Loncastuximab tesirine injection 隆卡昔单抗注射液

Loncastuximab tesirine, marketed as Zynlonta, is a monoclonal antibody-drug conjugate used to treat large B-cell lymphoma and high-grade B-cell lymphoma. It is an antibody-drug conjugate (ADC) consisting of a humanized antibody that targets the protein CD19.
Loncastuximab tesirine was approved for medical use in the United States in April 2021 and in the European Union in December 2022. The U.S. Food and Drug Administration (FDA) considers it a first-in-class drug.
Loncastuximab tesirine was granted orphan drug designation by the FDA for the treatment of diffuse large B-cell lymphoma. Loncastuximab tesirine was approved under the FDA’s accelerated approval program.
【Mechanism of Action】
Loncastuximab tesirine-lpyl is an antibody-drug conjugate (ADC) composed of a monoclonal IgG1 kappa antibody component that binds to human CD19, a transmembrane protein expressed on the surface of B-lineage cells. After binding to CD19, loncastuximab tesirine-lpyl is internalized, followed by the release of SG3199, a pyrrolobenzodiazepine dimer cytotoxic alkylating agent. The released SG3199 binds to the DNA minor groove and forms highly cytotoxic DNA interstrand crosslinks, which subsequently induce cell death.
【Indications】
Adult patients with relapsed or refractory large B-cell lymphoma after ≥2 lines of systemic therapy, including diffuse large B-cell lymphoma (DLBCL) not otherwise specified, DLBCL derived from low-grade lymphoma, and high-grade B-cell lymphoma.
Zynlonta Dosage and Administration
Adults
For BMI ≥35kg/m2, calculate dose based on adjusted body weight (ABW): ABW in kg = 35kg/m2 x (height in meters)2. Pre-medicate with dexamethasone (oral or IV) for 3 consecutive days starting the day before treatment (or at least 2 hours before treatment). Administer via 30-minute IV infusion on Day 1 of each cycle (every 3 weeks). 0.15mg/kg every 3 weeks for 2 cycles, then 0.075mg/kg every 3 weeks for subsequent cycles. Dose Adjustments: See full label. If dosing is delayed >3 weeks due to toxicity, reduce subsequent doses by 50%. If toxicity recurs after dose reduction, consider discontinuation.
Children
Not established.
Warnings/Precautions
Monitor for edema or effusion; if ≥Grade 2 reactions occur, withhold until symptoms resolve. Consider diagnostic imaging if symptomatic pleural or pericardial effusion occurs. Risk of severe myelosuppression. Monitor complete blood counts during treatment. Monitor for infections; if Grade 3 or 4 infection occurs, withhold until symptoms resolve. Monitor for skin reactions (including photosensitivity); if Grade 3 reaction occurs, withhold until symptoms resolve. Minimize or avoid direct exposure to natural or artificial sunlight as recommended. Avoid extravasation. Mild hepatic impairment: Monitor. Moderate/severe hepatic impairment, severe renal impairment, ESRD with or without dialysis: Not studied. Embryo-fetal toxicity. Use effective contraception during treatment and for 10 months (females of childbearing potential) or 7 months (males with female partners) after the last dose. Pregnancy: Exclude status prior to starting treatment. Lactating mothers: Not recommended (during treatment and for 3 months after the last dose).
[Adverse Reactions]
Thrombocytopenia, elevated γ-glutamyl transferase, neutropenia, anemia, hyperglycemia, elevated transaminases, fatigue, hypoalbuminemia, rash, edema, nausea, musculoskeletal pain; febrile neutropenia, pneumonia, pleural effusion, sepsis, hyperpigmentation.
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