[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Antibody-drug conjugates (ADCs)](https://durgical.com/en/pharmacology/classes/antibody-drug-conjugates/) › Trastuzumab emtansine

# Trastuzumab emtansine

## ADCs?

Antibody-drug conjugates (ADCs)

## High alert?

An error with this medicine can cause serious harm: double checks and protocols are used.

## Pregnancy: avoid?

Avoid in pregnancy. Can harm the fetus (boxed warning); a negative pregnancy test is required and effective contraception is used during and after treatment.

Trastuzumab joined to the microtubule poison DM1; used in HER2-positive breast cancer. Watch the liver, the heart and the platelets.

Updated Nov 1, 2026

Also called: ado-trastuzumab emtansine, T-DM1

## Quick facts

**Group**
[Antibody-drug conjugates (ADCs)](https://durgical.com/en/pharmacology/classes/antibody-drug-conjugates/)

**Target**
HER2 (ErbB2) receptor on tumour cells

**Used for**
Early HER2-positive breast cancer

**Key effects**
Fatigue · Nausea · Muscle and joint pain

**Monitor**
Liver tests before each dose · Heart function

**ATC**
L01FD03

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

◎**HER2 (ErbB2) receptor on tumour cells**Trastuzumab emtansine

ⓘ The cryo-EM structure shows the HER2 extracellular domain bound by trastuzumab (the antibody part of this conjugate) and pertuzumab; the DM1 payload is not in the structure.

**Target in 3D:** HER2 (ErbB2) receptor on tumour cells. PDB structure 6OGE (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6OGE) · Drag to rotate · pinch to zoom

The antibody keeps trastuzumab's HER2 blockade and delivers DM1 (emtansine), a maytansine derivative attached to lysine residues. After binding HER2 the complex enters the cell by receptor-mediated endocytosis; proteases in the lysosome release DM1 into the cytosol, where it disrupts microtubules, arrests mitosis and triggers apoptosis.

- Binds HER2 on the breast cancer cell
- Taken in by endocytosis and digested in lysosomes
- DM1 is released and disrupts microtubules
- Mitotic arrest and apoptosis

## Indications

- HER2-positive metastatic breast cancer previously treated with trastuzumab and a taxane. [Breast cancer →](https://durgical.com/en/conditions/breast-cancer/)
- Early HER2-positive breast cancer with residual invasive disease after neoadjuvant treatment (adjuvant use). [Breast cancer →](https://durgical.com/en/conditions/breast-cancer/)

## Adverse effects

### Common

- Fatigue, headache
- Nausea, constipation, diarrhoea
- Muscle and joint pain
- Dry or watery eyes, blurred vision
- Nosebleeds and easy bruising

### Serious (rare, important)

- Serious or fatal hepatotoxicity (boxed warning)
- Reduced left ventricular function and heart failure (boxed warning)
- Embryo-fetal toxicity (boxed warning)
- Thrombocytopenia and bleeding
- Peripheral neuropathy
- Infusion and allergic reactions

## Contraindications

- Allergy to the drug or to trastuzumab
- Caution in liver disease and heart disease

## Key interactions

**Trastuzumab and trastuzumab deruxtecan**
Different drugs: never substituted for one another.

**Aspirin, anticoagulants and other drugs that raise bleeding risk**
Bleeding is more likely when platelets are low.

**Other liver-toxic medicines and grapefruit**
May raise the risk of liver damage; they are discussed before use.

## What is monitored

- Liver tests before each dose
- Heart function (ejection fraction) before and during treatment
- Platelet count
- Signs of neuropathy
- Confirmation that the tumour is HER2-positive before starting

## Administration and safety

- Intravenous infusion only, never as a push; the first infusion is watched closely for reactions.
- Check the full name: «trastuzumab» alone and the two trastuzumab conjugates are different drugs.
- Hazardous drug: prepared and handled with chemotherapy precautions.

## Pregnancy and breastfeeding

Avoid in pregnancy. Can harm the fetus (boxed warning); a negative pregnancy test is required and effective contraception is used during and after treatment.

## Nursing care

- Check liver tests and platelets before each dose.
- Observe the patient during and after the infusion for chills, fever or breathing difficulty.
- Ask about swelling, breathlessness or palpitations (heart failure) and tingling in the hands or feet.
- Teaching: report yellow skin, dark urine, black stools or unusual bleeding; use effective contraception.

## Pharmacokinetics

**Absorption**
Intravenous infusion every few weeks.

**Elimination**
The antibody part is catabolised like other proteins.

## Memory aid

«T-DM1: Destroys Microtubules, watch 1-2-3»: 1 liver, 2 heart, 3 platelets.

## Test yourself

Think of the answer, then tap the question to see it.

## What is the payload of trastuzumab emtansine and what does it target?

DM1 (emtansine), a maytansine derivative that disrupts microtubules.

## What are the three boxed warnings of trastuzumab emtansine?

Hepatotoxicity, cardiac toxicity (reduced ejection fraction) and embryo-fetal toxicity.

## In which early breast cancer setting is trastuzumab emtansine used?

HER2-positive early breast cancer with residual invasive disease after neoadjuvant therapy.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/trastuzumab-emtansine/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**High alert**
An error with this medicine can cause serious harm: double checks and protocols are used.

**Pregnancy: avoid**
Avoid in pregnancy. Can harm the fetus (boxed warning); a negative pregnancy test is required and effective contraception is used during and after treatment.

## Connections

## Related drugs 2

- [Trastuzumab](https://durgical.com/en/pharmacology/trastuzumab/)
- [Trastuzumab deruxtecan](https://durgical.com/en/pharmacology/trastuzumab-deruxtecan/)

## Related conditions 1

- [Breast cancer](https://durgical.com/en/conditions/breast-cancer/)

[← Back to the class: Antibody-drug conjugates (ADCs)](https://durgical.com/en/pharmacology/classes/antibody-drug-conjugates/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Ado-trastuzumab Emtansine Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a613031.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Ado-Trastuzumab Emtansine - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/ado-trastuzumab-emtansine) (National Cancer Institute, 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01FD03) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/trastuzumab-emtansine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/trastuzumab-emtansine/
