SUN13837 / Daiichi Sankyo - LARVOL DELTA

Discovery of 1,2,3-triazole-based fibroblast growth factor receptor modulators. (PubMed, Bioorg Med Chem Lett) - "To avoid production of a phospholipidosis-inducing metabolite, we replaced the amide structure of SUN13837 (1) with a 1,2,3-triazole...In addition, installation of a methyl group at the 5-position of 1,2,3-triazole of 10 significantly boosted the neuroprotective activity. These 1,2,3-triazole derivatives displayed reduced phospholipidosis risk, sufficient systemic exposure, and high central nervous system penetration, and therefore may be potentially useful agents for the treatment of neurodegenerative diseases."

Journal • CNS Disorders

Systemic treatment with a novel basic fibroblast growth factor mimic small-molecule compound boosts functional recovery after spinal cord injury. (PubMed, PLoS One) - "What is more remarkable is that SUN13837 is eliminated the bioactivity to induce cell proliferation of non-neuronal somatic cells. On the bases of studies of pharmacology, behavior, physiology and histology, the present study reports that SUN13837 is characterized as a promising synthetic compound for treatment of devastating damages onto the rat spinal cord."

Journal • CNS Disorders • Complement-mediated Rare Disorders • Orthopedics

Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential. (PubMed, Bioorg Med Chem) - "SUN13837 (1), a fibroblast growth factor receptor modulator, has been an attractive candidate for treating neurodegenerative diseases...Further structural modifications to reduce hydrogen bond donors afforded 17 with improved brain exposure. Oral administration of 17 at 1 mg/kg once daily for 10 days showed enhanced recovery of coordinated movement in a rat acute stroke model, suggesting that it is a promising follow-up compound for 1 with reduced risk of phospholipidosis."

Journal • Cardiovascular • CNS Disorders • FGF • FGFR