Recently, Hengrui Pharmaceuticals' subsidiary Chengdu Shengdi Pharmaceutical Co., Ltd. has received the Certificate of Drug Registration approved by the State Drug Administration, which authorizes the company's self-developed Abiraterone Acetate Tablets (II) (Trademark: Eragon®) to be listed on the market. This is the first Abiraterone Acetate nanocrystalline preparation approved for marketing in China, and also the second new chemical drug of Class 2 approved for marketing by Hengrui Pharmaceuticals. Abiraterone Acetate Tablets (II) innovatively introduces nanocrystal technology, which can significantly improve drug bioavailability and reduce the degree of food influence, thus improving patients' drug adherence, and will bring new and better therapeutic choices for metastatic prostate cancer patients in China.

Prostate cancer is the most common malignant tumor of the urinary male reproductive system. In China, the incidence rate and mortality rate of prostate cancer account for the sixth and tenth of male malignant tumors, respectively. The 5-year survival rate of Chinese prostate cancer patients is 69.2%, which is much lower than the 97.4% in the United States.

Abiraterone acetate, as a CYP17 enzyme inhibitor, can be converted into androgen biosynthesis inhibitor abiraterone in vivo, blocking androgen synthesis in testes, adrenal glands and prostate gland, thus inhibiting the progression of prostate cancer. Currently, abiraterone acetate + prednisone has become an important therapeutic agent for metastatic prostate cancer, and the consensus of international and domestic guidelines unanimously recommend it as the first-line treatment option for metastatic prostate cancer. However, ordinary abiraterone acetate is characterized by low solubility and low permeability, low bioavailability, large intra-individual variability, and 4 tablets per dose, which can only be taken 1h before or 2h after meals, affecting patient compliance and not applicable to the target indication population of middle-aged and elderly people.

In the face of the above problems, Abiraterone Acetate Tablets (II) takes an innovative step: adopting nanocrystal technology to efficiently improve the solubility and dissolution rate of difficult-to-soluble drugs; adding a new type of excipient, sodium 8-(2-hydroxybenzamido)octanoate (SNAC), which enhances the gastrointestinal permeation and absorption of drugs and further improves oral bioavailability, with the dosage being reduced to 1/3 that of ordinary Abiraterone Acetate Tablets; Significantly improve the effect of food influence, oral intake can not be subject to dietary restrictions; smaller tablet size and at the same time the use of scored design, more suitable for liver insufficiency and other special groups of patients who need to take half a tablet.

The approval of abiraterone acetate tablets (II) is based on the results of its Phase I clinical study and Phase II clinical study (ABTL-PD-01). Its Phase I clinical study supported the improved pharmacokinetic behavior resulting from the technology modification, confirming that the exposure level of abiraterone acetate tablets (II) 300 mg is comparable to that of regular abiraterone acetate tablets 1,000 mg and that the former is not subject to dietary restrictions.The results of the ABTL-PD-01 study showed that abiraterone acetate tablets (II), with the modification of the prescription process, can achieve the same level of exposure as the generic abiraterone acetate tablets with the lower oral dosage of 300 mg once daily. The results of the ABTL-PD-01 study indicate that abiraterone acetate tablets (II), modified by the prescription process, at a lower oral dose of 300 mg, once daily, can achieve comparable efficacy and efficacy to that of regular abiraterone acetate tablets 1,000 mg, with a trend toward improved overall safety.

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