Jiangsu Hengrui Pharmaceuticals Co., Ltd. (Hengrui Pharma, 01276) has received National Medical Products Administration (NMPA) clearance for a third indication of its in-house developed antibody-drug conjugate (ADC) trastuzumab rezetecan for injection. The drug is now approved to treat adult patients with HER2-positive colorectal cancer (CRC) who have failed prior therapy with oxaliplatin, fluorouracil and irinotecan, making it the first anti-HER2 product sanctioned for CRC in China.
The newly endorsed product is classified as a Class 2.2 therapeutic biological and will be marketed in 0.1 g/vial injectable form as a prescription-only medicine. Trastuzumab rezetecan had previously been cleared domestically for (1) unresectable or metastatic non-small cell lung cancer with activating HER2 mutations after at least one systemic treatment and (2) locally advanced or metastatic HER2-positive breast cancer after one or more anti-HER2 regimens.
Regulatory approval was underpinned by the randomized, open-label Phase III HORIZON-CRC01 (SHR-A1811-III-309) trial led by Professor Li Jin of Shanghai GoBroad Cancer Hospital and Professor Yuan Ying of the Second Affiliated Hospital of Zhejiang University. The study met its primary endpoint and was showcased at the 2026 American Society of Clinical Oncology (ASCO) Annual Meeting.
Colorectal cancer remains one of the most prevalent malignancies worldwide, with HER2 alterations (amplification 5.8%, overexpression 5.0%, mutation 2.0%) representing a clinically significant subset lacking effective targeted options until now. The China Society of Clinical Oncology (CSCO) has already incorporated trastuzumab rezetecan into its 2026 Colorectal Cancer Guidelines for later-line HER2-positive CRC therapy.
Trastuzumab rezetecan employs a cleavable linker to release a high-permeability cytotoxin after internalization into HER2-expressing tumor cells, enabling both direct tumor cell apoptosis and a bystander killing effect. Eleven potential indications across lung, breast, gastric, colorectal, biliary and gynecological cancers have obtained Breakthrough Therapy Designation.
Comparable HER2-targeting ADCs on the Chinese market include Roche’s ado-trastuzumab emtansine, AstraZeneca/Daiichi Sankyo’s fam-trastuzumab deruxtecan, RemeGen’s disitamab vedotin and Kelun-Biotech’s trastuzumab botidotin. According to EvaluatePharma, global sales of these analogues reached approximately USD 8.16 billion in 2025.
Hengrui Pharma has invested an estimated RMB 2.14 billion in the development of trastuzumab rezetecan (unaudited). Management notes that post-approval manufacturing scale-up and commercialization remain subject to customary uncertainties, advising investors to consider associated risks.