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Olutasidenib

Generic Name
Olutasidenib
Brand Names
Rezlidhia
Drug Type
Small Molecule
Chemical Formula
C18H15ClN4O2
CAS Number
1887014-12-1
Unique Ingredient Identifier
0T4IMT8S5Z

Overview

Olutasidenib (FT-2102) is a selective and potent isocitrate dehydrogenase-1 (IDH1) inhibitor approved by the FDA in December 2022. It is indicated for the treatment of relapsed or refractory acute myeloid leukemia (AML) in patients with a susceptible IDH1 mutation as determined by an FDA-approved test. IDH1 mutations are common in different types of cancer, such as gliomas, AML, intrahepatic cholangiocarcinoma, chondrosarcoma, and myelodysplastic syndromes (MDS), and they lead to an increase in 2-hydroxyglutarate (2-HG), a metabolite that participates in tumerogenesis. Olutasidenib inhibits the mutated IDH1 specifically, and provides a therapeutic benefit in IDH1-mutated cancers. Other IDH1 inhibitors, such as ivosidenib, have also been approved for the treatment of relapsed or refractory AML. Olutasidenib is orally bioavailable and capable of penetrating the blood-brain barrier, and is also being evaluated for the treatment of myelodysplastic syndrome (MDS), as well as solid tumors and gliomas (NCT03684811).

Background

Olutasidenib (FT-2102) is a selective and potent isocitrate dehydrogenase-1 (IDH1) inhibitor approved by the FDA in December 2022. It is indicated for the treatment of relapsed or refractory acute myeloid leukemia (AML) in patients with a susceptible IDH1 mutation as determined by an FDA-approved test. IDH1 mutations are common in different types of cancer, such as gliomas, AML, intrahepatic cholangiocarcinoma, chondrosarcoma, and myelodysplastic syndromes (MDS), and they lead to an increase in 2-hydroxyglutarate (2-HG), a metabolite that participates in tumerogenesis. Olutasidenib inhibits the mutated IDH1 specifically, and provides a therapeutic benefit in IDH1-mutated cancers. Other IDH1 inhibitors, such as ivosidenib, have also been approved for the treatment of relapsed or refractory AML. Olutasidenib is orally bioavailable and capable of penetrating the blood-brain barrier, and is also being evaluated for the treatment of myelodysplastic syndrome (MDS), as well as solid tumors and gliomas (NCT03684811).

Indication

Olutasidenib is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test.

Associated Conditions

  • Refractory Acute Myeloid Leukemia (AML)
  • Relapsed Acute Myelogenous Leukemia (AML)

FDA Approved Products

REZLIDHIA
Manufacturer:Rigel Pharmaceuticals, Inc.
Route:ORAL
Strength:150 mg in 1 1
Approved: 2022/12/08
NDC:71332-005

Singapore Approved Products

No Singapore products found for this drug

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