What Are the Uses of Oclatinib?

1. The role of Oclacitinib

Oclacitinib is a synthetic, intracellular, non-receptor tyrosine kinase inhibitor that works by inhibiting various cytokines that depend on JAK1 and JAK3 enzyme activity, which induce itching, inflammation, and allergic cytokines.

Oclacitinib is a novel JAK inhibitor that also inhibits the function of JAK1-dependent cytokines in some anti-allergy, inflammation, and itching reactions. Studies have shown that oral administration of 0.4-0.6mg/kg of Oclacitinib twice a day in experimental animals (dogs) is safe and effective for treating itching caused by atopic dermatitis, and oclacitinib maleate for dogs has better efficacy than oral corticosteroids such as prednisolone. During treatment, Oclacitinib can relieve itching within 24 hours, and over 70% of experimental animals showed a reduction of more than 50% in itching reactions by day 7.

2. Clinical applications of Oclacitinib

Currently, Oclacitinib has been approved by the US FDA in 2013 for controlling itching and atopic dermatitis caused by canine allergic dermatitis. However, although Oclacitinib has good efficacy in treating canine allergic skin diseases, its scope of action is relatively narrow. On the one hand, it has little impact on cytokines that do not participate in JAK1 activation. On the other hand, its effect on allergic reactions ultimately only manifests in inhibiting the release of mast cell granules, i.e., allergic mediators, and cannot fundamentally block the binding of allergic mediators to their relevant receptors, thereby not fundamentally preventing the occurrence and development of allergic skin diseases.

Oclacitinib is a novel Janus kinase (JAK) inhibitor with activity against allergy-related cytokines. It was approved by the US FDA in 2013 for controlling itching and atopic dermatitis caused by canine allergic dermatitis. Oclacitinib (PF03394197) is a novel JAK and JAK1-dependent cytokines inhibitor with IC50 values of 10-99nM (JAK family members) and 36-249nM (JAK1-dependent cytokines), respectively. It is a highly effective JAK1 inhibitor and also inhibits the function of JAK1-dependent cytokines in some anti-allergy, inflammation, and itching reactions. It has little impact on cytokines that do not participate in JAK1 activation. Oral administration of Oclacitinib twice a day at a dose of 0.4-0.6mg/kg is safe and effective for treating itching caused by atopic dermatitis. During treatment, Oclacitinib can relieve itching within 24 hours, and in experiments, over 70% of experimental animals (dogs) showed a reduction of more than 50% in itching reactions by day 7.