dizhe pharmaceutical (stock code: 688192.SH) announced that the research results of the world's first highly selective JAK1 inhibitor golixitinib phase I clinical trial (part a of the JACKPOT8) in the field of T cell lymphoma (PTCL) independently developed by the company were published in the top international journal Annals of Oncology (Annals of Oncology), with a impact factor of 51.8 from 2022 to 2023. The journal is the official authoritative journal of the European Society of Oncology (ESMO). It is one of the most influential journals in the field of oncology, and its influence ranks among the top five in the world. this time, it is a rare clinical research article with the highest impact factor published by Chinese scholars in the field of lymphoma as corresponding authors and first authors in the past 5 years.

The results of the JACKPOT8 Part A study showed that golixetinib showed favorable safety, pharmacokinetic properties and encouraging anti-tumor efficacy in patients with relapsed or refractory T-cell lymphoma (r/r PTCL) who had previously received multiple lines of therapy.

golicitinib, as a national innovative drug with source innovation, has won many international awards since entering phase I international multi-center clinic. consecutive 4 won 5 oral reports of top international academic conferences , in which the phase I clinical research results were presented at the 2020 ASH, 2021 ICML and 2022 EHA conferences respectively; the 2023 Global Key Clinical Trial (Part B of the JACKPOT8) results were once again presented in an oral presentation to ASCO and ICML.

the latest research results of part B of the JACKPOT8 show that the objective response rate (ORR) of golicetinib monotherapy for relapsed or refractory T cell lymphoma (r/r PTCL) is 44.3 , and the complete response rate (CR) is 23.9 , which is much higher than the existing treatment scheme and is expected to break through the current bottleneck of r/r PTCL treatment, open a new era of targeted therapy for PTCL.

with the excellent clinical data of "4 years and 5 consecutive championships" widely recognized by the international academic community, golicetinib has also been continuously recognized by overseas regulatory agencies, and was recognized by us food and drug administration (FDA) "fast track recognition" in February 2022.

Golicitinib continues to shine on the international stage. This is a typical representative of Chinese biomedical companies that are proud to independently develop innovative drugs from the source to the world.

Differentiated clinical value-oriented innovation

PTCL is a highly heterogeneous and aggressive non-Hodgkin's lymphoma (NHL), accounting for about 7% - 10% of NHL worldwide. The incidence of PTCL in China is significantly higher than that in Europe and the United States, accounting for about 25% of NHL. According to Frost & Sullivan's analysis, there will be about 22600 new cases in China in 2019 and it is expected to increase to 29000 in 2030. PTCL has the characteristics of multiple subtypes, easy recurrence and poor prognosis. The prognosis of r/r PTCL after initial treatment failure is extremely poor, and the annual overall survival rate of 3 is only 21%-28%, There is still a lack of effective treatment in clinical practice.

At present, the first-line treatment of PTCL is still based on anthracycline-based CHOP or CHOP-like chemotherapy, but patients with remission after first-line treatment still have a very high risk of recurrence. The prognosis of relapsed and refractory cases that relapse after first-line treatment or do not relapse after treatment is extremely poor, and there is no routinely approved standard treatment at home and abroad for many years, suggesting that there are great challenges in the treatment of this disease. The efficacy of traditional salvage chemotherapy for r/r PTCL is significantly poor, with a median overall survival of only a few months. Although new methods such as targeted drugs and immunotherapy for r/r PTCL have emerged in recent years, the objective response rate is still unsatisfactory, less than 30%. Therefore, for r/r PTCL patients, there is an urgent need for more effective treatment.

The JAK/STAT signaling pathway plays an important role in the development of a variety of hematological malignancies, including T-cell lymphoma. Golixitinib is one of the important research results of Dizhe Translational Science, and the company was the first to discover and validate that targeting the JAK1/STAT pathway is a high-potential treatment for PTCL. As a new generation, potent and highly selective JAK1 inhibitor, golicitinib can effectively inhibit the growth and proliferation of tumor cells by targeting the JAK/STAT pathway. To date, golicitinib is the world's first and only highly selective JAK1 inhibitor in critical clinical trials in the PTCL field.

both efficacy and safety are excellent, which is expected to break the situation r/r PTCL

Data from the international multicenter pivotal study (Part B of the JACKPOT8) showed that the efficacy of golisetinib in the treatment of r/r PTCL at RP2D dose (150 mg) broke the ceiling of previous therapies, showing significant and lasting anti-tumor efficacy, as well as good safety and tolerability.

Primary study endpoint: ORR assessed by the Independent Imaging Review Committee (IRC) was 44.3%,CR rate was 23.9%, tumor remission was observed in a variety of common subtypes of PTCL. At present, the median duration of remission (DoR) has not been reached, the longest DoR is 16.8 months , and the patient is still in remission.

Golicetinib, as a new generation of highly selective inhibitor of JAK1, has 200 - 400 times selectivity to other members of JAK family. It belongs to a new generation of JAK inhibitor that needs to be developed in clinic at present, and effectively reduces the drug safety risk caused by off-target. Treatment-related adverse events (TRAEs) were mostly recoverable or clinically manageable and well tolerated in the JACKPOT8 Part B study, with a median relative dose strength of 100%, validating the safety advantage of golicitinib as a highly selective JAK1 inhibitor.

The remarkable efficacy and safety of golicitinib have been unanimously recognized by experts at home and abroad, and it is expected to become a "world-class national innovative drug", bringing new hope to the treatment field of PTCL. International multi-center key studies (Part B of the JACKPOT8) have been carried out in China, the United States, South Korea, Australia and other countries. Dizhe Pharmaceuticals will continue to explore new clinical research directions to further verify the clinical efficacy and safety of golixitinib, and to carry out combination treatment programs and explore in more populations.

About Golicetinib

Golicetinib is the world's first and so far the only highly selective JAK1 inhibitor in the field of T-cell lymphoma in the global registration clinical stage. The first indication is relapsed/refractory peripheral T-cell lymphoma (r/r PTCL), and key clinical trials are being carried out in China, the United States, South Korea, Australia and other countries. As of February 16, 2023, in the international multi-center key clinical study (Part B of JACKPOT8), golicitinib single drug showed strong and lasting anti-tumor activity, with an objective response rate (ORR) of 44.3, and more than half of the subjects with tumor remission achieved complete remission (CR), with a CR rate of 23.9. Golicotinib is used to treat r/r PTCL and was recognized by the US Food and Drug Administration (FDA) as "Fast Track Designation" in February 2022.

About Dizhe Medicine

Dizhe Pharmaceuticals (stock code: 688192.SH) is an innovative biomedical company focused on the research, development and commercialization of innovative therapies in the field of malignant tumors and immune diseases. The company adheres to the research and development concept of source innovation, with the goal of introducing the world's first drug (First-in-class) and treatment methods with breakthrough potential, aiming to fill the world's unmet clinical needs. Based on the industry-leading translational science and new drug molecular design and screening technology platform, the company has established five globally competitive product pipelines, two leading products in the global key clinical trials stage, one of which has been approved for listing.