In the fiercely competitive global race for anti-cancer drug development, targeted radiopharmaceuticals are emerging as a rising star in cancer treatment due to their unique advantages of "precise targeting, high efficiency, and low toxicity." Recently, Shandong Weizhi Zhike Pharmaceutical 's 177Lu-PSMA-VG01 injection received implied clinical approval from the NMPA, marking a crucial step forward for domestically produced targeted radiopharmaceuticals in the treatment of prostate cancer.

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Technical Analysis

Prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein that plays a crucial role in prostate cancer. Normally, PSMA is expressed at low levels in prostate tissue, but its expression increases dramatically after cell carcinogenesis. It is significantly upregulated in hormone-refractory and metastatic prostate cancer, making it an ideal target for molecular targeted therapy of prostate cancer. Mechanistically, PSMA possesses glutamate carboxypeptidase II activity, hydrolyzing N-acetyl-L-aspartyl-L-glutamate (NAAG), regulating extracellular glutamate levels, influencing neurotransmission and the tumor microenvironment, promoting cancer cell growth and spread, and potentially participating in cell adhesion, migration, and angiogenesis, thus playing a vital role in tumor invasion and metastasis.

The core therapeutic mechanism of 177Lu-PSMA-VG01 injection is to utilize β particles released by the radioactive isotope 177Lu to attack cancer cells. When 177Lu decays, the β particles transfer radiation energy to cells expressing PSMA and surrounding cells. Once inside the cell, these β particles interact with intracellular substances, inducing DNA damage. When DNA is severely damaged and cannot be repaired, the cell cannot perform normal life activities and eventually dies, thereby inhibiting the proliferation and spread of cancer cells.

Compared to traditional radiotherapy, 177Lu-PSMA-VG01 injection offers a precision advantage . Traditional radiotherapy, while killing cancer cells, often causes severe collateral damage to surrounding normal tissues. Because traditional radiotherapy uses external irradiation, the radiation inevitably passes through many normal tissues as it penetrates the body to reach the tumor site, damaging the cells in these tissues and leading to a series of side effects such as radiation pneumonitis and radiation enteritis. In contrast, 177Lu-PSMA-VG01 injection, through the specific targeted binding of PSMA-VG01 to PSMA-positive cells, can precisely deliver 177Lu to cancer cells, achieving targeted elimination of cancer cells. This significantly reduces radiation damage to normal tissues, lowers the probability of side effects, and provides patients with a gentler and safer treatment option.

Compared to existing targeted drugs, 177Lu-PSMA-VG01 injection offers unique advantages. While existing targeted drugs can target specific points on cancer cells, their efficacy is poor due to tumor heterogeneity, with some cancer cells being insensitive and developing drug resistance with long-term use. 177Lu-PSMA-VG01 injection exhibits a 2.6-fold increased affinity for PSMA and a 2.4-fold increased internalization efficiency , enabling it to act rapidly and precisely on cancer cells. It also maintains a long-lasting effect, remaining in tumor tissue for sustained killing, while exhibiting low uptake levels in normal tissues, resulting in good safety and reduced damage to normal tissues.

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Competitive Landscape

In the fiercely competitive global market for targeted radiopharmaceuticals, numerous pharmaceutical companies are vying for a place in the market, each relying on its unique technological approach and product advantages.

Novartis' Pluvicto (177Lu-PSMA-617) is undoubtedly a strong contender in the field of targeted nuclear medicine for prostate cancer. In March 2022, it was approved by the US FDA for the treatment of patients with prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC), bringing a revolutionary breakthrough to the treatment of this disease. Since its launch, Pluvicto's market performance has been phenomenal, with global sales reaching $1.392 billion in 2024, a year-on-year increase of 42%, quickly becoming a blockbuster product with enormous market potential and clinical value. The key to its success lies in its precise targeting; by specifically binding to PSMA-positive cells, it achieves precise attack on cancer cells, greatly improving treatment efficacy while reducing damage to normal tissues, bringing patients a better quality of life and treatment experience.

Bayer's Nubeqa (dalolutamide) is another drug with significant influence in the treatment of prostate cancer. It is an oral androgen receptor inhibitor that competitively inhibits androgen receptor binding, blocks nuclear translocation and transcriptional activation, thereby suppressing tumor growth at its source. On July 21, 2025, the European Commission approved Nubeqa in combination with androgen deprivation therapy (ADT) for metastatic hormone-sensitive prostate cancer (mHSPC), its third approved indication. Based on the Phase III ARANOTE trial, compared with placebo plus ADT, dalolutamide plus ADT significantly reduced the risk of radiographic progression or death by 46% (HR 0.54, P < 0.0001), providing a new and effective treatment option for patients with this stage of prostate cancer. Moreover, Nubeqa does not cross the blood-brain barrier and has fewer central nervous system side effects, a unique advantage that makes it stand out among many similar drugs and more suitable for long-term use.

