FP-1039

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Ligands
FP-1039

GtoPdb Ligand ID: 11581

Synonyms: FGFR1:Fc | FP1039 | GSK-3052230 | GSK3052230 | HGS1036

Compound class: Peptide or derivative

Comment: FP-1039 (GSK3052230) is a fusion protein that comprises the extracellular domain of FGF receptor 1c (FGFR1c; to act as a trap for FGF ligands) fused with the Fc region of IgG1. The full peptide sequence is not disclosed in the primary citation [1]. FP-1039 is an oncology lead candidate [1,3].

References
1. Harding TC, Long L, Palencia S, Zhang H, Sadra A, Hestir K, Patil N, Levin A, Hsu AW, Charych D et al.. (2013) Blockade of nonhormonal fibroblast growth factors by FP-1039 inhibits growth of multiple types of cancer. Sci Transl Med, 5 (178): 178ra39. [PMID:23536011]
2. Tolcher A, Flaherty K, Shapiro GI, Berlin J, Witzig T, Habermann T, Bullock A, Rock E, Elekes A, Lin C et al.. (2018) A First-in-Human Phase I Study of OPB-111077, a Small-Molecule STAT3 and Oxidative Phosphorylation Inhibitor, in Patients with Advanced Cancers. Oncologist, 23 (6): 658-e72. [PMID:29511132]
3. Tolcher AW, Papadopoulos KP, Patnaik A, Wilson K, Thayer S, Zanghi J, Gemo AT, Kavanaugh WM, Keer HN, LoRusso PM. (2016) A phase I, first in human study of FP-1039 (GSK3052230), a novel FGF ligand trap, in patients with advanced solid tumors. Ann Oncol, 27 (3): 526-32. [PMID:26646757]

References

1. Harding TC, Long L, Palencia S, Zhang H, Sadra A, Hestir K, Patil N, Levin A, Hsu AW, Charych D et al.. (2013)
Blockade of nonhormonal fibroblast growth factors by FP-1039 inhibits growth of multiple types of cancer.
Sci Transl Med, 5 (178): 178ra39. [PMID:23536011]

2. Tolcher A, Flaherty K, Shapiro GI, Berlin J, Witzig T, Habermann T, Bullock A, Rock E, Elekes A, Lin C et al.. (2018)
A First-in-Human Phase I Study of OPB-111077, a Small-Molecule STAT3 and Oxidative Phosphorylation Inhibitor, in Patients with Advanced Cancers.
Oncologist, 23 (6): 658-e72. [PMID:29511132]

3. Tolcher AW, Papadopoulos KP, Patnaik A, Wilson K, Thayer S, Zanghi J, Gemo AT, Kavanaugh WM, Keer HN, LoRusso PM. (2016)
A phase I, first in human study of FP-1039 (GSK3052230), a novel FGF ligand trap, in patients with advanced solid tumors.
Ann Oncol, 27 (3): 526-32. [PMID:26646757]