Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours.

ABSTRACT:

Background

Sapanisertib (TAK-228) is an investigational, orally available, potent and highly selective mTORC1/2 inhibitor demonstrating promise in numerous malignancies. This phase I study (NCT02412722) evaluated the safety, tolerability, pharmacokinetics and antitumour activity of single-agent TAK-228 (milled capsules), administered daily (QD) or weekly (QW) and in combination with paclitaxel in patients with advanced solid tumours. Pharmacokinetic comparisons of milled versus unmilled TAK-228 and the impact of food were also investigated.

Methods

Patients were enrolled to receive: TAK-228 QD, TAK-228 3 days/week plus paclitaxel 80 mg/m² days 1, 8, 15 (TAK-228+P) or TAK-228 QW (all 28-day cycles); starting TAK‑228 doses were 4, 6 and 20 mg, respectively.

Resul

SUBMITTER: Moore KN 

PROVIDER: S-EPMC5812400 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature