Gemtuzumab
Class: Antineoplastic Agents
Chemical Name: Methyl [(1R,4Z,8S,13E)-[8-[[2-O-[4-(acetylethylamino)-2,4-dideoxy-3-O-methyl-α-L-threo-pentopyranosyl]-4,6-dideoxy-4-[[[2,6-dideoxy-4-S-[4-[6-deoxy-3-O-methyl-α-L-mannopyranosyl)oxy]-3-iodo-5,6-dimethoxy-2-methylbenzoyl]-4-thio-β-D-ribo-hexopyranosyl]oxy]amino]-β-D-glucopyranosyl]oxy]-13-[2-[[3-[[1-[4-(4-amino-4-oxobutoxy)phenyl]ethylidene]hydrazino]-1,1-dimethyl-3-oxopropyl]-dithio]ethylidene]-1-hydroxy-11-oxobicyclo[7.3.1]trideca-4,9-diene-2,6-diyn-10-yl]carbamate conjugate dimer disulfide with human-mouse monoclonal hP67.6 κ-chain anti-(human CD33 (antigen)) (human-mouse monoclonal hP67.6 γ4-chain, immunoglobulin G4
CAS Number: 220578-59-6
Brands: Mylotarg
Warning
Risk of hepatotoxicity, including hepatic veno-occlusive disease (VOD; also known as sinusoidal obstruction syndrome); may be life-threatening or fatal. (See Hepatotoxicity under Cautions.)
Reported in patients receiving the drug as monotherapy or as part of a combination chemotherapy regimen.
Monitor frequently for manifestations of hepatic VOD.
Introduction
Antineoplastic agent; CD33-directed antibody-drug conjugate consisting of an anti-CD33 monoclonal antibody covalently linked to a cytotoxic calicheamicin derivative (N-acetyl-γ-calicheamicin).
Uses for Gemtuzumab
Acute Myeloid Leukemia (AML)
Used in combination with daunorubicin and cytarabine for induction and consolidation therapy in adults with newly diagnosed CD33-positive de novo AML. Subgroup analysis suggests possible lack of clinical benefit in patients with unfavorable cytogenetics. (See Decreased Efficacy in Patients with Unfavorable Cytogenetics under Cautions.)
Used alone (i.e., as single agent) for induction and continuation therapy in adults with newly diagnosed CD33-positive AML.
Used as single-agent therapy for relapsed or refractory CD33-positive AML in adults and children ≥2 years of age.
Designated an orphan drug by FDA for treatment of AML.
Gemtuzumab Dosage and Administration
General
To minimize risk of infusion-related reactions in adults, premedicate with acetaminophen 650 mg and diphenhydramine hydrochloride 50 mg 1 hour prior to each infusion, followed by methylprednisolone 1 mg/kg (or equivalent) within 30 minutes prior to infusion. (See Infusion-related Effects under Cautions.)
To minimize risk of infusion-related reactions in pediatric patients, premedicate with acetaminophen 15 mg/kg (up to maximum dose of 650 mg), diphenhydramine hydrochloride 1 mg/kg (up to maximum dose of 50 mg), and methylprednisolone 1 mg/kg (or equivalent) 1 hour prior to each infusion; may administer additional doses of acetaminophen and diphenhydramine hydrochloride every 4 hours.
If WBC counts ≥30,000/mm3, cytoreduction prior to administration is recommended.
Take appropriate measures to prevent tumor lysis syndrome.
Consult specialized references for procedures for proper h...
