Drug intelligence / Profile preview

golidocitinib + PD-1 inhibitor + gemcitabine + pegaspargase

Development stage
Unknown
Lead developer
Dizal Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules, Recombinant Proteins and Enzymes
Administration
Intravenous, Oral, Intramuscular
01

Overview

This combination regimen consists of the highly selective oral JAK1 inhibitor golidocitinib (Gao Ruizhe), an anti-PD-1 monoclonal antibody, and the chemotherapy agents gemcitabine and pegaspargase. It is primarily being investigated as a first-line treatment for advanced or high-risk extranodal natural killer/T-cell lymphoma (ENKTL). Golidocitinib selectively blocks the JAK/STAT pathway, which is frequently mutated or aberrantly activated in T-cell and NK-cell malignancies, thereby suppressing tumor cell proliferation and survival. The addition of a PD-1 inhibitor aims to reverse tumor-mediated immunosuppression by blocking the PD-1/PD-L1 checkpoint axis. Gemcitabine acts as an antimetabolite that incorporates into DNA to cause chain termination and inhibits ribonucleotide reductase, while pegaspargase depletes circulating L-asparagine to selectively starve lymphoma cells that lack asparagine synthetase. Together, this multi-targeted immunochemotherapy regimen leverages synergistic mechanisms of direct cytotoxicity, metabolic starvation, targeted pathway inhibition, and immune checkpoint blockade to improve outcomes in aggressive ENKTL.

Other names
golidocitinib + PD-1 blockade + gemcitabine + pegaspargasegolidocitinib + PD-1 inhibitor + gemcitabine + pegaspargase戈利昔替尼 + PD-1 抑制剂 + 吉西他滨 + 培门冬酶戈利昔替尼 + PD-1 阻断剂 + 吉西他滨 + 培门冬酶高瑞哲 + PD-1 抑制剂 + 吉西他滨 + 培门冬酶高瑞哲 + PD-1 阻断剂 + 吉西他滨 + 培门冬酶
02

Targets

DNAJAK1 (Janus kinase 1)PDCD1 (Programmed cell death protein 1 receptor)RRM1

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