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PF-06273340
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
PF-06273340 is a potent and selective small molecule inhibitor of the tropomyosin receptor kinase (Trk) family—specifically TrkA, TrkB, and TrkC—with nanomolar inhibitory activity. It was developed by Pfizer as an orally available and peripherally restricted agent for the treatment of acute and chronic pain. The drug demonstrated efficacy in rodent models of inflammatory pain and showed anti-hyperalgesic effects in human pharmacodynamic studies. Mechanistically, it blocks nerve growth factor (NGF) signaling through inhibition of Trk receptors. Clinical development reached Phase 1 trials but was subsequently discontinued[1][4][5][6].
02
Targets
NTRK2 (Tropomyosin-related kinase receptor type B)NTRK1 (Tropomyosin-related receptor kinase A)NTRK3 (Tropomyosin receptor kinase C)PGHS-1 (Prostaglandin G/H Synthase 1)DAT (Dopamine plasma membrane transport protein)IRAK1 (Interleukin-1 receptor-associated kinase 1)FLT3 (Fms related receptor tyrosine kinase 3)MUSK (Muscle skeletal receptor tyrosine-protein kinase MuSK)
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