Drug intelligence / Profile preview

tenalisib

Development stage
Phase 2
Lead developer
Rhizen Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Tenalisib is an orally active, highly selective small molecule inhibitor targeting the delta and gamma isoforms of phosphoinositide 3‑kinase (PI3Kδ/γ), as well as salt-inducible kinase 3 (SIK3). It is being developed primarily for hematological malignancies, including T-cell lymphomas and various leukemias, and has shown promising efficacy in clinical trials. Tenalisib acts by inhibiting PI3Kδ/γ signaling pathways involved in cell proliferation and survival, particularly in malignant lymphocytes. The drug is under investigation for use both as a single agent and in combination with other therapies such as romidepsin. It was originally developed by Rhizen Pharmaceuticals[2][5][7].

Other names
(S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one3-(3-fluorophenyl)-2-((1S)-1-(7H-purin-6-ylamino)propyl)chromen-4-one3-(3-fluorophenyl)-2-[ (1S ) -1-(7H-purin -6 - ylamino ) propyl ] chromen -4-oneTenalisib [INN]
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)SIK3

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