Drug intelligence / Profile preview

tenalisib + CHOP

Development stage
Preclinical
Lead developer
Rhizen Pharmaceuticals
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous, Oral (prednisone)
01

Overview

**Tenalisib + CHOP** is an experimental combination regimen for hematologic malignancies, particularly T-cell lymphomas. Tenalisib is a selective, orally available inhibitor of phosphoinositide-3-kinase delta/gamma (PI3Kδ/γ) and salt-inducible kinase 3 (SIK3), developed primarily for its antitumor and immune-modulatory activity. CHOP is a standard multi-agent chemotherapy regimen for non-Hodgkin lymphoma, consisting of cyclophosphamide, doxorubicin, vincristine, and prednisone. While tenalisib has been combined in clinical studies with agents such as romidepsin but not directly with CHOP in published data, the combination would theoretically pair targeted PI3K inhibition with classic cytotoxic agents to enhance anti-lymphoma activity. Tenalisib inhibits proliferation and survival signaling in malignant lymphocytes and can alter the tumor microenvironment, while CHOP offers broad cytotoxic effects. This combination, if studied, would be primarily indicated for aggressive lymphomas such as peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL).

02

Targets

DNATOP2A (DNA topoisomerase II)GR (Glucocorticoid receptor)MicrotubulePIK3CD (Phosphatidylinositol 3-kinase delta)SIK3TUBB (Tubulin (alpha and beta subunits))PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)

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