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LOXO-435 + pembrolizumab
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
LOXO-435 + pembrolizumab is an investigational combination therapy for advanced solid tumors, specifically those harboring activating fibroblast growth factor receptor 3 (FGFR3) alterations[1][2][4][5][6][7]. LOXO-435 is a highly isoform-selective small molecule inhibitor of FGFR3 designed to target both wild-type and mutant FGFR3, including gatekeeper resistance mutations, with minimal inhibition of other FGFR isoforms, aiming for reduced off-target toxicities compared to pan-FGFR inhibitors[3][6]. Pembrolizumab is a monoclonal antibody checkpoint inhibitor targeting programmed cell death protein 1 (PD-1), used in immunotherapy to enhance anti-tumor immune responses. The primary indication in trials is metastatic urothelial carcinoma and other FGFR3-altered advanced solid tumors. The combination is trialed in cohorts with and without prior FGFR inhibitor treatment, with therapeutic rationale based on targeted inhibition (LOXO-435) and immune checkpoint blockade (pembrolizumab)[1][2][4][5][6][7].
- Other names
- LOXO-435 + pembrolizumab
02
Targets
FGFR3 (Fibroblast growth factor receptor 3)PDCD1 (Programmed cell death protein 1 receptor)
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