Drug intelligence / Profile preview

sapanisertib + serabelisib + paclitaxel

Development stage
Phase 2
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy of three drugs—**sapanisertib**, an oral dual mTORC1/2 (mTOR Complex 1 and 2) inhibitor; **serabelisib**, an oral selective PI3K-alpha inhibitor; and **paclitaxel**, a cytotoxic taxane chemotherapy agent. The regimen is designed to achieve more complete inhibition of the PI3K/mTOR/AKT pathway by simultaneously targeting multiple key nodes. This pathway is commonly mutated in cancers and mediates both tumor growth and resistance to therapy. Preclinical and early clinical studies support that the triple combination can sensitize tumor cells to paclitaxel and overcome taxane resistance, with promising response rates and safety profile in advanced solid tumors, particularly endometrial, breast, and ovarian cancers harboring PI3K pathway aberrations[1][3][7]. The combination, sometimes referred to as "PIKTOR plus paclitaxel," is under investigation for advanced, refractory solid tumors.

Other names
PIKTOR + paclitaxel
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)TUBB (Tubulin (alpha and beta subunits))Mechanistic target of rapamycin complex 1Mechanistic target of rapamycin kinase complex 2

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