Drug intelligence / Profile preview

everolimus + nab-paclitaxel

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

Overview

A combination therapy consisting of everolimus, an mTOR inhibitor, and nab-paclitaxel, an albumin-bound formulation of paclitaxel. Everolimus inhibits mTOR by binding to FKBP-12, forming a complex that reduces downstream effector activity, blocking cell progression from G1 to S phase and inducing cell growth arrest and apoptosis. It also inhibits hypoxia-inducible factor expression, decreasing vascular endothelial growth factor expression, which reduces cell proliferation, angiogenesis, and glucose uptake. Nab-paclitaxel is an antimicrotubule agent that promotes microtubule assembly from tubulin dimers and stabilizes microtubules to prevent depolymerization. The nab-drug delivery system utilizes albumin properties to improve drug uptake into tumor cells. This combination has shown synergistic effects in preclinical models, particularly in breast cancer cell lines at an optimal molar ratio of 1:0.5 (paclitaxel:everolimus). Clinical investigations have assessed its safety and pharmacokinetic interactions in patients with advanced malignancies.

02

Targets

TUBB (Tubulin (alpha and beta subunits))Mechanistic target of rapamycin complex 1

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