Idelalisib · Zydelig, TRU-016

What is Idelalisib?

Idelalisib is an orally bioavailable small molecule inhibitor of the delta isoform of class I phosphoinositide 3-kinase (PI3Kδ), which is expressed mainly in hematopoietic cells. It blocks production of PIP3, reducing B-cell receptor signaling, cell trafficking, proliferation and survival. It is studied in chronic lymphocytic leukemia and in several follicular and T-cell lymphomas.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Zydelig, TRU-016, GS-1101

Drug type

Small molecule

Targets

phosphatidylinositol 3-kinase delta (PI3Kδ) (PIK3CD)

Mechanism

Inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ) (PIK3CD)

Pathways

B-cell receptor signaling, CXCR4 and CXCR5 signaling, chemotaxis and adhesion, apoptosis

Therapy area

Oncology

Developer

Gilead Sciences Inc

In trials of

ADCT, APVO

FDA status

Approved as Zydelig (July 23, 2014), NDA205858 · FDA label

UNII

YG57I8T5M0

✅ FDA-approved uses

• Chronic lymphocytic leukemia (CLL), relapsed, in combination with rituximab

From the indications section of the FDA label (version of Feb 20, 2025). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Chronic Lymphocytic LeukemiaPeripheral T-cell LymphomaRefractory Follicular LymphomaRelapsed Follicular Lymphoma

Sources

• FDA label (DailyMed)
• FDA label Zydelig (2025-02-20), indications
• NCI Thesaurus
• ClinicalTrials.gov NCT01644253
• ClinicalTrials.gov NCT01644253
• ClinicalTrials.gov NCT01644253
• ClinicalTrials.gov NCT01644253

Updated Oct 11, 2026.