AiWeiDa® Approved for New Indication HER2-Positive Colorectal Cancer: A New Option for Precision Treatment
In recent years, Antibody-Drug Conjugates (ADCs) have continued to drive advances in precision oncology, gradually becoming one of the most important areas of innovation in cancer drug development. From breast and lung cancer to gastrointestinal malignancies, an increasing number of ADC therapies have entered clinical development, offering new treatment possibilities for patients who have limited responses to conventional therapies or few remaining standard treatment options.
On August 6, 2026, AiWeiDa® (Trastuzumab Rezetecan for Injection) was officially approved by the National Medical Products Administration (NMPA) for its third indication: the treatment of adult patients with HER2-positive colorectal cancer whose disease has progressed following treatment with oxaliplatin, fluoropyrimidine, and irinotecan. The approval of this new indication marks a significant milestone in AiWeiDa approved for new indication HER2-positive colorectal cancer, making it the first domestically developed anti-HER2 ADC approved in China for HER2-positive colorectal cancer.
More importantly, the approval addresses a longstanding need for high-level clinical evidence and targeted treatment options in this specific patient population. AiWeiDa® is supported by the first positive randomized, controlled Phase III study of an anti-HER2 therapy in HER2-positive colorectal cancer, providing important evidence for the use of HER2-targeted ADC therapy in this setting.
For global healthcare institutions, pharmaceutical procurement organizations, and eligible patients, the approval of AiWeiDa® for this new indication further expands the potential application of innovative cancer therapies and provides an additional option for international pharmaceutical procurement and access to HER2-targeted treatment.
Key Product Information
AiWeiDa® (Trastuzumab Rezetecan for Injection) is an innovative HER2-targeted ADC developed in China, with its clinical applications continuing to expand across multiple tumor types. The product has established a broad development and treatment profile across solid tumors. Key product information is summarized below:
| Item | Key Information |
|---|---|
| Brand Name | AiWeiDa® |
| Generic Name | Trastuzumab Rezetecan for Injection |
| Drug Class | ADC (Antibody-Drug Conjugate) |
| Target | HER2 |
| Approved Indications | HER2-mutant non-small cell lung cancer (NSCLC), HER2-positive breast cancer, and HER2-positive colorectal cancer (newly approved) |
| Route of Administration | Intravenous infusion, once every 3 weeks |
| Strength | 0.1 g/vial (lyophilized powder for injection) |
| Approval of Colorectal Cancer Indication | August 2026 |
✨ It is worth noting that the new colorectal cancer indication was officially approved approximately six months after the New Drug Application (NDA) was accepted for priority review. The expedited review process reflects the regulatory focus on addressing unmet clinical needs and highlights the potential clinical value of this new treatment option for patients with HER2-positive colorectal cancer.
Clinical Challenges in HER2-Positive Colorectal Cancer
Colorectal cancer (CRC) is one of the most common malignancies worldwide and remains a major cause of cancer-related morbidity and mortality. HER2 is an established therapeutic target in oncology, and HER2-targeted therapies have already been widely used in breast cancer and gastric cancer, helping improve outcomes for selected patients. However, the treatment landscape for HER2-positive colorectal cancer has historically had fewer established targeted treatment options.
Clinical data suggest that HER2-positive colorectal cancer accounts for approximately 2%–5% of colorectal cancer cases. This subgroup may have distinct molecular characteristics and, in certain settings, limited responses to conventional therapies. For patients whose disease continues to progress after treatment with fluoropyrimidines, oxaliplatin, and irinotecan, available later-line treatment options remain relatively limited, highlighting the need for additional HER2-targeted therapies.
The approval of AiWeiDa® for HER2-positive colorectal cancer therefore provides a new treatment option for adults with HER2-positive advanced colorectal cancer following failure of standard chemotherapy, further expanding the role of HER2-directed ADC therapy in colorectal cancer.
Precision Targeting: Mechanism of Action and Distinctive Design of AiWeiDa®
Compared with conventional chemotherapy, which can affect both cancerous and healthy cells, Trastuzumab Rezetecan utilizes advanced antibody-drug conjugate (ADC) technology to selectively target HER2-expressing tumor cells and deliver a potent cytotoxic payload. This targeted approach is designed to enhance antitumor activity while maintaining a manageable safety profile.
1. Mechanism of Action
AiWeiDa® consists of three key components: a humanized anti-HER2 monoclonal antibody, a cleavable tetrapeptide linker, and a highly potent cytotoxic payload.
After administration, the antibody component selectively binds to HER2 antigens on the surface of tumor cells. The ADC is then internalized into the cancer cell and transported to lysosomes, where the linker is cleaved and releases the DNA topoisomerase I inhibitor SHR169265. The released payload interferes with DNA replication and causes DNA damage, ultimately promoting tumor-cell death.
