On September 29, 2022 (Beijing time), LEPU BIOPHARMA (2157.HK) announced that its first innovative biological drug, anti-PD-1 antibody – Puyouheng (generic name: pucotenlimab injection) has been approved for marketing by the National Medical Products Administration (NMPA) for the indication of unresectable or metastatic melanomas after the failure of previous systemic therapy. It is another approved indication for Puyouheng (pucotenlimab injection) following the approval of the indication of MSI-H/dMMR solid tumor in July this year, and will bring a new immunotherapy treatment option for patients with melanoma in China.

Bringing a new option to tumor immunotherapy for patients

This approval was mainly based on a single-arm, open-label, pivotal phase II clinical study with a primary endpoint of the objective response rate (ORR) assessed by the Independent Review Committee (IRC) according to the RECIST 1.1. A total of 119 patients were enrolled in this trial. As of July 30, 2021, the ORR assessed by the IRC was 20.2% (95% CI: 13.4-28.5, 1 case of complete response, 23 cases of partial response). The results of the study show that Puyouheng brings significant benefits to patients in the treatment of unresectable or metastatic melanomas after the failure of previous systemic therapy, and meets the preset primary endpoint with excellent safety. The results of the clinical study were first published at the 2021 American Society of Clinical Oncology (ASCO) annual meeting.

Melanoma is a malignant tumor of melanocytes. Although melanoma only accounts for less than 5% of skin cancers, it is the deadliest form which takes up more than 75% of all deaths caused by skin cancers. Surgical treatment is the main option for malignant melanomas in the early stage with a better prognosis, while the treatment of advanced melanomas is limited with a poor prognosis. As an innovative anti-PD-1 humanized monoclonal antibody drug, Puyouheng innovatively prolongs its half-life through triple mutations and can bind to PD-1 with high affinity to restore the ability of immune cells to kill cancer cells by blocking the binding of PD-1 to its ligands PD-L1 and PD-L2.

With a strong affinity to PD-1 and outstanding binding stability, Puyouheng has demonstrated excellent anti-tumor efficacy in both in vitro and clinical trials.

Actively conducting studies on the combination therapy within our pipelines under the support of a clinical layout covering multiple solid tumors

Puyouheng has been approved for marketing with indications of microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) advanced solid tumors and advanced melanomas. In addition to the two approved indications, focusing on Puyouheng, LEPU BIOPHARMA is accelerating its development in the treatment of multiple solid tumors and actively investigating combined tumor immune immunotherapies, including the treatment of gastric cancer, liver cancer, lung cancer, and other cancer types with high incidence. In terms of international development, LEPU BIOPHARMA is also speeding up its efforts to expand the international market, promoting joint development, cooperation and authorization of new drugs globally. In January 2022, it obtained IND approval from the US FDA for pucotenlimab in the treatment of advanced solid tumors.

About Puyouheng (pucotenlimab injection)

Puyouheng (pucotenlimab injection) is a humanized IgG4 monoclonal antibody against human PD-1 independently developed in China. It can bind to PD-1 with high affinity to restore the ability of immune cells to kill cancer cells by blocking the binding of PD-1 to its ligands PD-L1 and PD-L2. Puyouheng (pucotenlimab injection) adopts an innovative molecular design to prolong its half-life, showing strong clinical anti-tumor activity and good safety. The innovative use of antibody engineering technology to introduce triple mutations in the Fc region improves the binding affinity of FcRn, thereby prolonging the drug’s half-life significantly, showing its promising clinical efficacy and drug compliance in patients. Compared with all rival anti-PD-1 antibodies that have been marketed or entered phase III clinical trials, the mean half-life of Puyouheng (pucotenlimab injection) is 21.8 days (single dosing) and 38.2 days (steady-state). In addition, the prolonged half-life does not cause additional adverse events, indicating the excellent clinical efficacy of the drug.

About LEPU BIOPHARMA (2157.HK)

LEPU BIOPHARMA is committed to innovation, focusing on the discovery, development and commercialization of first-in-class and best-in-class drug candidates in targeted anti-tumor therapy and immunotherapy drugs in China and the US. The company’s mission is to develop the safest, most effective, and most accessible drugs for patients to improve their quality of life and fill the huge demand gap in the medical system. The company attaches great importance to the continuous construction of its commercialization capabilities, and strives to achieve a strong transformation from core technologies to finished drugs as well as the goal of industrialization. At present, the product pipeline of LEPU BIOPHARMA covers three major areas, namely immunotherapies, ADC targeted therapies and oncolytic virus drugs, including 1 commercially marketing drug and 7 drug candidates at the clinical stage (5 of which are ADC drugs) and the combination therapies of multiple major drug candidates at the clinical stage. The company houses the leading ADC drug candidate pipeline in China.