For patients with HER2-positive advanced colorectal cancer (CRC), treatment options have remained limited after failure of standard chemotherapy.

Now, this treatment landscape has reached an important milestone.

On August 6, 2026, China’s National Medical Products Administration (NMPA) approved a new indication for Trastuzumab Rezetecan, a HER2-targeted antibody-drug conjugate (ADC) developed by Hengrui Pharmaceuticals, for the treatment of adult patients with HER2-positive colorectal cancer who have experienced disease progression after oxaliplatin-, fluoropyrimidine-, and irinotecan-based therapies.

This approval marks the third approved indication for Trastuzumab Rezetecan in China and makes it the first HER2-targeted ADC approved in China specifically for HER2-positive colorectal cancer.

As a China pharmaceutical wholesaler closely following global innovative drug approvals, DengYueMed provides an overview of this approval, the pivotal clinical data behind it, and what it means for the future of HER2-targeted ADC therapy in colorectal cancer.

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Why Do Patients with HER2-Positive Colorectal Cancer Need New Treatment Options?

Colorectal cancer (CRC) is one of the most commonly diagnosed cancers and a leading cause of cancer-related deaths worldwide. As precision oncology continues to evolve, HER2 has emerged as an important biomarker in colorectal cancer.

Studies have shown that approximately 2%–5% of patients with metastatic colorectal cancer (mCRC) harbor HER2 amplification or overexpression, most commonly in tumors with RAS and BRAF wild-type status. These patients often respond poorly to conventional anti-EGFR therapies.

For patients whose disease progresses after standard chemotherapy with Fluorouracil, oxaliplatin, and irinotecan, treatment options remain limited.

In recent years, antibody-drug conjugates (ADCs) have become one of the most promising therapeutic strategies for HER2-positive malignancies. By combining the targeting ability of monoclonal antibodies with highly potent cytotoxic agents, ADCs offer more precise tumor targeting while minimizing damage to healthy tissues, bringing new hope to patients with HER2-positive colorectal cancer.

Trastuzumab Rezetecan Receives Its Third Approved Indication

The newly approved indication allows Trastuzumab Rezetecan to be used for:

Adult patients with HER2-positive colorectal cancer whose disease has progressed after treatment with oxaliplatin, Fluorouracil, and irinotecan.

This represents the drug’s third approved indication in China, following approvals for:

• Adults with unresectable locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring HER2 (ERBB2)-activating mutations who have received at least one prior systemic therapy.
• Adults with locally advanced or metastatic HER2-positive breast cancer previously treated with one or more anti-HER2 therapies.

With this latest approval, Trastuzumab Rezetecan further expands its role across HER2-positive solid tumors.

Phase III HORIZON-CRC01 Trial Met Its Primary Endpoint

The new indication is supported by positive results from the pivotal Phase III HORIZON-CRC01 trial (NCT06199973).

This multicenter, open-label, randomized controlled study enrolled 130 patients with centrally confirmed HER2-positive (IHC 3+ or IHC 2+/ISH+), RAS/BRAF wild-type advanced colorectal cancer whose disease had progressed after fluoropyrimidine-, oxaliplatin-, and irinotecan-based therapies.

The primary endpoint was progression-free survival (PFS) assessed by an Independent Review Committee (IRC) according to RECIST v1.1. Key secondary endpoints included overall survival (OS), objective response rate (ORR), and safety.

As of October 31, 2025, with a median follow-up of 9.6 months, the study reported the following results:

Endpoint	Trastuzumab Rezetecan	Standard of Care (SOC)
Median PFS (IRC)	5.5 months	2.8 months
Hazard Ratio (HR)	0.33	—
Objective Response Rate (ORR)	40.7%	4.5%
Duration of Response (DoR)	4.4 months	3.4 months
Overall Survival (OS)	Data not yet mature	23% reduction in the risk of death (HR=0.77)

Investigator-assessed PFS results were consistent with the IRC assessment, with median PFS of 5.6 months versus 2.8 months, respectively.

Overall, Trastuzumab Rezetecan significantly prolonged progression-free survival and substantially improved objective response rates compared with standard treatment.

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Favorable Safety Profile

In addition to demonstrating improved efficacy, Trastuzumab Rezetecan also showed a favorable safety profile.

No new safety signals were identified during the study, and no patients discontinued treatment because of treatment-related adverse events (TRAEs) in either treatment group.

Investigators concluded that for patients with HER2-positive, RAS/BRAF wild-type advanced colorectal cancer who had progressed after standard therapies, Trastuzumab Rezetecan offers meaningful clinical benefit with manageable safety, making it a promising new treatment option.

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Competition in the HER2 ADC Landscape Continues to Intensify

HER2-targeted ADCs have become one of the fastest-growing areas of oncology drug development worldwide.

To date, five HER2-targeted ADCs have been approved in China, including:

• Trastuzumab Emtansine
• Trastuzumab Deruxtecan
• Disitamab Vedotin
• Trastuzumab Rezetecan
• Trastuzumab Botidotin

However, before this approval, no HER2-targeted therapy had been approved in China specifically for HER2-positive colorectal cancer.

With this indication, Trastuzumab Rezetecan becomes the first HER2-targeted ADC approved for this patient population in China, filling an important treatment gap.

Meanwhile, competition in the HER2-positive colorectal cancer ADC field continues to accelerate. Several HER2-targeted ADC candidates have already entered Phase III clinical development, including:

• TQB2102 (Chia Tai Tianqing)
• Anbenitamab Repodatecan (Alphamab Oncology/CSPC)
• BL-M07D1 (Biokin)

In addition, Trastuzumab Deruxtecan and Disitamab Vedotin are also being investigated for HER2-positive colorectal cancer.

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Looking Ahead: HER2 ADC Therapy May Move Into Earlier-Line Treatment

Development of Trastuzumab Rezetecan is not limited to later-line therapy.

Early clinical studies evaluating Trastuzumab Rezetecan in combination with chemotherapy and the bevacizumab biosimilar BP102 as first-line treatment for HER2-expressing metastatic colorectal cancer have already demonstrated encouraging preliminary antitumor activity.

If ongoing clinical studies continue to produce positive results, HER2-targeted ADC therapy may move into earlier lines of treatment, offering more patients access to precision medicine at an earlier stage of disease.

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Conclusion

The approval of Trastuzumab Rezetecan for HER2-positive colorectal cancer represents not only its third approved indication in China, but also makes it the first HER2-targeted ADC approved in China specifically for HER2-positive colorectal cancer.

For patients whose disease has progressed after standard therapy, this approval provides a valuable new treatment option. More broadly, it also highlights the continued advancement of China-developed HER2-targeted ADCs in the treatment of solid tumors.

As more innovative ADC therapies enter late-stage clinical development and combination treatment strategies continue to evolve, HER2-targeted ADCs are expected to play an increasingly important role in reshaping the treatment landscape for HER2-positive colorectal cancer.

As a China-based pharmaceutical wholesaler specializing in global innovative medicine supply chain services, DengYueMed closely follows the latest developments in oncology therapies, rare disease medicines, biologics, and other innovative pharmaceutical products.

We remain committed to sharing timely updates on global drug approvals, clinical research, and pharmaceutical innovation, helping healthcare providers, pharmaceutical distributors, and industry partners stay informed about the latest advances in medicine.