IntravenousHER2-positive early breast cancerAdult: As adjuvant treatment in patients who have residual invasive disease after neoadjuvant taxane-based and HER2-targeted therapy: 3.6 mg/kg every 3 weeks (21-day cycle) for a total of 14 cycles unless there is disease recurrence or unmanageable toxicity. Doses are given via infusion; administer the initial dose as a 90-minute infusion, if well tolerated, subsequent doses may be given as a 30-minute infusion. Dose reduction, dosing interruption or discontinuation may be required according to individual safety and tolerability.
IntravenousHER2-positive metastatic breast cancerAdult: As monotherapy for cases that previously received conventional trastuzumab and a taxane, separately or in combination. In patients who have received previous therapy for locally advanced or metastatic disease, or who have developed disease recurrence during or within 6 months of completing adjuvant therapy: 3.6 mg/kg every 3 weeks (21-day cycle) until disease progression or unmanageable toxicity. Doses are given via infusion; administer the initial dose as a 90-minute infusion, if well tolerated, subsequent doses may be given as a 30-minute infusion. Dose reduction, dosing interruption or discontinuation may be required according to individual safety and tolerability.
|
|
|
Check the vial labels to ensure the appropriate product is being reconstituted. Slowly inject 5 mL or 8 mL of sterile water for inj into a vial labelled as containing 100 mg or 160 mg, respectively, to make a 20 mg/mL reconstituted solution. Gently swirl the vial to dissolve; do not shake. Further dilute the reconstituted solution with 250 mL NaCl 0.45% or NaCl 0.9% solution prior to infusion. Gently invert the bag to mix; do not shake.
|
Incompatible with 5% dextrose in water due to the increased risk of protein aggregation.
|
|
|
Patient with thrombocytopenia; known active hepatic disease (e.g. HBV or HCV); dyspnoea at rest associated complications of advanced malignancy, comorbidity, or concurrent pulmonary radiation therapy. Not recommended for use in patients who had previously discontinued trastuzumab therapy due to infusion reaction or hypersensitivity. Ensure that the appropriate drug is being given prior to administration; trastuzumab emtansine is not interchangeable with other products containing conventional trastuzumab, trastuzumab deruxtecan, and other preparations that contain trastuzumab in combination with other agents. Avoid extravasation. Patients taking anticoagulants or antiplatelet agents. Asian ancestry. Hepatic and severe renal impairment. Pregnancy and lactation.
|
Significant: Reduced left ventricular ejection fraction, heart failure; extravasation, delayed skin necrosis, local reactions secondary to extravasation (e.g. erythema, irritation, pain, swelling, tenderness); bone marrow suppression (e.g. thrombocytopenia); peripheral neuropathy; infusion-related reactions. Rarely, severe anaphylactic reaction.
Blood and lymphatic system disorders: Anaemia, neutropenia, leucopenia.
Eye disorders: Conjunctivitis, dry eye, blurred vision, increased lacrimation.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, constipation, abdominal pain, stomatitis, dry mouth, stomatitis, dysgeusia, gingival bleeding, dyspepsia.
General disorders and administration site conditions: Pyrexia, fatigue, asthenia, peripheral oedema, chills.
Investigations: Increased transaminases, blood alkaline phosphatase and bilirubin.
Musculoskeletal and connective tissue disorders: Musculoskeletal pain, myalgia, arthralgia.
Nervous system disorders: Headache, dizziness, memory impairment.
Psychiatric disorders: Insomnia.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Epistaxis, cough, dyspnoea.
Skin and subcutaneous tissue disorders: Rash, pruritus, alopecia, nail disorder, palmar-plantar erythrodysaesthesia syndrome, urticaria.
Vascular disorders: Hypertension.
Potentially Fatal: Hepatotoxicity (e.g. liver failure), nodular regenerative hyperplasia of the liver; haemorrhagic events (e.g. CNS, respiratory, and gastrointestinal haemorrhage); interstitial lung disease, including pneumonitis which may result in acute respiratory distress syndrome.
|
IV: Z (Risk of oligohydramnios resulting in neonatal complications. If unavoidable, closely monitor the amniotic fluid status.)
|
Women and men with female partners of childbearing potential must use effective contraception during treatment and for 7 months after treatment discontinuation. Do not breastfeed during and for 7 months after the last dose.
|
Verify pregnancy status prior to treatment initiation. Monitor platelet count, serum transaminases and bilirubin at baseline and before each dose. Perform standard cardiac function test (e.g. ECG or multigated acquisition scanning) before treatment initiation and at least every 3 months during treatment. HBV screening, including HBsAg, hepatitis B core antibody, total Ig or IgG, and antibody to HBsAg is recommended before or at the beginning of systemic anticancer therapy. Closely monitor for signs of infusion-related reactions (e.g. fever, chills) for approx 90 minutes after the initial infusion; if tolerated, monitor for approx 30 minutes after the subsequent infusions. Monitor the infusion site during administration for possible subcutaneous infiltration. Assess for signs and symptoms of bleeding, neurotoxicity (including peripheral neuropathy) and pulmonary toxicity.
|
Symptom: Thrombocytopenia. Management: Symptomatic and supportive treatment.
|
Increased plasma concentration of the DM1 component with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, atazanavir, indinavir, nelfinavir, ritonavir, saquinavir, and nefazodone). May increase the risk of haemorrhagic events with anticoagulants or antiplatelet agents.
|
Description:
Mechanism of Action: Trastuzumab emtansine is a human epidermal growth factor receptor 2 (HER2)-antibody drug conjugate which contains trastuzumab and DM1 (a maytansine derivative) linked via a stable thioether linker. Trastuzumab possesses HER2 targeted activities and DM1 is a cytotoxic microtubule inhibitor. The combination allows for selective delivery into HER2 overexpressing cells, thereby causing cell cycle arrest and apoptosis.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Near the end of the infusion.
Distribution: Volume of distribution: 3.13 L. Plasma protein binding: 93% (DM1).
Metabolism: Metabolised in the liver by the CYP3A4 and CYP3A5 isoenzymes (DM1). Undergoes deconjugation and catabolism by proteolysis in cellular lysosomes.
Excretion: Elimination half-life: Approx 4 days.
|
Intact vial: Store between 2-8°C. Reconstituted solution and diluted solution for infusion: May be stored between 2-8°C for up to 24 hours. Do not freeze or shake the intact vial, reconstituted vial, or diluted solution for infusion. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
|
|
|
L01FD03 - trastuzumab emtansine ; Belongs to the class of HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors. Used in the treatment of cancer.
|
Ado-Trastuzumab Emtansine. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/04/2025. Ado-Trastuzumab Emtansine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/04/2025. Brayfield A, Cadart C (eds). Trastuzumab. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/04/2025. Joint Formulary Committee. Trastuzumab Emtansine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/04/2025. Kadcyla (Roche [Malayasia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/04/2025. Kadcyla 160 mg Powder for Concentrate for Solution for Infusion (Roche Products Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/04/2025. Kadcyla Injection, Powder, Lyophilized, for Solution (Genentech, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/04/2025. Roche Products (New Zealand) Limited. Kadcyla 100 mg and 160 mg Powder for Concentrate for Solution for Infusion data sheet 3 February 2025. Medsafe. http://www.medsafe.govt.nz. Accessed 07/04/2025.
|
Sign Out
