Drug intelligence / Profile preview

lapatinib + temozolomide

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Lapatinib + temozolomide is a combination therapy investigated primarily for the treatment of recurrent ependymoma and other brain tumors. Lapatinib is an oral small molecule tyrosine kinase inhibitor that targets ErbB1 (epidermal growth factor receptor, EGFR) and ErbB2 (human epidermal growth factor receptor 2, HER2), both of which are often overexpressed in certain brain tumors such as ependymoma. Temozolomide is an oral alkylating agent that acts by methylating DNA at the guanine base, leading to DNA damage and apoptosis in tumor cells. The combination has shown clinical activity with objective responses and prolonged disease control in adult patients with recurrent ependymoma[1][3][5]. Both drugs are orally administered small molecules; lapatinib was developed by GSK for breast cancer while temozolomide was developed at Aston University for gliomas.

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)

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