Drug intelligence / Profile preview

vorinostat + lapatinib

Development stage
Unknown
Lead developer
University of Maryland, Baltimore
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy consists of vorinostat, a pan-histone deacetylase (HDAC) inhibitor, and lapatinib, a dual tyrosine kinase inhibitor targeting EGFR (HER1) and HER2. Developed in this specific context by the University of Maryland, Baltimore, the regimen was evaluated in a Phase I/II clinical trial (GCC 0845) for patients with advanced solid tumors and HER2-positive metastatic breast cancer. Vorinostat works by inducing cell cycle arrest and apoptosis through chromatin remodeling, while lapatinib inhibits the intracellular kinase domains of HER1 and HER2, blocking downstream signaling pathways. Preclinical evidence suggested that the combination synergistically targets cancer stem cells and reduces metastasis more effectively than monotherapy.

Brand names
ZolinzaTykerbTyverb
Other names
suberoylanilide hydroxamic acidSAHAlapatinib ditosylate
02

Targets

HDAC (HDAC family)EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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