margetuximab-cmkb

　　【Indications】

　　MARGENZA(margetuximab-cmkb)is a HER2/neu receptor antagonist indicated in combination with chemotherapy for the treatment of adult patients with metastatic HER2-positive breast cancer,who have previously received two or more prior anti-HER2 regimens,at least one of which was for metastatic disease.

　　【Recommended Dosage】

　　Administered exclusively via intravenous infusion.

　　Administer a loading dose of 15 mg/kg as an intravenous infusion over 120 minutes;subsequent maintenance doses are administered every 3 weeks over at least 30 minutes.

　　Continue treatment until disease progression or unacceptable toxicity occurs.

　　When administered on the same day as chemotherapy,MARGENZA may be given immediately following the completion of chemotherapy.

　　【Adverse Reactions】

　　The most common adverse reactions(incidence>10%)reported with MARGENZA in combination with chemotherapy include fatigue/asthenia,nausea,diarrhea,vomiting,constipation,headache,pyrexia,alopecia,abdominal pain,peripheral neuropathy,arthralgia/myalgia,cough,decreased appetite,dyspnea,infusion-related reactions,palmar-plantar erythrodysesthesia syndrome(PPES),and extremity pain.

　　【Mechanism of Action】

　　Margetuximab-cmkb binds to the extracellular domain of human epidermal growth factor receptor 2(HER2).Binding to HER2-expressing tumor cells inhibits cell proliferation,reduces HER2 ectodomain shedding,and mediates antibody-dependent cellular cytotoxicity(ADCC).

　　In vitro,the engineered Fc region of margetuximab-cmkb enhances binding to the activating Fc receptor FCGR3A(CD16A)and reduces binding to the inhibitory Fc receptor FCGR2B(CD32B).These modifications result in enhanced ADCC activity and NK cell activation in vitro.

　　【Storage and Handling】

　　Store vials in the original carton to protect from light at 2°C to 8°C(36°F to 46°F)until use.Do not freeze.