GP(HK) Global Innovative RDC TLX250-CDX Dosed the First Patient with the Expanding Indication in Australia, and the Self-developed “Tadalafil Tablets” is Granted a Drug Registration Certificate, Continuously Improving Research Strength and Enriching Its Product Pipelines

GP(HK) Global Innovative RDC TLX250-CDX Dosed the First Patient with the Expanding Indication in Australia, and the Self-developed “Tadalafil Tablets” is Granted a Drug Registration Certificate, Continuously Improving Research Strength and Enriching Its Product Pipelines

(July 7, 2021 - Hong Kong) China Grand Pharmaceutical and Healthcare Holdings Limited (“GP (HK)” or the “Company”, together with its subsidiaries, the “Group”, stock code: 00512) is pleased to announce that Telix Pharmaceuticals Limited (ASX: TLX) (“Telix”), the Group’s partner in the field of radionuclide-drug conjugates (“RDC”), has successfully dosed the first patient in Phase I clinical study of TLX250-CDx (89Zr-DFO-girentuximab) (“TLX250-CDx”), a global innovative RDC for the treatment of clear cell renal cell carcinoma (“ccRCC”), on its expanding indication, urothelial carcinoma or bladder cancer, in Australia. According to the licensing agreement between the Group and Telix, the expanding indications for the product are also within the licensed scope that the Group has been granted. Moreover, the Group's self-developed product “Tadalafil Tablets” has been granted a drug registration certificate by the National Medical Products Administration of the People's Republic of China.

The Group always puts focus on the R&D of innovative products and advanced technologies. Sticking to patients-centered and innovation-driven, the Group will continue to increase its investment in the world-class innovative products and advanced technologies to meet unmet clinical needs and enrich product pipeline and improve supply chain. The Group adopts the strategy of “global expansion and dual-cycle operation”, forming a new pattern of domestic and international cycles that synergize with each other. In this way, the Group can make full use of its industrial advantages and R&D capabilities, to accelerate commercialization process for innovative products and provide patients with more advanced and diverse treatment options in the world.

TLX250-CDx is a global innovative diagnosis RDC drug based on radionuclide-antibody conjugated technology, which targeting on Carbonic anhydrase IX (“CA9”). CA9 is over-expressed in urologic malignancies. 89Zr is a positron nuclide with half-life about 78.4 hours and average positron energy 0.389MeV. 89Zr’s physical half-life is matched with the biological half-life of monoclonal antibody and its fragment, thereby is the ideal nuclide for positron emission computed tomography (“PET”) imaging. TLX250-CDx is suitable for the diagnosis of urologic malignancies. Given its possible breakthrough in the diagnosis and staging of the most common and most aggressive form of kidney cancer, ccRCC, TLX250-CDx has been granted Breakthrough Therapy designation by the United States Food and Drug Administration (FDA) in July 2020. Currently, the Phase III clinical study for the diagnosis of ccRCC is progressing smoothly.

The clinical study of TLX250-CDx on the diagnosis of urothelial carcinoma or bladder cancer in Australia, is led by Professor Dickon Hayne at the Fiona Stanley Hospital in Perth, Australia. It will evaluate the feasibility of using TLX250-CDx and PET/CT to image CA9 for urothelial carcinoma or bladder cancer diagnosis and staging in 20 patients, and further explore CA9 as a therapeutic target for this type of patient. It is the first study that applies 89Zr to evaluate CA9’s degree of expression in cancers other than renal cancer, thus also lays the foundation for the expansion of clinical application of TLX250-CDx.

According to the latest global cancer burden data 2020 released by World Health Organization International Agency for Research on Cancer (IARC), bladder cancer was the tenth most common cancer types. In 2020, there were more than 570,000 new cases of bladder cancer worldwide, and more than 210,000 deaths. Among which, China has about 86,000 cases and 39,000 deaths, and the mortality rate exceeds the world average. At present, cystoscopy is the gold standard for clinical diagnosis of bladder cancer. But it is mainly suitable for the non-muscular invasive bladder cancer, not for carcinoma in situ, muscle invasive bladder cancer, and atypical hyperplastic lesions. Therefore, accurate and early diagnosis of bladder cancer is still a major clinical need. Nuclide-based molecular imaging technology combines imaging and molecular biology. Using targeted contrast agent as probe to non-invasively display the changes of the lesion part at the molecular level, it can detect early lesions and achieve continuous observation of the therapeutic effect, which will become a solid supplement to the existing clinical diagnostic methods.

Tadalafil is used to treat the erectile dysfunction, which is a selective and reversible type 5 phosphodiesterase (PDE5) inhibitor. Compared with sildenafil and vardenafil which have half-lives of less than 4 hours, Tadalafil has a half-life of 17.5 hours and an effective blood concentration of 36 hours, Tadalafil is more suitable for regular use in small doses and is well tolerated. According to the data of Menet, the market size of Tadalafil in 2020 is RMB 870 million, with a five-year CAGR of approximately 5.5%. The market share of the original drug takes up approximately 89%, and the potential of substitution of domestic products is great.

Erectile dysfunction (“ED”) is an inability of men to continuously obtain and maintain sufficient penile erections, which is not only one of the most common sexual dysfunction in men, but also be an early symptom and danger signal of cardiovascular disease. According to the “The Men's Attitudes to Life Events and Sexual Behaviour Study”, the total prevalence of various levels of ED among people between the ages of 20 and 75 is 16%, and with age and the incidence of ED is increasing gradually.

The Board of China Grand Pharmaceutical and Healthcare Holdings Limited, commented, “The dosing of TLX250-CDx in the first patient on the diagnosis of urothelial carcinoma or bladder cancer in phase I clinical study implies an important progress of radionuclide-drug conjugates. While enriching the cancer types that the Group’s oncology products have covered, it also continuously expands to the unmet clinical needs. And the self-developed ‘Tadalafil Tablets’ that obtained the drug registration certificate recognizes the company's R&D strength again, further reinforces the Group's product pipeline, and helps to expand out-of-hospital market. Looking ahead, the Group will continue to adopt the strategy of ‘global expansion and dual-cycle operation’, increase investment and development in the world-class innovative products and advanced technologies, to provide patients with more advanced and diverse treatment options in the world, as well as creating greater returns for shareholders.”