Drug intelligence / Profile preview

erlotinib + AT-101

Development stage
Preclinical
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib is a small molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR). It blocks the kinase activity of EGFR, which is involved in cell growth and survival, thereby inhibiting cancer cell proliferation. Erlotinib is primarily used for the treatment of non-small cell lung cancer (NSCLC) with specific EGFR mutations and for advanced pancreatic cancer in combination with gemcitabine[1][3][7]. AT-101 (also known as R-(–)-gossypol acetic acid) is an orally active small molecule Bcl-2 family protein inhibitor that promotes apoptosis in tumor cells. The combination of erlotinib and AT-101 has been investigated in clinical trials for synergistic anti-tumor effects, particularly in NSCLC.

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)BCL2L1 (B-cell lymphoma-extra large protein)MCL1 (Myeloid cell leukemia sequence 1)

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