The payload also has high membrane permeability, which may allow it to diffuse from targeted tumor cells into neighboring HER2-low or HER2-negative cells. This mechanism, known as the bystander effect, may further enhance the overall antitumor activity of the ADC.
2. Distinctive Drug Design: Balancing Antitumor Activity and Safety
The molecular design of AiWeiDa® incorporates several features intended to optimize the balance between efficacy and safety:
- Potent payload: AiWeiDa® utilizes the topoisomerase I inhibitor SHR169265, with favorable lipophilicity and membrane permeability that may contribute to its cytotoxic activity across tumor cells with different levels of HER2 expression.
- Optimized drug-to-antibody ratio (DAR): The drug is designed with a DAR of approximately 6:1. Rather than directly comparing DAR values between different ADCs, this optimized ratio is intended to maintain an appropriate balance between payload delivery, pharmacological activity, and drug stability.
- Stable linker design: The cleavable linker incorporates structural modifications, including a chiral cyclopropyl group, designed to improve linker stability and help minimize premature payload release before the ADC reaches the target tumor cells.
Preclinical studies have demonstrated antitumor activity in tumor models with different levels of HER2 expression, supporting further clinical evaluation of AiWeiDa® in HER2-targeted cancer treatment.
Phase III Clinical Evidence: HORIZON-CRC01 Demonstrates Significant PFS Benefit
The approval of AiWeiDa® for HER2-positive colorectal cancer was supported by HORIZON-CRC01, a randomized, controlled Phase III study evaluating an anti-HER2 therapy in patients with HER2-positive colorectal cancer. The study was led by Professor Jin Li and Professor Ying Yuan, and its results were presented at the 2026 ASCO Annual Meeting, providing important high-level clinical evidence for the use of AiWeiDa® in this patient population.
1. Study Design
The study enrolled 130 patients with RAS/RAF wild-type, HER2-positive advanced colorectal cancer. HER2 positivity was defined as IHC 3+ or IHC 2+/ISH+.
Patients were randomized in a 2:1 ratio to receive either AiWeiDa® (n=86) or standard treatment (n=44), which included fruquintinib, regorafenib, or trifluridine/tipiracil. Patients in the standard-treatment group were permitted to cross over to AiWeiDa® after disease progression.
2. Key Efficacy Results
| Endpoint | AiWeiDa® Group | Standard Treatment Group | Key Result |
|---|---|---|---|
| Median PFS | 5.5 months | 2.8 months | 67% reduction in risk of disease progression (HR=0.33, P<0.0001) |
| Objective Response Rate (ORR) | 40.7% | 4.5% | 36.2 percentage-point improvement (P<0.0001) |
| Median DoR | 4.4 months | 3.4 months | Longer observed duration of response |
| Median OS | Not reached | Not reached | OS data remain immature; HR=0.77 (95% CI: 0.35–1.73) |
The results demonstrated a statistically significant improvement in progression-free survival and objective response rate with AiWeiDa® compared with standard treatment. Because overall survival data remain immature and the confidence interval for the OS hazard ratio crosses 1, the current results should be interpreted as requiring further follow-up to determine the potential overall survival benefit.
Subgroup analyses generally showed consistent treatment effects across different patient characteristics, including HER2 expression level, number of prior treatment lines, prior anti-HER2 therapy, primary tumor location, and number of metastatic sites. However, individual subgroup sample sizes were limited, so these findings should be interpreted cautiously.
3. Manageable Safety Profile
The safety analysis showed that Grade ≥3 treatment-related adverse events occurred in 48.8% of patients in the AiWeiDa® group, compared with 50.0% in the standard-treatment group. Overall, the safety profile was manageable, with no new safety signals identified.
AiWeiDa® is administered by intravenous infusion once every three weeks, providing a standardized dosing schedule that can facilitate routine clinical management and treatment planning.
Industry Significance: Expanding Precision Treatment Options in Colorectal Cancer
The approval of this new indication marks the third major solid-tumor indication for AiWeiDa® (Trastuzumab Rezetecan) following its applications in lung and breast cancer. It further expands the clinical role of HER2-targeted ADC therapy across multiple HER2-positive solid tumors and provides an additional precision treatment option for patients with HER2-positive colorectal cancer. AiWeiDa® has also been included in the relevant treatment recommendations of the 2026 edition of the CSCO Guidelines for Colorectal Cancer Diagnosis and Treatment, providing a new later-line treatment option for patients with HER2-positive advanced colorectal cancer.
