DNA topoisomerase 1, Receptor tyrosine-protein kinase erbB-2
Receptor tyrosine-protein kinase erbB-2
Modality
Small molecule
Monoclonal antibody
Phase
FDA-approved
FDA-approved
Therapeutic area
Oncology
Oncology
First approval
—
2013
Mechanism of action
Enhertu
—
Kadcyla
Trastuzumab emtansine is a HER2-targeted antibody-drug conjugate that works by binding to the HER2 receptor and releasing a cytotoxic agent.
Approved indications
Enhertu
Advanced HER2positive gastric or gastroesophageal junction (GEJ) adenocarcinoma
Metastatic human epidermal growth factor 2 positive carcinoma of breast
Kadcyla
Adjuvant treatment of HER2-positive breast cancer
Treatment of HER2-positive breast cancer in patients who have received prior trastuzumab-based therapy
Treatment of HER2-positive breast cancer in patients for whom trastuzumab and pertuzumab are indicated
Treatment of HER2-positive unresectable or metastatic breast cancer in patients who have received prior anti-HER2-based therapy
Common side effects
Enhertu
Decreased white blood cell count
Decreased hemoglobin
Decreased neutrophil count
Nausea
Increased alanine aminotransferase
Diarrhea
Increased aspartate aminotransferase
Decreased lymphocyte count
Kadcyla
Fatigue
Nausea
Musculoskeletal pain
Hemorrhage
Thrombocytopenia
Increased transaminases
Headache
Constipation
Boxed warnings
Enhertu
No boxed warnings.
Kadcyla
WARNING: HEPATOTOXICITY, CARDIAC TOXICITY, EMBRYO-FETAL TOXICITY Hepatotoxicity: Serious hepatotoxicity has been reported, including liver failure and death in patients treated with KADCYLA. Monitor serum transaminases and bilirubin prior to initiation of KADCYLA treatment and prior to each KADCYLA dose. Reduce dose or discontinue KADCYLA as appropriate in cases of increased serum transaminases or total bilirubin. ( 2.3 , 5.1 ) Cardiac Toxicity: KADCYLA administration may lead to reductions in left ventricular ejection fraction (LVEF). Evaluate left ventricular function in all patients prior to and during treatment with KADCYLA. Withhold treatment for clinically significant decrease in left ventricular function. ( 2.3 , 5.2 ) Embryo-Fetal Toxicity: Exposure to KADCYLA during pregnancy can result in embryo-fetal harm. Advise patients of these risks and the need for effective contraception. ( 5.3 , 8.1 , 8.3 ) WARNING: HEPATOTOXICITY, CARDIAC TOXICITY, EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning Hepatotoxicity, liver failure and death have occurred in KADCYLA-treated patients. Monitor hepatic function prior to initiation and prior to each dose. Institute dose modifications or permanently discontinue as appropriate. ( 2.3 , 5.1 ) KADCYLA may lead to reductions in left ventricular ejection fraction (LVEF). Assess LVEF prior to initiation. Monitor and withhold dosing or discontinue as appropriate. ( 2.3 , 5.2 ) Embryo-Fetal Toxicity: Exposure to KADCYLA during pregnancy can result in embryo-fetal harm. Advise patients of these risks and the need for effective contraception. ( 5.3 , 8.1 , 8.3 )