Mylotarg (gemtuzumab ozogamicin)

Antineoplastic Monoclonal Antibodies Intravenous Vial (Ea)

Advertisement

Last reviewed · Source: First Databank (FDB) drug data

Overview

Gemtuzumab ozogamicin, a CD33-directed antibody-drug conjugate consisting of a recombinant humanized immunoglobulin G4(IgG4) kappa monoclonal antibody (gemtuzumab) covalently linked to a cytotoxic calicheamicin derivative (N-acetyl-gamma-calicheamicin), is an antineoplastic agent.

Gemtuzumab ozogamicin, an anti-CD33 antibody-drug conjugate, is an antineoplastic agent. The anti-CD33 antibody, a recombinant humanized IgG4 kappa immunoglobulin, is covalently linked to the cytotoxic antitumor antibiotic N-acetyl-gamma-calicheamicin; the cytotoxic moiety is a derivative of calicheamicin, a natural product isolated from the microorganism Micromonospora echinospora subsp. calichensis. The formulation of gemtuzumab ozogamicin consists of both conjugated and unconjugated antibody; on average, approximately 2-3 moles of the calicheamicin derivative are attached to each mole of antibody.

The antibody portion of gemtuzumab ozogamicin binds specifically to antigen CD33, a transmembrane glycoprotein that is expressed on the surface of leukemic blasts in more than 80% of patients with acute myeloid leukemia (AML). Following binding of the antibody portion of gemtuzumab ozogamicin to antigen CD33, the resultant complex is internalized by the myeloid cell. The calicheamicin derivative of the antibody-drug conjugate is released via hydrolytic cleavage of the linker and binds to DNA in the minor groove causing double-strand breaks and subsequent cell cycle arrest and apoptosis.

Maximum delivery of calicheamicin to leukemic blast cells appears to be dependent on saturation of a high percentage of antigen CD33; in a pharmacodynamic analysis, near maximal saturation of antigen CD33 in peripheral blood was observed with gemtuzumab ozogamicin doses as low as 2 mg/m2. Although formal pharmacokinetic analyses have not been conducted in patients receiving a gemtuzumab ozogamicin dosage of 3 mg/m2 on days 1, 4, and 7 (fractionated regimen), simulations suggest that peak plasma concentrations and systemic exposure of the drug are reduced following the initial dose and full course of a fractionated regimen compared with peak plasma concentrations following dosing with an unfractionated regimen (gemtuzumab ozogamicin 9 mg/m2 for 2 doses administered 14 days apart). Because increased peak plasma concentrations following the initial dose of gemtuzumab ozogamicin 9 mg/m2 have been correlated with an increased risk of hepatic veno-occlusive disease (VOD), these data suggest that a lower-dose fractionated regimen may reduce the risk of hepatic VOD without compromising efficacy. (See Uses: Acute Myeloid Leukemia.)

In vitro studies indicate that the calicheamicin derivative of the antibody-drug conjugate is extensively metabolized, primarily by nonenzymatic reduction. In vitro, the calicheamicin derivative is approximately 97% bound to plasma proteins. The terminal half-life of unconjugated gemtuzumab is 62 and 90 hours following the first and second doses, respectively, of the antibody-drug conjugate.

USES: This medication is used to treat a certain type of leukemia (CD33-positive acute myeloid leukemia-AML). This medication works by slowing or stopping the growth of cancer cells.

Generic name: gemtuzumab ozogamicin
Pronunciation: (jem-TOOZ-ue-mab OH-zoe-ga-MYE-sin)
Drug class: Antineoplastic Monoclonal Antibodies
Therapeutic class: Antineoplastics

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Mylotarg

Intelligence content is not available yet.

Indications

The following indications are listed for Mylotarg:

  • Cd33 Positive Acute Myeloid Leukemia

Also known as: Cd33 (+) Acute Myeloid Leukemia, Cd33 Positive Aml.

Dosing

If treatment-related toxicities occur, the manufacturer states that CBCs and blood chemistries should be monitored at least 3 times per week until resolution of the toxicity.

Drug interactions

In vitro, gemtuzumab ozogamicin is unlikely to inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2A6, 2C8, 2C9, 2C19, 2D6, and 3A4/5 at clinically relevant concentrations. In vitro studies also indicate that the calicheamicin derivative of the antibody-drug conjugate is unlikely to inhibit CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4/5 inhibit uridine diphosphate-glucuronosyltransferase (UGT) 1A1, 1A4, 1A6, 1A9, and 2B7, or induce CYP isoenzymes 1A2, 2B6, and 3A4 at clinically relevant concentrations.

The calicheamicin derivative of the antibody-drug conjugate also is unlikely to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 2, organic anion transport protein (OATP) 1B1, and OATP1B3.

No formal drug interaction studies have been performed to date with gemtuzumab ozogamicin.

Contraindications

Known hypersensitivity to gemtuzumab ozogamicin or any ingredient in the formulation.

Adverse reactions

Adverse effects reported in at least 15% of adults receiving gemtuzumab ozogamicin in combination with daunorubicin and cytarabine for newly diagnosed de novo AML in the ALFA-0701 trial include hemorrhage, infection, prolonged thrombocytopenia (platelet counts less than 50,000/mm3 lasting longer than 42 days in the absence of active disease), anemia, and neutropenia. Grade 3 or greater laboratory abnormalities reported in at least 10% of patients receiving gemtuzumab ozogamicin who had grade 2 or lesser severity of the laboratory abnormality at baseline include hypophosphatemia, hypokalemia, hyponatremia, elevated concentrations of alkaline phosphatase, and elevated concentrations of aminotransferases (ALT, AST).

Adverse effects reported in at least 15% of adults receiving gemtuzumab ozogamicin monotherapy for newly diagnosed AML in the AML-19 study include hepatotoxicity, fatigue, infection, cardiac effects, hemorrhage, febrile neutropenia, and metabolic abnormalities.

Adverse effects reported in at least 15% of patients receiving gemtuzumab ozogamicin monotherapy for relapsed or refractory AML include pyrexia, infection, elevated concentrations of ALT and/or AST, hemorrhage, nausea and vomiting, constipation, mucositis, headache, and rash. Grade 3 adverse effects reported in more than 30% of these patients include sepsis.

Precautions

No enhanced messaging available.

ICD codes

CodeTypeDescription
Cd33 positive acute myeloid leukemia
C92.0ICD10CMAcute myeloblastic leukemia
C92.00ICD10CMAcute myeloblastic leukemia, not having achieved remission
C92.02ICD10CMAcute myeloblastic leukemia, in relapse

ICD code information from First Databank (FDB).

Formulary status

Search health-plan coverage for this drug by ZIP code.

Enter a ZIP code to view available health plans.

Last reviewed · Source: First Databank (FDB) drug data