Drug intelligence / Profile preview

everolimus + paclitaxel + trastuzumab

Development stage
Unknown
Lead developer
Novartis
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

This is a combination regimen of three drugs—everolimus, paclitaxel, and trastuzumab—used primarily in the treatment of HER2-positive advanced or metastatic breast cancer. Everolimus is an oral small molecule inhibitor of the mammalian target of rapamycin (mTOR), which disrupts cell growth, proliferation, and survival pathways often upregulated in cancer. Paclitaxel is a microtubule-stabilizing chemotherapeutic agent that inhibits cell division by promoting tubulin polymerization and preventing microtubule disassembly. Trastuzumab is a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2), blocking downstream signaling that drives tumor growth in HER2-overexpressing cancers. This triple combination has been studied extensively in clinical trials such as BOLERO-1 for patients with HER2-positive breast cancer who are resistant to trastuzumab or pretreated with taxanes[1][6][3]. The regimen aims to overcome resistance mechanisms by simultaneously inhibiting mTOR signaling (everolimus), disrupting mitosis (paclitaxel), and blocking HER2-driven proliferation (trastuzumab).

Brand names
Afinitor + Herceptin + Taxol
Other names
everolimus + trastuzumab + paclitaxel
02

Targets

Mechanistic target of rapamycin kinase (mTOR) FKBP12-rapamycin binding (FRB) domainTUBB (Tubulin (alpha and beta subunits))

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