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CF101
Drug
Product
CF101 is an oral small molecule formulated in a tablet. The active ingredient
in CF101 is IB-MECA, a highly specific and selective agonist at the A3
adenosine receptor (A3AR).
Preclinical
Pharmacology
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 dramatic anti-inflammatory effect measured by clinical
and histological disease scores.
Mechanism
of action
CF101 down-regulates the PI3K/PKB/Akt pathway, resulting in the inhibition
of NF-kB and TNF-a.
It has been further demonstrated that the mechanism involves the up-regulation
of caspase-3 leading to apoptosis of inflammatory cells. The immuno-modulatory
effect of CF101 entails inhibition of inflammatory cytokine production
and inhibition of auto-regulatory T cell proliferation.
Safety
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 600 patients with RA, Psoriasis, Dry Eye and Cancer.
Efficacy
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 addition, CF101 met the primary endpoint of a Phase II study
in Dry Eye syndrome demonstrating the drug's ability
to improve disease symptoms. In the Dry Eye study, a reduction in intraocular
pressure (IOP) was observed demonstrating CF101's potential as a glaucoma
therapy.
A Phase II study in Rheumatoid
Arthritis (RA) demonstrated efficacy of CF101 given as a monotherapy.
Moreover, the expression level of A3AR was directly
correlated with patient responses to CF101, suggesting its utilization
as a predictive biomarker.
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