golidocitinib (DZD4205)

P2, N=30, Not yet recruiting, M.D. Anderson Cancer Center

In June 2024, golidocitinib received conditional approval in China for the treatment of adult patients with relapsed or refractory (r/r) PTCL who have received at least one line of systemic treatment. This article summarizes the milestones in the development of golidocitinib leading to this first approval for the treatment of adults with PTCL.

P2, N=18, Not yet recruiting, Ruijin Hospital

P2, N=150, Recruiting, Dizal Pharmaceuticals

P2, N=130, Active, not recruiting, Dizal Pharmaceuticals

P2, N=69, Not yet recruiting, Cancer Institute and Hospital, Chinese Academy of Medical Sciences

In this phase 2 study, golidocitinib showed a favourable benefit-risk profile in treating relapsed or refractory peripheral T-cell lymphoma. The results of this study warrant further randomised clinical studies to confirm activity and assess efficacy in this population.

In this phase I study, golidocitinib demonstrated an acceptable safety profile and encouraging antitumor efficacy in heavily pretreated patients with r/r PTCLs. These results support the initiation of the multinational pivotal study in patients with r/r PTCLs.

In conclusion, golodocitinib showed manageable safety profile and promising effect in maintaining and enhancing tumor response in patients with PTCL post first-line therapies. This result supports further clinical development of golidocitnib in the first-line setting. The updated data will be presented in the conference.

According to data from the phase III IELSG37 trial, consolidation radiotherapy is unnecessary for patients with primary mediastinal B-cell lymphoma who respond completely to standard immunochemotherapy. Two other studies of peripheral T-cell lymphomas and adult T-cell leukemia/lymphoma, respectively, point to golidocitinib, an investigational JAK1 inhibitor, and mogamulizumab, which targets CCR4, as potential new treatment options.

P2, N=160, Recruiting, Dizal Pharmaceuticals | Trial completion date: Jul 2023 --> Dec 2024 | Trial primary completion date: Jan 2023 --> Sep 2023

Do we require an autologous stem cell transplantation in all patients? Is there room for improvement in the setting of relapsed and refractory disease?

No apparent correlation between mutations in JAK/STAT pathway and clinical response was observed while baseline high pSTAT level seems to predict clinical benefit. Larger sample size is needed to confirm the findings.

The majority of TEAEs were reversible or clinically manageable with dose modifications. Conclusion Golidocitinib shows good safety and promising anti-tumor efficacy in r/r PTCL, indicating its potential as a therapeutic option for this unmet medical need.

JAK1, JAK2, JAK3, and TYK2 belong to the JAK (Janus kinase) family. Compound 21 has good preclinical pharmacokinetics. Compound 21 displayed an enhanced antitumor activity in combination with approved EGFR inhibitor, osimertinib, in a preclinical non-small cell lung cancer (NSCLC) xenograft NCI-H1975 model.

P1/2, N=10, Completed, Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Active, not recruiting --> Completed | N=120 --> 10 | Trial completion date: Jul 2022 --> Jan 2020 | Trial primary completion date: Jul 2020 --> Sep 2019

P1/2, N=120, Active, not recruiting, Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Recruiting --> Active, not recruiting