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navitoclax + erlotinib
- Development stage
- Phase 1
- 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
Bcl-w (B-cell lymphoma 2-like 2)BCL2L1 (B-cell lymphoma-extra large protein)EGFR (Epidermal growth factor receptor)BCL2L2 (BCL-2-like protein 2)
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