loncastuximab tesirine

High Alert

Relapsed or refractory large B-cell lymphoma after ≥2 lines of systemic therapy, including diffuse large B-cell lymphoma not otherwise specified, diffuse large B-cell lymphoma arising from low-grade lymphoma, and high-grade B-cell lymphoma

Contraind./Precautions ⬆ ⬇

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Hepatic impairment;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema, PERICARDIAL EFFUSION, pericarditis

Derm: photosensitivity, pruritus, rash, dermatitis, erythema, hyperpigmentation

Endo: hyperglycemia

GI: ↑liver enzymes, abdominal pain, constipation, diarrhea, hypoalbuminemia, nausea, vomiting, ascites

GU: ↓fertility (men)

Hemat: anemia, neutropenia, thrombocytopenia

Local: extravasation

Metab: ↓appetite

MS: pain

Neuro: fatigue

Resp: dyspnea, pleural effusion, pneumonitis

Misc: infection

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Lyophilized powder for injection: 10 mg/vial

Route/Dosage ⬆ ⬇

IV (Adults ): 0.15 mg/kg on Day 1 (of each cycle) every 3 wk for 2 cycles, followed by 0.075 mg/kg on Day 1 (of each cycle) every 3 wk; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

An antibody-drug conjugate made up two parts: an antibody specific for human CD19 (expressed on surface of B cells) and an alkylating agent. Once loncastuximab tesirine binds to CD19, it is internalized and releases the alkylating agent via proteolytic cleavage. The alkylating agent then leads to cell death.

Therapeutic effects:

Decreased spread of B-cell lymphoma.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: drug-antibody conjugates, monoclonal antibodies

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Not extensively distributed to tissues.

Metabolism/Excretion: The monoclonal antibody portion is metabolized into small peptides by catabolic pathways. The alklyating agent is metabolized by the liver via the CYP3A4 and CYP3A5 isoenzymes. Excretion pathway of alklyating agent is unknown.

Half-Life: 20.8 days.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	unknown	end of infusion	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Advise patient to notify health care professional if skin rash appears, or experience dyspnea, new or worsening swelling in arms or legs, ↑ in weight and abdominal size, chest pain, or cough.
Advise patient to immediately contact health care professional if fever (≥100.4°F) or signs and symptoms of bruising or bleeding occur. Advise patient of the need of periodic monitoring of blood counts.
Advise patient to avoid direct natural and artificial sunlight and to wear sun-protective clothing and/or use sunscreen.
Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception during therapy and for 10 mo after last dose. Advise men with female partners of reproductive potential to use effective contraception during therapy and for 7 mo after last dose. Breastfeeding should be discontinued during therapy and for 3 mo after last dose. May cause fertility problems in men.

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Indications ⬇