Provided are 2,4-disubstituted quinoline derivatives that are A3 adenosine receptor modulators (A3RM), for use in the treatment of a condition which is treatable by adenosine, an A3 adenosine receptor (A3AR) agonist, or an A3 adenosine receptor antagonist. The 2,4-disubstituted quinoline derivatives can be used in the treatment of a condition treatable by an adenosine or an A3AR agonist, by enhancing activity of a protein (by binding of said 2,4-disubstituted quinoline derivative to the A3AR). Some conditions treatable by the 2,4-disubstituted quinoline derivative when used for enhancing activity include, malignancy, an immuno-compromised affliction, high intraocular pressure, or a condition associated with high intraocular pressure. Further provided is a method for treatment of a subject having a condition treatable by adenosine, an A3AR agonist, or an A3AR antagonist making use of the defined 2,4-disubstituted quinoline derivative (s), and pharmaceutical composition and comprising said derivative and a kit comprising the derivative and instructions for use thereof. One specific 2,4-disubstituted quinoline derivative includes N-{2-[(3,4-dichlorophenyl)amino]quinolin-4-yl}cyclohexanecarboxamide. The 2,4-disubstituted quinoline derivatives can be formulated in a form suitable for oral administration.
