Name:
Olutasidenib
CAS: 1887014-12-1
Develop Company: Rigel Pharmaceuticals
Indication: Acute myeloid leukemia
English trade name: REZLIDHIA
FDA approval date: December 1, 2022
Formulation: Capsules 150mg
2102-HEM-101 (NCT02719574) Test
Trial Information
147 adult patients with relapsed or resistant AML who had the IDH1 mutation were enrolled in the clinical trial.
Olutasidenib was given orally at a dose of 150 mg twice daily until the disease progressed, unacceptable toxicity developed, or a hematopoietic stem cell transplant was performed. The average length of treatment was 4.7 months (range: 0.1-26 months). Following olutasidenib therapy, sixteen patients underwent hematopoietic stem cell transplantation.
Trial results
In adult patients with recurrent or refractory AML having the IDH1 mutation, the combined rate of complete remission (CR) + complete remission with partial hematological (CRh) remission was 35%, with CR at 32% and CRh at 2.7%. The median length of remission was 25.9 months (95% CI: 13.5 months, not attained), with a median time to CR+CRh of 1.9 months (range: 0.9-5.6 months).
Rezlidhia showed good tolerance, with side effects characterized by symptoms and characteristics similar to those seen in treated AML patients. In 16% of individuals, fractionation syndrome was found, which could be controlled in most cases by discontinuing dosage and using corticosteroids. Hepatotoxicity, shown by increased liver function markers in 23% of patients, was manageable in most cases by dosage modification. By 56 days after baseline, 29 (34%) of the 86 patients who were dependent on red blood cell (RBC) and/or platelet transfusions were non-reliant on RBC and platelet transfusions. 39 (64%) of the 61 patients who did not require RBC and platelet transfusions at baseline were transfusion-independent for 56 days beyond baseline.
Olutasidenib synthetic route
Reference: WO2016044789
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