2-fluorofucose (SGN-2FF) / Pfizer - LARVOL DELTA

Blockade of the Notch Pathway by Inhibition of Fucosylation Ameliorates Chondrocyte Inflammation and Extracellular Matrix Degradation. (PubMed, J Inflamm Res) - "In in vitro experiments, we established a cellular inflammation model on a mature human chondrocyte cell line and intervened with the inhibitor SGN-2FF...Animal experiments showed that inhibition of fucoidan glycosylation could effectively reduce the expression of IL-6 and TNF-α, reduce cartilage damage and alleviate OA. Inhibition of fucosylation can ameliorate chondrocyte inflammation and extracellular matrix degradation by decreasing Notch1 activity and down-regulating the expression of the Notch pathway, which can effectively alleviate the development of OA."

Journal • Immunology • Inflammation • Osteoarthritis • Pain • Rheumatology • IL6 • NOTCH1 • TNFA

SGN-2FF: A small-molecule inhibitor of fucosylation modulates immune cell activity in preclinical models and demonstrates pharmacodynamic activity in early phase 1 analysis (AACR 2018) - "Collectively, these data demonstrate robust biological effects of SGN-2FF. The pharmacodynamic biomarkers and PK analysis are informing next steps in identifying an optimal dose and dosing schedule for SGN-2FF."

P1 data • PK/PD data • Solid Tumor

First-In-Human, First-In-Class, Phase I Trial of the Fucosylation Inhibitor SGN-2FF in Patients with Advanced Solid Tumors. (PubMed, Oncologist) - "SGN-2FF demonstrated proof-of-mechanism and preliminary antitumor activity but was associated with thromboembolic events leading to study termination."

Clinical • Journal • P1 data • Breast Cancer • Cardiovascular • Fatigue • Head and Neck Cancer • Immune Modulation • Inflammation • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer

A Safety Study of SGN-2FF for Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=47; Terminated; Sponsor: Seattle Genetics, Inc.; Active, not recruiting ➔ Terminated; Due to overall benefit/risk profile

Clinical • PD(L)-1 Biomarker • Trial termination

A Safety Study of SGN-2FF for Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=47; Active, not recruiting; Sponsor: Seattle Genetics, Inc.; Recruiting ➔ Active, not recruiting; N=308 ➔ 47; Trial completion date: Aug 2022 ➔ Jun 2019; Trial primary completion date: Dec 2019 ➔ Jun 2019

Clinical • Enrollment change • Enrollment closed • PD(L)-1 Biomarker • Trial completion date • Trial primary completion date