Ninlaro®Ixazomib Citrate Capsules

1. Indications and Usage
Multiple Myeloma (MM): In combination with lenalidomide and dexamethasone, for the treatment of adult patients with multiple myeloma who have received at least one prior therapy .
2. Dosage and Administration
Administration: Oral administration. Swallow capsules whole with water. Do not chew, crush, or open the capsules.
Food Requirement: Must be taken on an empty stomach. Take at least 1 hour before or 2 hours after a meal .
Standard Dose:
Recommended Dose: 4 mg once weekly for 3 weeks (Days 1, 8, and 15) of a 28-day cycle .
Missed Dose: If a dose is missed or vomiting occurs, do not make up for the missed dose. Resume at the next scheduled dose. If the next dose is due within 72 hours, skip the missed dose. Do not take a double dose .
Dose Adjustment: Mandatory dose reduction (e.g., to 3 mg or 2.3 mg) for severe toxicities or hepatic impairment .
3. Mechanism of Action
Ixazomib is an oral, second-generation, reversible proteasome inhibitor.
It preferentially binds to and inhibits the chymotrypsin-like activity of the β5 subunit of the 20S proteasome.
By blocking the proteasome, it prevents the degradation of proteins within cells, leading to cell cycle arrest and induction of apoptosis in myeloma cells .
4. Safety and Warnings
Thrombocytopenia: Can cause severe and life-threatening thrombocytopenia. Monitor platelet counts before each dose .
Peripheral Neuropathy: Can cause or worsen peripheral neuropathy. Monitor for symptoms (numbness, tingling, pain). Dose adjustments may be required .
Gastrointestinal Toxicity: Can cause severe diarrhea, constipation, nausea, and vomiting. Monitor and treat supportive care .
Hepatotoxicity: Monitor liver function tests (ALT, AST) regularly .
Embryo-Fetal Toxicity: May cause fetal harm. Contraception is required for females and males during treatment and for at least 90 days after the final dose .
5. Adverse Reactions
Common adverse reactions (incidence ≥20%) include:
Gastrointestinal: Diarrhea, Constipation, Nausea, Vomiting.
Hematologic: Thrombocytopenia, Neutropenia, Anemia, Lymphopenia.
General: Fatigue, Asthenia, Pyrexia, Peripheral edema.
Neurologic: Peripheral neuropathy (numbness, tingling, or pain in hands/feet).
Dermatologic: Rash, Pruritus .
6. Drug Interactions
CYP3A Inducers: Avoid co-administration with strong CYP3A inducers (e.g., rifampin) as they significantly reduce Ixazomib exposure .
CYP3A Inhibitors: Co-administration with strong CYP3A inhibitors (e.g., ketoconazole, clarithromycin) does not require dose adjustment based on clinical data, but caution is advised .
Oral Contraceptives: Ixazomib may decrease the efficacy of hormonal contraceptives; barrier contraception is recommended .
7. Pharmaceutical Information
Chemical Name: (3R,5S)-3-benzyl-5-(benzylamino)-4-[(2E)-4-(3-chlorophenyl)-4-oxobut-2-enoyl]-1,3,4-oxadiazolidin-2,5-diolate boron .
Molecular Formula: C23H22BClN2O5 .
Storage: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) .