Onureg

Acute myeloid leukemia (AML) — continued treatment (maintenance) in adult patients who achieved first complete remission (CR) or complete remission with incomplete blood count recovery (CRi) following intensive induction chemotherapy and are not able to complete intensive curative therapy

300 mg orally once daily on Days 1-14 of each 28-day cycle
Continue until disease progression or unacceptable toxicity
Take with or without food at approximately the same time each day
Swallow whole with water; do not split, crush, or chew
Administer antiemetic 30 minutes before each dose for the first 2 cycles

Tablets: 200 mg, 300 mg

Hypersensitivity to azacitidine or mannitol.

• Myelosuppression: Neutropenia (41%), thrombocytopenia (22%), anemia (14%). Monitor CBCs before start of therapy and before each cycle. Delay cycles for persistent toxicity.
• Increased Early Mortality in MDS Patients: Not indicated for MDS. Increased early mortality in MDS clinical trial.
• Gastrointestinal Toxicity: Nausea (65%), vomiting (60%), diarrhea (50%). Pre-medicate with antiemetics.
• NOT interchangeable with injectable azacitidine
• Embryo-Fetal Toxicity

Nausea (65%), vomiting (60%), diarrhea (50%), fatigue (44%), constipation (39%), pneumonia (22%), abdominal pain (22%), arthralgia (14%), decreased appetite (13%), febrile neutropenia (12%), dizziness (11%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Oral azacitidine is a nucleoside metabolic inhibitor. After cellular uptake and conversion to its active triphosphate form (decitabine triphosphate), it is incorporated into DNA, where it inhibits DNA methyltransferase (DNMT), leading to DNA hypomethylation. At low doses, this epigenetic modulation restores expression of silenced tumor suppressor genes, promoting cellular differentiation and apoptosis in leukemia cells. At higher concentrations, it is directly cytotoxic through incorporation into DNA and RNA.

Tmax: 1 hour. Half-life: approximately 0.5 hours (azacitidine oral rapidly degraded). Oral bioavailability ~11%. Not significantly metabolized by CYP enzymes; cleared by spontaneous hydrolysis and deamination by cytidine deaminase. Excreted primarily in urine.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• QUAZAR AML-001 — Oral azacitidine maintenance vs. placebo in AML in first remission. Phase III, n=472.
  🔬 NCT01757535 ↗ 📄 Primary Publication ↗

Onureg has FDA-approved indications across the following cancer types covered on PipelineEvidence: