Generic
Trastuzumab Emtansine
2 brands available in the market
At a glance
Trastuzumab Emtansine is a HER2-targeted antibody-drug conjugate indicated for HER2-positive, unresectable locally advanced or metastatic breast cancer previously treated with trastuzumab and a taxane.
Description
Trastuzumab Emtansine is a HER2-targeted antibody-drug conjugate containing trastuzumab covalently linked to DM1 via MCC linker. It delivers DM1 to HER2-overexpressing tumor cells, causing cell cycle arrest and apoptosis.
Indications
- HER2-positive metastatic breast cancer
Therapeutic class
Anti neoplastic preparations
Pharmacological class
Antibody-Drug Conjugate
Pharmacology
Trastuzumab Emtansine binds to HER2, undergoes receptor-mediated internalization and lysosomal degradation, releasing DM1-containing cytotoxic catabolites. DM1 inhibits tubulin polymerization, causing G2/M arrest and apoptosis.
Mechanism of action
Binds to HER2 and delivers DM1, inhibiting tubulin polymerization and causing apoptosis.
Dosage
Adult Dose (IV):
- 3.6 mg/kg IV every 3 weeks (21-day cycle) until disease progression or unacceptable toxicity
- First infusion: over 90 minutes; observe during and for at least 90 minutes after
- Subsequent infusions: over 30 minutes if prior infusions well tolerated; observe for at least 30 minutes
Administration
- Administered by a healthcare professional as IV infusion
- Do not administer doses greater than 3.6 mg/kg
- Do not substitute for or with trastuzumab
- Monitor infusion site for subcutaneous infiltration
Missed dose
If you miss a dose, consult your doctor.
Side effects
Common Side Effects:
- Fatigue
- Nausea
- Headache
- Decreased blood cells
- Increased liver enzymes
- Musculoskeletal pain
- Bleeding
- Infusion reactions
Precautions & warnings
- Confirmed HER2-positive tumor status required
- Risk of cardiotoxicity; cardiac monitoring required
- Observe for infusion reactions
- May cause fetal harm; use effective contraception
- Discontinue for severe hypersensitivity reactions
Contraindications
- Hypersensitivity to Trastuzumab Emtansine or any excipients
Drug interactions
- Strong CYP3A inhibitors: decreased DM1 metabolism; caution advised
Food interactions
Food interactions are not significant.
Use in pregnancy
Use in Pregnancy: Not recommended; may cause fetal harm or death; do not use during pregnancy.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; discontinue nursing prior to treatment; may begin nursing 7 months after concluding treatment.
Pediatric use
Safety and efficacy not established in children under 18 years
Geriatric use
Insufficient data in patients 75 years or older
Renal / hepatic impairment
Renal Impairment: Limited information
Hepatic Impairment: Limited information
Overdose effects
Symptoms: Bone marrow suppression, cardiotoxicity.
Treatment: Supportive care.
Storage conditions
Store vials at 2-8°C.