Drug intelligence / Profile preview

dactolisib + paclitaxel

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

Overview

Dactolisib (NVP-BEZ235) is a synthetic small molecule of the imidazoquinoline class that acts as a dual inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR). It inhibits the catalytic subunit p110α of PI3K by competing at its ATP binding site and also inhibits mTOR activity. Paclitaxel is a microtubule-stabilizing cytotoxic agent that causes mitotic arrest leading to cell death. The combination has been investigated in preclinical and clinical studies for enhanced antitumor efficacy in various solid tumors, including breast cancer and gastric cancer. Dactolisib may sensitize tumors to paclitaxel by inhibiting PI3K/mTOR pathway activation associated with taxane resistance[1][2][5][6].

Other names
BEZ235 + paclitaxel
02

Targets

mTOR (Mammalian target of rapamycin kinase)PIK3CA (Phosphoinositide 3-kinase alpha)TUBB (Tubulin (alpha and beta subunits))

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