Cancers, Vol. 12, Pages 2293: Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma

Cancers, Vol. 12, Pages 2293: Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma Cancers doi: 10.3390/cancers12082293 Authors: Auris Huen Bradley M. Haverkos Jasmine Zain Ramchandren Radhakrishnan Mary Jo Lechowicz Sumana Devata Neil J. Korman Lauren Pinter-Brown Yasuhiro Oki Prajak J. Barde Ajit Nair Kasi Viswanath Routhu Srikant Viswanadha Swaroop Vakkalanka Swaminathan P. Iyer 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 e...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Article Source Type: research