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FPFT-2216
- Development stage
- Preclinical
- Lead developer
- Tenova Pharma
- Modality
- Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
- Administration
- Oral, Intraperitoneal (preclinical)
01
Overview
**FPFT-2216** is a novel small molecule "molecular glue" compound that induces proteasomal degradation of casein kinase 1α (CK1α), IKAROS family zinc finger proteins IKZF1 and IKZF3, and phosphodiesterase 6D (PDE6D)[1][3][5][6][7][8]. The drug's mechanism involves recruiting these proteins to cereblon, a substrate receptor of the CRL4^CRBN^ E3 ubiquitin ligase, promoting their ubiquitination and subsequent degradation[6][8]. FPFT-2216 activates the p53 tumor suppressor pathway and inhibits the activity of the CARD11/BCL10/MALT1 (CBM) complex and downstream NFκB signaling, resulting in inhibition of lymphoma cell proliferation and strong antitumor activity[1][2]. It has shown efficacy in models of lymphoma, including diffuse large B-cell lymphoma, and synergizes with both MDM2 inhibitors and rituximab[1][2]. FPFT-2216 also demonstrates immunomodulatory activity via upregulation of IL-2 production[4].
- Brand names
- FPFT-2216FPFT2216FPFT 2216
- Other names
- FPFT-2216FPFT2216FPFT 2216
02
Targets
CK1α (Casein kinase I alpha)IKZF1 (Ikaros family zinc finger protein 1)PDE6D (Phosphodiesterase 6-delta)IKZF3 (Zinc finger protein Aiolos)CARD11 (CARD11-BCL10-MALT1 complex)
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