Trastuzumab deruxteca (Enhertu)

Antibody-Drug Conjugate · Approved since 2019

US Off-label IV 8 Clinical Trials
HER2

Description

Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate that targets HER2-positive colorectal cancers, which represent approximately 2-5% of all colorectal cancer cases. This precision medicine combines the HER2-targeting antibody trastuzumab with a potent topoisomerase I inhibitor payload. In colorectal cancer, it is specifically used for patients whose tumors demonstrate HER2 overexpression or amplification, providing a treatment option for this molecularly defined subset of patients.

Mechanism of Action

The drug binds to HER2 receptors on cancer cell surfaces through its trastuzumab component, allowing selective uptake into HER2-positive tumor cells. Once internalized, the linker is cleaved, releasing the cytotoxic deruxtecan payload (a topoisomerase I inhibitor) which causes DNA damage and cell death in both the targeted cell and nearby tumor cells through a bystander effect.

Molecular Targets

Side Effects

Interstitial lung disease Nausea Fatigue Vomiting Alopecia Decreased appetite Constipation Anemia Neutropenia Diarrhea Thrombocytopenia Increased liver enzymes

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT07124000 Not Applicable
Recruiting
DESTINY-PANTUMOUR04
United States
NCT06324357 Phase 1
Recruiting
Beamion BCGC-1: A Study to Find a Suitable Dose of Zongertinib Used Alone and in Combination With Other Treatments to Test Whether it Helps People With Different Types of HER2+ Cancer That Has Spread
United States, Belgium, China, France, Germany, Italy, Japan, South Korea, Spain
NCT05824975 Phase 1
Recruiting
A Study to Evaluate the Safety and Therapeutic Activity of GI-102 As a Single Agent and in Combination with Conventional Anti-cancer Drugs, Pembrolizumab or Trastuzumab Deruxtecan(T-DXd) in Patients with Advanced Solid Tumors (KEYNOTE-G08)
United States, South Korea
NCT05845450 Phase 2
Recruiting
Pre-operative Targeted Treatments in Molecularly Selected Resectable Colorectal Cancer (UNICORN)
Italy
NCT07318389 Early Phase 1
Not yet recruiting
ASCEND-CRC: Profiling and Targeting Dynamic Tumor Resistance in Patients With Metastatic Colorectal Cancer
United States
NCT05091528 Phase 1
Archived
A Safety and Activity Study of SBT6050 in Combination With Other HER2-directed Therapies for HER2-positive Cancers
United States
View all 8 clinical trials →