On November 10, 2025, according to the official website of the National Medical Products Administration (NMPA), the generic drug of Class 3, Enzalutamide Tablets, submitted by Kelun Pharmaceutical, was approved for marketing and deemed to have passed the consistency evaluation, making it the first generic drug enterprise in China to receive approval for Enzalutamide Tablets.

As a super blockbuster in the field of androgen receptor (AR) inhibitors, the clinical value and market potential of Enzalutamide (Xtandi^®) have long been verified. It is jointly developed by Astellas and Pfizer, is a second-generation highly selective androgen receptor (AR) inhibitor. Its core advantage lies in its triple-block mechanism of action, which fundamentally inhibits the proliferation and metastasis of prostate cancer cells. Firstly, Enzalutamide can competitively bind to the androgen receptor, preventing the binding of androgens such as testosterone and dihydrotestosterone to the receptor, thereby cutting off the “signal source” for cancer cell growth. Secondly, even if some receptors have been activated, Enzalutamide can still inhibit the transport of receptors into the cell nucleus, blocking the signal transduction pathway. Lastly, it can also prevent the androgen receptor from binding to the promoter region of target genes in the cell nucleus, blocking the expression of genes related to cancer cell proliferation downstream. This multi-site, comprehensive blocking mode enables it to exert significant efficacy even in patients resistant to traditional endocrine therapy, making it the standard treatment for advanced castration-resistant prostate cancer (CRPC).

In terms of clinical efficacy, the advantages of enzalutamide have been fully validated by multiple international multicenter Phase III studies. The ARCHES study showed that enzalutamide combined with androgen deprivation therapy (ADT) in patients with metastatic hormone-sensitive prostate cancer (mHSPC) significantly reduced the risk of radiographic progression or death by 61%, with a median overall survival extension of more than 26 months compared to the placebo group, and benefits were observed in patients with different tumor burdens. The latest TALAPRO-2 international Phase III clinical study further expanded its application value. The study confirmed that the combination of talazoparib and enzalutamide in patients with advanced prostate cancer carrying homologous recombination repair (HRR) gene mutations not only effectively controls tumor progression but also extends the patients’ high-quality life time by more than 7 months and reduces the risk of quality of life decline by 31%.

In terms of safety, enzalutamide also performs exceptionally well. Compared to similar AR inhibitors such as apalutamide and rezvilutamide, enzalutamide has not been reported to significantly increase the risk of adverse reactions such as rash and hepatotoxicity. Furthermore, it can be used in patients with mild, moderate, and severe liver dysfunction, making it more widely applicable to a wider range of patients. This dual characteristic of “high efficacy + safety” makes it the preferred treatment drug for clinicians.

The market performance serves as a direct testament to its clinical value. Statistics indicate that the global sales of enzalutamide surpassed $8.3 billion in 2024, marking a year-on-year increase of 35.94%, maintaining a sustained high-growth trajectory. In the domestic market, enzalutamide soft capsules were approved for marketing in 2019 and successfully included in the national medical insurance directory in 2020, significantly enhancing drug accessibility and triggering explosive sales growth. The sales revenue from all terminal hospitals exceeded 500 million yuan in 2024, and reached 370 million yuan in the first half of 2025, marking a year-on-year increase of 58.92%.

It is worth noting that the original enzalutamide is available in two dosage forms: soft capsules and tablets, which were approved for marketing by the FDA in 2012 and 2020, respectively. The enzalutamide soft capsules currently have one patent in China, “200680025545.1”, with an expiration date of March 29, 2026. The current patent protection scope is: based on the amended claims 1-6 submitted by the patentee on May 3, 2018, it remains valid. For details, please refer to the “Examination Decision on Request for Invalidation” (corresponding invalidation case number: 4W118345) issued by the China National Intellectual Property Administration on March 6, 2025. The tablet dosage form is more suitable for prostate cancer patients who need long-term medication due to its advantages such as convenient administration, precise dosage, and high patient compliance. Since December 2020, the indications approved by the National Medical Products Administration (NMPA) for enzalutamide tablets include: (1) metastatic castration-resistant prostate cancer (mCRPC), which is not dependent on chemotherapy: used directly after ADT failure (International Phase III PREVAIL regimen); (2) non-metastatic castration-resistant prostate cancer (nmCRPC), which must meet the requirement of PSA doubling time ≤10 months (PROSPER regimen); (3) metastatic hormone-sensitive prostate cancer (mHSPC) (newly expanded in September 2023), which is used in combination with ADT without considering high/low tumor burden (ARCHES Chinese population data). The “non-metastatic hormone-sensitive” indication has not been officially approved in China, but it has been included in the Grade I recommendation in the 2024 CSCO Guidelines. Previously, only soft capsule dosage forms were available for sale in the domestic market, and 10 enterprises had obtained production approvals for this dosage form, leading to a gradual homogenization of market competition. The approval of Kelun Pharmaceutical’s Enzalutamide Tablets has filled the gap in tablet dosage form, providing a better choice for clinical treatment and injecting new vitality into market competition.

In the field of generic drugs, the value of “first generic” lies not only in the market opportunity, but also in the precise replication of the efficacy and quality of the original drug. The approval of the Enzalutamide Tablets from Kelun Pharmaceutical as a Class 3 generic drug and its deemed passing of the consistency evaluation signifies that its quality and efficacy have reached the same level as the original drug, providing patients with a cost-effective treatment option. China’s approval requirements for Class 3 generic drugs are extremely strict, requiring them to meet the core standard of “consistency with the quality and efficacy of the original drug”. This “quality equivalence + efficacy consistency” advantage of the first generic holds significant clinical and social value.

For patients, the launch of generic drugs will significantly reduce medication costs. Considering the price of the original drug after medical insurance reimbursement, which is 3000-4000 yuan per box, the price of Kelun’s Enzalutamide Tablets is expected to decrease by 20%-30%. This will significantly alleviate the financial burden for prostate cancer patients who need long-term medication and improve treatment compliance.

Reference:

1. https://mp.weixin.qq.com/s/KsmR0j_FcX-AetD3UbW1Eg

2. https://www.sohu.com/a/953179390_121035734