Drug intelligence / Profile preview

navitoclax + erlotinib

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

Overview

**Navitoclax + erlotinib** is an investigational oral combination therapy used in early-stage clinical trials for advanced solid tumors, notably non-small cell lung cancer. The regimen pairs navitoclax (ABT-263), a potent small-molecule inhibitor of anti-apoptotic Bcl-2 family proteins (including BCL-2, BCL-X_L, and BCL-W), with erlotinib, a small-molecule inhibitor of the Epidermal growth factor receptor (EGFR) tyrosine kinase. Navitoclax promotes apoptosis in cancer cells by lowering their apoptotic threshold, while erlotinib blocks proliferation by inhibiting EGFR signaling. The combination aimed to synergistically induce cancer cell death by both suppressing growth signals and overcoming apoptotic resistance. Clinical studies found no pharmacokinetic interaction, but the combination's efficacy was limited, and notable side effects (such as diarrhea, nausea, and vomiting) were observed.

Other names
navitoclax + erlotinibABT-263 + erlotinib
02

Targets

BCL2L1 (B-cell lymphoma-extra large protein)Bcl-w (B-cell lymphoma 2-like 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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