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erlotinib + sulindac
- Development stage
- Phase 2
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Erlotinib + sulindac is a combination of two small molecule drugs used experimentally for chemoprevention in patients with familial adenomatous polyposis (FAP). Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, while sulindac is a non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase-1 and -2 (COX-1/2). Clinical trials have shown that this combination significantly reduces the number and burden of duodenal and colorectal polyps in FAP patients compared to placebo. The mechanism involves inhibition of EGFR signaling by erlotinib and suppression of prostaglandin synthesis by sulindac, which together interfere with molecular pathways driving polyp formation. This regimen has not been approved for general use but has demonstrated efficacy as an adjunct to surgical management in FAP[1][2][3][4][5].
- Other names
- erlotinib + sulindac
02
Targets
PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)EGFR (Epidermal growth factor receptor)
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