Drug intelligence / Profile preview

lapatinib + everolimus

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Lapatinib + everolimus is a combination of two oral small molecule drugs used in oncology research, particularly for advanced solid tumors. Lapatinib is a dual tyrosine kinase inhibitor targeting the intracellular domains of epidermal growth factor receptor (HER1/EGFR/ERBB1) and human epidermal growth factor receptor type 2 (HER2/ERBB2), thereby inhibiting tumor cell proliferation driven by these receptors. Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR), a key regulator in cell growth, proliferation, and survival pathways. Preclinical studies suggest that mTOR inhibition can enhance the efficacy of HER inhibitors like lapatinib. The combination has been evaluated in phase I clinical trials for safety, pharmacokinetics, and preliminary antitumor activity in patients with various advanced cancers including breast cancer and thymic cancer[1][2][3][6]. The maximum tolerated dose was established as 1250 mg lapatinib plus 5 mg everolimus daily[1][2][3].

Other names
lapatinib + everolimus
02

Targets

EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)Mechanistic target of rapamycin complex 1

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