroscopy
- FT-IR spectroscopy
- Chiral HPLC/SFC
- UV-Visible spectroscopy
- XRPD for solid-state characterization
- DSC/TGA for thermal and solid-form evaluation
For pharmaceutical development, chromatographic methods can be used to monitor assay and related substances, while chiral methods are particularly relevant for controlling the S-enantiomeric drug substance.
Impurity and Quality Control
Quality control of olutasidenib API may include:
- Identification
- Assay
- Related substances
- Degradation products
- Chiral purity
- Residual solvents
- Water content
- Elemental impurities
- Residual catalysts
- Solid-state form
- Stability-indicating chromatographic analysis
The FDA's general Q6A guidance recommends specific identity procedures and stability-indicating assays for new drug substances, with appropriate controls for organic and inorganic impurities and residual solvents.
Stereochemical Characteristics
Olutasidenib is specifically identified as the S-enantiomer. This makes stereochemical purity an important quality attribute for pharmaceutical-grade material.
The FDA GSRS record provides the stereochemical InChIKey and chemical identity corresponding to the S configuration.
Storage
Olutasidenib API should be stored in a tightly closed pharmaceutical container under controlled environmental conditions, protected from excessive moisture, heat and direct light.
Storage and retest conditions should ultimately follow the validated stability data and approved API specification.
Detailed Specifications
| Parameter |
Specification |
| Appearance |
White crystalline powder or crystals |
| Identification |
IR & HPLC compliant |
| Assay (HPLC) |
98.0% – 102.0% |
| Solubility |
Practically insoluble in aqueous solutions between pH 1.2 and 7.4 |
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