Trastuzumab Emtansine

Generic Details

Generic Name

Trastuzumab-emtansine

Other Names

  • T-DM1
  • Kadcyla

Drug Class

  • Monoclonal Antibody-Drug Conjugate (ADC)

Chemical Formula

C6478H10048N1720O2024S44

Molecular Weight

146096.2 g/mol

Mechanism of Action

  • Trastuzumab binds to HER2 receptors on cancer cells, delivering emtansine (a microtubule inhibitor) into the cells, causing cell death.

Indications

  • Breast cancer
  • Gastric cancer

Common Dosage Forms

  • Single-dose vial for intravenous injection

Typical Dosage

  • 3.6 mg/kg every 3 weeks

Pediatric Dosage

  • Limited data available, dosage based on weight and the indication

Geriatric Dosage

  • Dose adjustment may be required based on age and overall health

Side Effects

  • Fatigue
  • Nausea
  • Muscle pain
  • Thrombocytopenia
  • Liver toxicity

Contraindications

  • Hypersensitivity to trastuzumab or emtansine
  • Severe heart disease

Pregnancy Category

  • Not recommended during pregnancy (Category D)

Lactation Safety

  • May harm the infant, discontinue breastfeeding or the drug

Drug Interactions

  • Hepatotoxic drugs
  • QT-prolonging drugs
  • Strong CYP3A4 inhibitors

Overdose Symptoms

  • Increased risk of severe toxicity

Antidote for Overdose

  • No specific antidote, manage symptoms and provide supportive care

Storage Conditions

  • Refrigerate at 2°C to 8°C, do not freeze

Pharmacokinetics

  • Absorption: Administered intravenously, rapid distribution phase
  • Distribution: Binds to HER2 receptors on tumor cells
  • Metabolism: Metabolized via proteolytic degradation
  • Excretion: Primarily excreted in feces

Precautions

  • Cardiotoxicity monitoring during treatment
  • Regular liver function tests

Warnings

  • Increased risk of liver toxicity and heart problems
  • May cause fetal harm if used during pregnancy

Others

  • Regular monitoring of blood cell counts is necessary during treatment