On September 29, 2022 LEPU BIOPHARMA reported 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 (Press release, Lepu Biopharma, SEP 29, 2022, View Source [SID1234633515]). 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. The Company is also pleased to announce that the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) of the People’s Republic of China (PRC) has granted MRG003 breakthrough therapy designation for the treatment of recurrent or metastatic nasopharyngeal cancer (R/M NPC).
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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) (Free ASCO Whitepaper) 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.
Breakthrough therapy designation granted by the CDE to MRG003 for the treatment of R/M NPC Breakthrough therapy designation is for innovative or modified new drugs that treat a condition that is seriously life-threatening or has serious quality-of- life impairment, and such condition has no effective therapies or compared with current available therapies, sufficient evidence demonstrates an obvious advantage in clinic treatment of the new drugs.
Previously, MRG003 has been granted the Orphan-drug Designation by the Food and Drug Administration of the United States (the "FDA") for the treatment of R/M NPC. MRG003 is the most advanced EGFR-targeted ADC in clinical-stage development in China and has the potential to seize market opportunities. The breakthrough therapy designation, which helps to expedite the development and review of the drug by the CDE, represent an encouraging signal to the promotion of MRG003 as well as the strategy of developing market-differentiating pipeline of the Company.
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 MRG003
MRG003 is an ADC comprised of an EGFR-targeted monoclonal antibody ("mAb") conjugated with the potent microtublin inhibiting payload monomethyl auristatin E ("MMAE") via a valinecitrulline linker. It binds specifically with high affinity to EGFR on the surface of tumor cells, releases the potent payload upon internalization and lysosomal protease cleavage of the linker and results in tumor cell death. EGFR is highly expressed in colorectal cancer, lung cancer, head and neck cancer and other malignant solid tumors, and is expressed in 89% advanced NPC. Therefore, EGFR is an important target for cancer treatment. In China, the Company is conducting exploring research of MRG003 in several indications and amongst others, patient enrollment was completed in March 2022 for exploratory Phase II clinical study of MRG003 in advanced NPC. It has entered the follow-up period and clinical data is outstanding.