CF101, generically known as IB-MECA (methyl 1-[N6-(3-iodobenzyl)-adenin-9-yl]-b-D-ribofuronamide), is an oral small molecule drug formulated in a tablet.
The drug molecular weight is 510 dalton, it is manufactured via a 4-step chemical synthesis (up-scaled to a semi-commercial level) and it’s half life time is 9 hours.
The activity of CF101 as an anti-inflammatory agent has been tested in a number of different experimental models including adjuvant and collagen induced arthritis and inflammatory bowel disease. In all models tested, CF101 induced a robust anti-inflammatory effect measured by clinical and histological disease scores.
Mechanism of Action
CF101 mechanism of action is A3AR mediated and includes modulation of key signaling proteins, such as PI3K, PKA, PKB/Akt, IKK and NF-кB, resulting in inhibition of inflammatory cytokine production.
The safety of CF101 has been demonstrated in preclinical studies, including among others, toxicology studies of up to 6 months in mice and 9 months in monkeys. CF101 has an excellent human safety profile, demonstrated in more than 1200 patients.
Can-Fite has tested CF101 in a number of Phase II studies in different diseases. A Phase II study in Psoriasis successfully met its primary endpoint showing that CF101 effectively ameliorated disease symptoms. In an interim analysis of the Phase II/III study the data justified full enrollment of the study. Phase II studies in Rheumatoid Arthritis (RA) demonstrated efficacy of CF101 given as a monotherapy. Moreover, a direct correlation between A3AR at baseline and patients’ response to CF101, suggesting its utilization as a predictive biomarker.