Beyond later-line treatment, AiWeiDa® is also being investigated in the first-line setting. Data from a Phase I/II study presented at the 2026 ASCO Annual Meeting showed that first-line treatment with AiWeiDa® in combination with bevacizumab plus mFOLFOX achieved an objective response rate (ORR) of 90.5%, a disease control rate (DCR) of 100%, and a 12-month progression-free survival (PFS) rate of 94.7%. These preliminary findings demonstrated encouraging antitumor activity, with a manageable overall safety profile. A corresponding pivotal Phase III clinical trial has now been initiated. If confirmed in the Phase III study, these findings could further expand the clinical application of AiWeiDa® in first-line treatment of HER2-positive advanced colorectal cancer.
As of now, Trastuzumab Rezetecan has been designated as a Breakthrough Therapy by the Center for Drug Evaluation (CDE) 11 times, covering multiple solid tumors including lung cancer, breast cancer, colorectal cancer, gastric cancer, biliary tract cancer, and ovarian cancer. The continued development of the drug across multiple tumor types highlights the expanding clinical potential of this innovative HER2-targeted ADC therapy.
Global Pharmaceutical Supply and Procurement Support
Following the approval of the new indication for Trastuzumab Rezetecan, its clinical potential in HER2-positive colorectal cancer has attracted growing attention.
👉 As a pharmaceutical wholesaler specializing in innovative and specialty medicines, DengYue Pharmacy provides pharmaceutical supply and procurement support to qualified healthcare institutions, pharmaceutical distributors, and professional procurement organizations, subject to the regulatory requirements of the destination country or region.
Core Services:
- Innovative medicine procurement consultation
- Supply through authorized pharmaceutical channels
- International pharmaceutical procurement coordination
- Export and logistics solution consultation
- Professional cold-chain transportation coordination
- Real-time inventory and supply availability inquiries
All pharmaceutical supply activities are conducted in accordance with applicable Chinese pharmaceutical export regulations and the regulatory requirements of the destination country or region. Prescription medicines should be procured through legally authorized local channels and used under the supervision of qualified healthcare professionals.
Conclusion
The approval of AiWeiDa® (Trastuzumab Rezetecan) for HER2-positive colorectal cancer represents an important development in the application of ADC therapies to precision treatment of gastrointestinal cancers. Supported by its innovative mechanism of action and Phase III clinical evidence, AiWeiDa® provides a new treatment option for patients with HER2-positive colorectal cancer whose disease has progressed following standard therapies.
As clinical research continues to explore its potential in first-line treatment and its international availability develops, Trastuzumab Rezetecan may further expand the clinical application of HER2-targeted ADC therapy across solid tumors. Its continued development also highlights the growing role of precision oncology and innovative ADC therapies in addressing unmet treatment needs.
AiWeiDa® | Trastuzumab Rezetecan for Injection | Lung Cancer | DengYueRX
Trastuzumab Rezetecan for Injection is a novel HER2-targeted ADC drug for non-small cell lung cancer. It combines the high targeting specificity of monoclonal antibody and powerful cytotoxicity of small-molecule payload, achieving precise killing of HER2-abnormal lung cancer cells.
FAQ About AiWeiDa® Approved for New Indication HER2-Positive Colorectal Cancer
What are the potential new treatments for colon cancer in 2026?
Data at ASCO 2026 Offer Clues. Data from two studies suggest that circulating tumor DNA (ctDNA) testing could help clarify adjuvant treatment decisions in colorectal cancer, including identifying which patients are likely to benefit from chemotherapy and how long treatment should continue.
What is the treatment for HER2-positive colorectal cancer?
What treatment options are available?
Colorectal tumors that have HER2 amplification and overexpression and are RAS and BRAF wild type should be treated with dual-targeted therapy against HER2. This includes the combination of trastuzumab with either pertuzumab or lapatinib, or with chemotherapy.
What is the survival rate for patients with HER2-positive colon cancer?
They reported that patients with HER-2 positivity showed a trend towards a better disease-free survival and a benefit in cancer-specific survival, and the 5-year survival rate was 96.0% (HER-2 positive) versus 80.0% (HER-2 negative).
How fast can HER2-positive cancer grow?
One study found that HER2-positive tumors grew at a rate of 0.859% per day, meaning they can become nearly one percent bigger each day. However, it’s typically very responsive to treatments. Triple negative breast cancer: The same study found that triple negative breast cancer tumors can grow at 1.003% per day.
Does HER2-positive always come back?
While HER2 positive breast cancer recurrence affects some patients, recent advancements in targeted therapies and long-term treatment approaches have made relapse less likely than ever before. The majority of patients with HER2 positive cancer do not experience recurrence.