In China, numerous companies are actively investing in targeted radiopharmaceuticals, demonstrating a robust development trend. Hengrui Medicine , a leading innovative drug company in China, is also actively involved in radiopharmaceuticals. Its subsidiary, Tianjin Hengrui, has spearheaded the Tianjin Radiopharmaceutical Innovation Consortium, dedicated to building an integrated R&D and transformation platform for radionuclide drugs for tumor diagnosis and treatment. Research projects on zinc-68 isotopes and other areas have already commenced, injecting strong innovative vitality into radiopharmaceutical development. Xiantong Pharmaceutical is one of the earliest companies in China to engage in radiopharmaceutical R&D, possessing rich experience and profound technological accumulation. Its core investigational product, XTR008, is a 177Lu-labeled somatostatin receptor (SSTR)-targeting radioligand for the treatment of neuroendocrine tumors. Currently in the registration stage, it is expected to bring new hope to patients with neuroendocrine tumors. Zhihe Bio is also actively exploring the field of radiopharmaceuticals, with its products demonstrating unique potential in tumor treatment, continuously driving the advancement of radiopharmaceutical technology in China.

Compared to domestic and international competitors, Vichitech's 177Lu-PSMA-VG01 injection has significant advantages. In terms of affinity, it can rapidly enter cancer cells to exert its effect. It also exhibits significant advantages in long-term retention and safety. Multi-dose and multi-model pharmacodynamic studies show that at the same dose, it has a stronger tumor-suppressive effect, and at low doses, its efficacy is comparable to or better than Pluvicto. It holds promise for reducing the amount of radionuclide used, lowering radiotoxicity, and maintaining efficacy, providing patients with a safer and more effective treatment option.

Weizhi Technology faces numerous challenges. While its 177Lu-PSMA-VG01 injection boasts significant advantages, the radiopharmaceutical market is fiercely competitive. International giants like Novartis and Bayer hold dominant positions due to their strong R&D capabilities, extensive market channels, and rich clinical experience. As a latecomer, Weizhi Technology needs to redouble its efforts in market promotion, brand building, and accumulating clinical application experience. Furthermore, radiopharmaceutical R&D and production are costly and technically challenging, requiring substantial investment in talent, equipment, and funding. Weizhi Technology must increase its R&D investment, attract and cultivate high-end talent, improve its production facilities and quality control system, and ensure product quality and safety to meet market and patient needs.
Targeted radiopharmaceutical track observation

Targeted radiotherapy, as an emerging force in the field of cancer treatment, is standing at the forefront of the times, and its development potential has attracted much attention. It is expected to become the next breakthrough point in cancer treatment.

From a technological perspective , the field of targeted radiopharmaceuticals is seeing a continuous stream of innovative achievements and a very broad development prospect. With the rapid development of science and technology, significant progress has been made in the research and development of novel radionuclides. Alpha nuclides , with their high linear energy transfer (LET) and short range characteristics, have demonstrated unique advantages in tumor treatment. They can more precisely destroy the DNA of cancer cells, efficiently killing them while reducing damage to surrounding normal tissues, bringing new hope to tumor treatment. Remarkable breakthroughs have also been achieved in the innovation of carrier molecules. In addition to traditional small molecules and peptides, antibodies are beginning to emerge as carrier molecules. The emergence of bispecific antibodies has injected new vitality into the development of targeted radiopharmaceuticals. Bispecific antibodies can bind to two different targets simultaneously, which not only improves the drug's targeting but also enhances its therapeutic effect, providing more possibilities for tumor treatment. The development of therapeutic technologies has further enhanced targeted radiopharmaceuticals. Through radiolabeling, doctors can observe the drug target binding capacity and metabolic kinetics in real time, adjusting treatment plans promptly during treatment to achieve personalized treatment. This not only improves the precision of treatment but also effectively reduces research and development risks, providing patients with higher-quality treatment services.

Policy support has also provided strong guarantees for the development of targeted radiopharmaceuticals. In recent years, governments around the world have introduced relevant policies to increase support for the biopharmaceutical field, and targeted radiopharmaceuticals, as an important component of innovative drugs, have also received policy favor. The promulgation of the "Medium and Long-Term Development Plan for Medical Isotopes (2021-2035)" has pointed the way for the development of nuclear medicine in China, further standardizing and promoting its development. The plan clearly states that it is necessary to strengthen the independent supply capacity of medical isotopes, improve the research and development and production level of radiopharmaceuticals, and promote the application of radiopharmaceuticals in clinical practice. The introduction of this policy has provided a favorable policy environment and development opportunities for the development of targeted radiopharmaceuticals in China. In terms of the approval process, relevant departments are also constantly optimizing and accelerating the approval speed of targeted radiopharmaceuticals, so that more patients can benefit from these innovative drugs as soon as possible. Some clinical trial applications and marketing applications for targeted radiopharmaceuticals have been approved in a short period of time, greatly shortening the drug research and development and marketing cycle.

Targeted radiopharmaceuticals are expanding into new areas by integrating with other popular technologies. Combined with PROTAC technology, they can target and degrade specific proteins to enhance efficacy; similar to ADC technology, they demonstrate potential for treating solid tumors; and they also have unique advantages in the treatment of hematological malignancies, precisely killing tumor cells while reducing damage to normal blood cells.

However, the development of targeted radiopharmaceuticals faces challenges. Dosage control requires precise control of the radionuclide dosage to avoid damage while ensuring efficacy. Supply chain issues include unstable and costly radionuclide supply; for example, Lu-177 isotopes rely on imports, and medical reactor capacity is limited. Physician training is also crucial; targeted radiopharmaceuticals are a novel approach, and a shortage of qualified professionals, coupled with insufficient physician knowledge and experience, hinders clinical adoption.

Despite the challenges, the future development trend of targeted radiopharmaceuticals remains promising. With continuous technological advancements and innovation, these challenges are expected to be gradually resolved.