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Ref Type Journal Article
PMID (32824175)
Authors Huen A, Haverkos BM, Zain J, Radhakrishnan R, Lechowicz MJ, Devata S, Korman NJ, Pinter-Brown L, Oki Y, Barde PJ, Nair A, Routhu KV, Viswanadha S, Vakkalanka S, Iyer SP
Title Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma.
Journal Vol Issue Date Pages Journal Short Title
Cancers 12 8 2020 Aug 15 Cancers (Basel)
URL
Abstract Text Tenalisib (RP6530), a dual phosphoinositide 3-kinase δ/γ inhibitor was evaluated in a phase I/Ib study for maximum tolerated dose (MTD), pharmacokinetics, and efficacy in patients with relapsed/refractory peripheral and cutaneous T-Cell Lymphoma (TCL). Histologically confirmed (TCL) patients, with ≥1 prior therapy received Tenalisib orally in a 28-day cycle in doses of 200 to 800 mg twice daily (800 mg in fasting and fed state) in escalation phase (n = 19) and 800 mg twice daily (fasting) in expansion phase (n = 39). The most frequently reported treatment emergent adverse events (TEAE) and related TEAE were fatigue (45%) and transaminase elevations (33%), respectively. Most frequently reported related Grade ≥3 TEAE was transaminase elevation (21%). Two dose-limiting toxicities occurred in the 800 mg fed cohort; hence, 800 mg fasting dose was deemed MTD. Tenalisib was absorbed rapidly with a median half-life of 2.28 h. Overall response rate in 35 evaluable patients was 45.7% (3 complete response (CR); 13 partial response (PR)) and median duration of response was 4.9 months. Responding tumors showed a marked downregulation of CD30, IL-31 and IL-32α. With an acceptable safety and promising clinical activity, Tenalisib can be a potential therapeutic option for relapsed/refractory TCL. Currently, a phase I/II combination study with romidepsin is ongoing.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Tenalisib Tenalisib 0 3
Drug Name Trade Name Synonyms Drug Classes Drug Description
Tenalisib RP6530|RP-6530|RP 6530 PIK3CD inhibitor 27 PIK3CG inhibitor 10 Tenalisib (RP6530) is an inhibitor of PIK3CG and PIK3CD, which blocks PI3K/AKT signaling to prevent cell proliferation and also may modulate the tumor microenvironment and induce macrophage phenotype conversion from M2 to M1 (PMID: 30352904, PMID: 31761713, PMID: 32824175).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References