carfilzomib

L01XG02

Forms & Strengths

Adult Dosing

Multiple myeloma (monotherapy or with dexamethasone): 20 mg/m² intravenously over 10-30 minutes on Days 1 and 2 of Cycle 1; if tolerated, increase to 27 mg/m² on Days 8, 9, 15, and 16 of Cycle 1, and 27 mg/m² on Days 1, 2, 8, 9, 15, and 16 of subsequent 28-day cycles
Once-weekly regimen (with daratumumab and dexamethasone or lenalidomide and dexamethasone): 20 mg/m² on Days 1 and 2, then 70 mg/m² on Days 8 and 15 of a 28-day cycle

Pediatric Dosing

Indications

Treatment of adult patients with relapsed or refractory multiple myeloma who have received 1 to 3 prior lines of therapy

Mechanism of Action

Selective and irreversible inhibitor of the chymotrypsin-like activity of the 20S proteasome, leading to accumulation of polyubiquitinylated proteins, cell cycle arrest, apoptosis, and inhibition of tumor growth

Contraindications

Adverse Reactions

Cardiac toxicities (heart failure, cardiomyopathy, myocardial ischemia)
Vascular toxicities (hypertension, pulmonary hypertension, venous thromboembolism)
Infections (upper respiratory tract infection, pneumonia)
Hematologic toxicities (thrombocytopenia, anemia, neutropenia, lymphopenia)
Hepatic failure, acute renal failure, tumor lysis syndrome, infusion-related reactions
Gastrointestinal disturbances (diarrhea, nausea, vomiting, constipation), fatigue, pyrexia, dyspnea

Drug Interactions

Strong CYP3A inhibitors/inducers do not significantly affect carfilzomib pharmacokinetics
Concomitant use with agents that cause peripheral neuropathy may worsen condition
Increased risk of thrombotic events when combined with immunomodulatory drugs (e.g., lenalidomide, thalidomide) or hormonal contraceptives

Curated Content: Needs Vetting Before Put to Clinical Use