E6130 / Eisai - LARVOL DELTA

CX3CR1 modulation can attenuate fractalkine-induced pro-tumourigenic effects in oesophageal adenocarcinoma (EACR-AACR 2024) - "In addition, the data presented here demonstrate the utility of E6130 in the radioresistant OAC tumour cell line OE33R. Future in vitro and in vivo studies will further elucidate the role of fractalkine in OAC tumour growth and metastasis and confirm the therapeutic utility of CX3CR1 modulation in this hard-to-treat cancer"

Esophageal Adenocarcinoma • Esophageal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • CX3CL1 • CX3CR1

CX3CR1 antagonism holds therapeutic utility to reverse the pro-tumourigenic effects of fractalkine in oesophageal adenocarcinoma (EACR 2023) - "In addition, we examined if CX3CR1 antagonism could block these effects in OAC.Material and MethodsTo determine the pro-tumourigenic effects of fractalkine and the anti-tumourigenic efficacy of CX3CR1 antagonism in OAC, the OE33 cell line and the metastatic OAC cell lines FLO-1 and FLO-1LM cell lines were pre-treated with CX3CR1 antagonist E6130 (0,1, 1, 4,9, 10, 100, 1000nM) and/or treated with recombinant fractalkine (0.1, 0.5, 1, 5, 10, 50, 100, 200ng/mL) for 24 hours...Furthermore, these novel findings indicate that CX3CR1 antagonism holds therapeutic potential to reverse these pro-tumourigenic effects. Future in vitro and in vivo studies will further elucidate the role of fractalkine in OAC tumour growth and metastasis and confirm the therapeutic utility of CX3CR1 antagonism in this hard-to-treat cancer."

Esophageal Adenocarcinoma • Esophageal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • CX3CL1 • CX3CR1

EXPLORING THE APPLICABILITY OF CX3CR1 ANTAGONISM TO PROMOTE NK CELL MIGRATION TOWARDS THE TUMOUR IN OBESITY ASSOCIATED CANCER. (EACR 2022) - "Material and Methods NK cells were treated with OAC patient-derived adipose conditioned media (ACM) +/- CX3CR1 antagonist E6130 or fractalkine and/or IL-15...Differential NK cell phenotypes exist in obese and non-obese OAC patients, highlighting the detrimental systemic effects of visceral obesity on NK cell tumour surveillance. Our data provide novel insights into the therapeutic utility of CX3CR1 antagonism to enhance NK cell movement towards tumour in OAC."

Esophageal Adenocarcinoma • Esophageal Cancer • Gastrointestinal Cancer • Genetic Disorders • Obesity • Oncology • Solid Tumor • CX3CL1 • CX3CR1 • FASLG • IL15

The Omentum in Obesity-Associated Cancer: A Hindrance to Effective Natural Killer Cell Migration towards Tumour Which Can Be Overcome by CX3CR1 Antagonism. (PubMed, Cancers (Basel)) - "Our data uncover diminished NK cell migration towards OAC tumour tissue conditioned media (TCM) following exposure to omental adipose tissue conditioned media (ACM) and reveal that this migration can be rescued with CX3CR1 antagonist E6130...Interestingly, treatment with fractalkine and/or IL-15 do not significantly affect NK cell adhesion to MAdCAM-1, despite changes they elicit to the expression of integrin α4β7. This study provides further evidence that CX3CR1 antagonism has therapeutic utility in rescuing NK cells from the deleterious effects of the omentum and fractalkine in OAC, thus limiting their dysfunction."

Journal • Esophageal Cancer • Gastric Adenocarcinoma • Gastric Cancer • Gastroesophageal Junction Adenocarcinoma • Gastrointestinal Cancer • Genetic Disorders • Obesity • Oncology • Solid Tumor • CX3CL1 • IL15 • ITGA4