Itari (linperlisib)

Here, we show that combining the PI3Kδ inhibitor linperlisib with the pan-peroxisome proliferator-activated receptor (PPAR) agonist chiglitazar, an agent that reprograms tumor metabolism, delivers robust antitumor activity across FL models, including cell-derived and patient-derived xenografts, with a favorable tolerability profile. Compared with monotherapy, the combination consistently achieves superior tumor control in vivo without overt toxicity, supporting its clinical translation potential. Collectively, these data provide a mechanistic rationale for dual targeting of PI3Kδ and PPARα in FL and advocate for clinical evaluation of this combination with FoxO1 as a pharmacodynamic biomarker.

With a median follow-up time of 13.0 months, median duration of response (DOR), progression-free survival, and overall survival (OS) were not reached. In conclusion, linperlisib plus chidamide demonstrated a favorable safety profile and encouraging preliminary efficacy in r/r PTCL.

P2, N=30, Not yet recruiting, The First Affiliated Hospital of Soochow University; The First Affiliated Hospital of Soochow University

P1/2, N=48, Not yet recruiting, Ruijin Hospital

P1/2, N=54, Not yet recruiting, Sun Yat-sen University

P=N/A, N=40, Not yet recruiting, The Affiliated Hospital of Southwest Medical University; The Affiliated Hospital of Southwest Medical University

P2, N=41, Recruiting, Institute of Hematology & Blood Diseases Hospital, China | Trial completion date: Oct 2025 --> Jan 2026 | Trial primary completion date: Jun 2025 --> Oct 2025

This all-oral combination may represent a new therapeutic option for advanced CTCL, particularly in mycosis fungoides. ClinicalTrials.gov Identifier: NCT06037239.

We present the case of an 80-year-old woman with relapsed/refractory (R/R) AITL who relapsed after CHOP and exhibited resistance to the following sequential therapies: second-line chidamide plus COP and third-line chidamide with mitoxantrone hydrochloride liposome...Salvage therapy with linperlisib, a selective PI3Kδ inhibitor, combined with gemcitabine/oxaliplatin induced sustained partial remission, followed by linperlisib maintenance...This case highlights the dual role of linperlisib as an effective and well-tolerated therapy for elderly R/R AITL patients who have exhausted prior lines. By precisely targeting PI3Kδ, our findings offer critical real-world evidence to address the unmet need for safe salvage strategies in this vulnerable population.

In a pilot trial of linperlisib (a PI3Kδ inhibitor) for refractory cases, 7 of 8 participants quickly respond with satisfactory safety. This study is registered at ClinicalTrials.gov (NCT05676710).

P1, N=12, Recruiting, Sun Yat-sen University | Not yet recruiting --> Recruiting

P2, N=33, Recruiting, The First Affiliated Hospital of Xiamen University | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2024 --> Dec 2027