Chinese Name: Quizartinib Tablets

Trade Names: Vanflyta, Weifeita, ZAGUDX

Generic Name: Quizartinib Tablets

Specifications: 17.7 mg × 28 tablets/box; 26.5 mg × 28 tablets/box

Manufacturer: Bigbear Pharmaceutical Laos

Drug Approval Numbers: 06L 1362/25; 06L 1361/25

[Composition]

Active Ingredient: Quizartinib

Chemical Name: N-[3-(Trifluoromethyl)phenyl]-5-aminoquinazoline-4-carboxamide

Molecular Formula: C₁₆H₁₁F₃N₄O

[Indications]

For the treatment of:

Newly diagnosed FLT3-ITD-positive Acute Myeloid Leukemia (AML) in adults, in combination with cytarabine and an anthracycline for induction, in combination with cytarabine for consolidation, and as monotherapy for maintenance following consolidation.

Not indicated for: Maintenance therapy following allogeneic hematopoietic stem cell transplantation (HSCT).

[Dosage and Administration]

Swallow tablets whole; may be taken with or without food, once daily at a fixed time.

1. Induction Therapy (28 days/cycle; Cycles 1–2)

35.4 mg, taken on Days 8–21 (total 14 days).

2. Consolidation Therapy (28 days/cycle; ≤ 4 cycles)

35.4 mg, taken on Days 6–19 (total 14 days).

3. Maintenance Therapy (≤ 36 cycles; continuous)

Cycle 1, Days 1–14: 26.5 mg/day.

From Day 15 onwards: If QTcF ≤ 450 ms, increase to 53 mg/day.

If QTcF > 500 ms during the induction/consolidation phase: Maintain at 26.5 mg/day.

4. Dose Adjustments

QTcF 481–500 ms: Dose reduction (53 → 35.4 mg; 35.4 → 26.5 mg)

QTcF > 500 ms: Discontinue treatment; resume at a reduced dose once QTcF < 450 ms

Concomitant use with strong CYP3A inhibitors: 53 → 26.5 mg; 35.4 → 17.7 mg

【Adverse Reactions】

Common (≥ 20%)

Hematologic: Neutropenia, thrombocytopenia, anemia

Gastrointestinal: Diarrhea, nausea, vomiting, abdominal pain, decreased appetite

Hepatic: Elevated ALT/AST

Other: Fatigue, headache, alopecia, rash

Serious (Boxed Warning)

QT interval prolongation, Torsades de Pointes, cardiac arrest

Myelosuppression (febrile neutropenia)

Infection (sepsis, pneumonia)

Pancreatitis, hepatic failure

【Contraindications】

Hypersensitivity to Quizartinib or excipients

Hypokalemia/hypomagnesemia, Long QT Syndrome, history of ventricular arrhythmias

Pregnancy, breastfeeding

Severe hepatic impairment (Child-Pugh C)

【Precautions】

1. Cardiac Monitoring (Key)

Perform ECGs prior to treatment, weekly during induction/consolidation phases, and weekly during the first month of maintenance therapy

Correct hypokalemia/hypomagnesemia prior to administration

Do not initiate/increase dose if QTcF > 450 ms; discontinue treatment if QTcF > 500 ms

2. Myelosuppression

Monitor complete blood counts regularly; suspend treatment for Grade ≥ 3 reductions, then resume at a reduced dose once recovered

3. Drug Interactions

Contraindicated: Strong CYP3A inducers (e.g., rifampin, carbamazepine)

Use with caution: Strong CYP3A inhibitors, QT-prolonging agents (e.g., ondansetron, azithromycin)

4. Reproductive Considerations & Contraception

Women of Childbearing Potential: Contraception required during treatment and for 7 months after discontinuing the drug.

Men: Contraception required during treatment and for 4 months after discontinuing the drug.

[Pharmacology & Toxicology]

Mechanism of Action: Highly selective inhibition of FLT3-ITD, thereby blocking tumor cell proliferation.

Pharmacokinetics: Peak plasma concentration reached 5–8 hours after oral administration; metabolized via CYP3A; elimination half-life is approximately 43 hours.

[Storage]

Store in a tightly sealed container in a dry place at 20–25°C (excursions between 15–30°C are permitted).

Important Note: Prescription-only medication. Indicated exclusively for AML with FLT3-ITD mutations. Must be prescribed by a physician certified under the REMS program. Strict ECG monitoring is required.