ENHERTU
Enhertu is a HER2-directed antibody-drug conjugate indicated for the treatment of several types of unresectable or metastatic cancers. It is used in adult patients with HER2-positive, HER2-low, or HER2-ultralow breast cancer who have received prior systemic therapies or experienced disease recurrence. Additionally, it is indicated for patients with HER2-mutant non-small cell lung cancer and those with HER2-positive locally advanced or metastatic gastric or gastroesophageal junction adenocarcinoma.
How ENHERTU Works
Enhertu consists of a humanized anti-HER2 antibody covalently linked to a topoisomerase I inhibitor payload. After the antibody binds to HER2 receptors on the surface of cancer cells, the complex is internalized and the linker is cleaved by intracellular lysosomal enzymes. The released payload then causes DNA damage and cell death, effectively targeting cells that express the HER2 protein or harbor HER2 mutations.
Details
- Status
- Prescription
- First Approved
- 2019-12-20
- Routes
- INJECTION
- Dosage Forms
- INJECTABLE
ENHERTU Approval History
What ENHERTU Treats
5 indicationsENHERTU is approved for 5 conditions since its original approval in 2019. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Unresectable or metastatic HER2-positive breast cancer
- Unresectable or metastatic hormone receptor-positive, HER2-low or HER2-ultralow breast cancer
- Unresectable or metastatic HER2-low breast cancer
- Unresectable or metastatic HER2-mutant non-small cell lung cancer
- Locally advanced or metastatic HER2-positive gastric or gastroesophageal junction adenocarcinoma
ENHERTU Boxed Warning
INTERSTITIAL LUNG DISEASE and EMBRYO-FETAL TOXICITY Interstitial Lung Disease (ILD) and pneumonitis, including fatal cases, have been reported with ENHERTU. Monitor for and promptly investigate signs and symptoms including cough, dyspnea, fever, and other new or worsening respiratory symptoms. Permanently discontinue ENHERTU in all patients with Grade 2 or higher ILD/pneumonitis. Advise patients of the risk and the need to immediately report symptoms [see Dosage and Administration (2.3) , Warnin...
WARNING: INTERSTITIAL LUNG DISEASE and EMBRYO-FETAL TOXICITY Interstitial Lung Disease (ILD) and pneumonitis, including fatal cases, have been reported with ENHERTU. Monitor for and promptly investigate signs and symptoms including cough, dyspnea, fever, and other new or worsening respiratory symptoms. Permanently discontinue ENHERTU in all patients with Grade 2 or higher ILD/pneumonitis. Advise patients of the risk and the need to immediately report symptoms [see Dosage and Administration (2.3) , Warnings and Precautions (5.1) ] . Embryo-Fetal Toxicity: Exposure to ENHERTU during pregnancy can cause embryo-fetal harm. Advise patients of these risks and the need for effective contraception [see Warnings and Precautions (5.4) , Use in Specific Populations (8.1 , 8.3) ] . WARNING: INTERSTITIAL LUNG DISEASE and EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. Interstitial lung disease (ILD) and pneumonitis, including fatal cases, have been reported with ENHERTU. Monitor for and promptly investigate signs and symptoms including cough, dyspnea, fever, and other new or worsening respiratory symptoms. Permanently discontinue ENHERTU in all patients with Grade 2 or higher ILD/pneumonitis. Advise patients of the risk and to immediately report symptoms. ( 2.3 , 5.1 ) Exposure to ENHERTU during pregnancy can cause embryo-fetal harm. Advise patients of these risks and the need for effective contraception. ( 5.4 , 8.1 , 8.3 )
ENHERTU Target & Pathway
ProTarget
A receptor tyrosine kinase that promotes cell growth and division. Approximately 20% of breast cancers overexpress HER2, leading to aggressive tumor growth. Targeting HER2 blocks these growth signals and can trigger immune-mediated destruction of cancer cells.
Pathway Context
HER2 forms dimers with other HER family members to activate growth signaling
A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.
ENHERTU Competitors
Pro10 other drugs also target HER2. Compare mechanisms, indications, and trial activity.
Competitors share the same molecular target (HER2). Earlier expiry dates signal biosimilar/generic opportunities.
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
ENHERTU FDA Label Details
ProIndications & Usage
FDA Label (PDF)ENHERTU is a HER2-directed antibody and topoisomerase inhibitor conjugate indicated: HER2-Positive Metastatic Breast Cancer in combination with pertuzumab as first-line treatment of adult patients with unresectable or metastatic HER2-positive (IHC 3+ or ISH+) breast cancer, as determined by an FDA-approved test. as monotherapy for the treatment of adult patients with unresectable or metastatic HER2-positive (IHC 3+ or ISH+) breast cancer who have received a prior anti-HER2-based regimen either in the metastatic setting, or, in the neoadjuvant or adjuvant setting and have developed disease recu...
WARNING: INTERSTITIAL LUNG DISEASE and EMBRYO-FETAL TOXICITY Interstitial Lung Disease (ILD) and pneumonitis, including fatal cases, have been reported with ENHERTU. Monitor for and promptly investigate signs and symptoms including cough, dyspnea, fever, and other new or worsening respiratory sympto...
Want competitive intelligence?
See who's developing similar drugs and track their progress
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.