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Drug Names(s): XOPH5
Topokine’s XAF5 is an undisclosed prostaglandin that selectively binds a G protein-coupled receptor and modifies a key metabolic pathway involved in lipid metabolism and adipocyte maturation. Applied to the lower eyelids once nightly, XAF5 penetrates the skin and shrinks fat cells which helps reduce under-eye bags.
XAF5 was initially developed as a treatment for glaucoma. Prostaglandin-associated periorbitopathy (PAP), is a side effect of prostaglandin eye drops and results in sunken eyes as well as the shrinking of bags under the eye. In PAP, prostaglandin molecules, specifically PGF2 and its analogues, bind the Prostaglandin F receptor on orbital preadipocytes and activate Mitogen Activated Protein Kinase. This results in the phosphorylation and thus inactivation of Peroxisome Proliferator Activated Receptor Gamma (PPAR-gamma) and results in an overall inhibition of adipocyte differentiation, a decrease in levels of lipoprotein lipase, and a subsequent decrease of fat accumulation within the adipocyte. While testing XAF5 for glaucoma, doctors noticed that within weeks it caused the fat around the eyes to shrink without any of the unwanted effects of PAP such as sunken eyes.
XAF5 may eventually be evaluated for fat reduction of double chins and belly fat.
Allergan and Topokine
In April 2016, Allergan announced that it has acquired Topokine Therapeutics. Under the terms of the agreement, Allergan acquired Topokine Therapeutics for an upfront payment of $85 million and success-based development and sales milestones for XAF5 for the treatment of steatoblepharon, also known as undereye bags.
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