Last reviewed 2026-04-20 · How we verify

Rezlidhia (OLUTASIDENIB)

Olutasidenib inhibits mutated IDH1, reducing 2-HG levels in AML cells.

Rezlidhia (OLUTASIDENIB) is a small molecule developed by Rigel Pharms, targeting the isocitrate dehydrogenase [NADP] cytoplasmic enzyme. It was FDA-approved in 2022 for the treatment of acute myeloid leukemia, specifically in patients with a susceptible IDH1 mutation. Rezlidhia is a patented medication with no generic manufacturers available. Key safety considerations include the need for monitoring of adverse reactions, and it is essential to follow the recommended dosage. Rezlidhia is a targeted therapy that aims to inhibit the mutated IDH1 enzyme, thereby reducing the production of a toxic metabolite that contributes to cancer progression.

At a glance

Mechanism of action

Olutasidenib targets specific mutations in the IDH1 enzyme that are common in AML, such as R132H and R132C. By inhibiting these mutated enzymes, it reduces the production of 2-HG, a compound that contributes to the disease. This leads to clinical improvements in patients.

Approved indications

• Acute myeloid leukemia, disease
• Refractory acute myeloid leukemia with a susceptible IDH1 mutation
• Relapsing acute myeloid leukemia with a susceptible IDH1 mutation

Boxed warnings

• WARNING: DIFFERENTIATION SYNDROME Differentiation syndrome, which can be fatal, can occur with REZLIDHIA treatment. Symptoms may include dyspnea, pulmonary infiltrates/pleuropericardial effusion, kidney injury, hypotension, fever, and weight gain. If differentiation syndrome is suspected, withhold REZLIDHIA and initiate treatment with corticosteroids and hemodynamic monitoring until symptom resolution [see Warnings and Precautions ( 5.1 )] . WARNING: DIFFERENTIATION SYNDROME See full prescribing information for complete boxed warning. Differentiation syndrome, which can be fatal, can occur with REZLIDHIA treatment. If differentiation syndrome is suspected, withhold REZLIDHIA and initiate corticosteroids and hemodynamic monitoring until symptom resolution. ( 5.1 )

Common side effects

• Differentiation syndrome
• Transaminitis
• Nausea
• Fatigue/malaise
• Arthralgia
• Constipation
• Lymphocytes increased
• Bilirubin increased
• Leukocytosis
• Uric acid increased
• Dyspnea
• Pyrexia

Key clinical trials

• MYELOMATCH: A Screening Study to Assign People With Myeloid Cancer to a Treatment Study or Standard of Care Treatment Within myeloMATCH (MyeloMATCH Screening Trial) (PHASE2)
• Testing the Use of an IDH1 Inhibitor, Olutasidenib, in Acute Myeloid Leukemia Added to ASTX727 and Venetoclax; in High-Risk MDS Added to ASTX727; and Alone in Low Risk MDS (A MyeloMATCH Treatment Substudy) (PHASE2)
• Olutasidenib DDI Study in Patients With IDH1 Mutation Positive Malignancies (PHASE4)
• Olutasidenib in Relapsed IDH1 Mutated AML Patients Who Have Previously Received Venetoclax (PHASE2)
• Olutasidenib for the Treatment of Patients With IDH1 Mutated AML, MDS or CMML After Donor Hematopoietic Cell Transplant (PHASE1)
• Olutasidenib With Azacitidine Followed by Olutasidenib Maintenance for the Treatment of IDH1-mutated Acute Myeloid Leukemia in Patients With Prior Treatment With Venetoclax Plus a Hypomethylating Agent (PHASE2)
• A Phase II Open-label Study of Olutasidenib Post-transplant Maintenance Therapy for Patients With IDH1-mutated Myeloid Malignancies (PHASE2)
• A Phase 2 Study Evaluating Olutasidenib in Patients With IDH1-mutated Clonal Cytopenia of Undetermined Significance and Lower-risk Myelodysplastic/Syndromes/Chronic Myelomonocytic Leukemia. (PHASE2)

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Rezlidhia CI brief — competitive landscape report
• Rezlidhia updates RSS · CI watch RSS
• Rigel Pharms portfolio CI