AP1189 is a first in class ip protected biased agonist to the melanocortin type 1 (MCr1) and type 3 (MCr3) receptors. The MC1r and MC3r are present on key cells in the immune system including neutrophils and macrophages. When the AP1189 compound activates the receptors EKR 1/2 phosphorylation is activated, which is associated to a number of anti-inflammatory and pro-resolving effects. The compound thereby reduces ongoing inflammation, but compared to most other anti-inflammatory compound in addition stimulate endogen pathways that promote facilitation on the clearance of the inflammation, ie resolution.
The compound has shown its effect in state-of-the-art models of inflammation as well as is experimental models of inflammatory and autoimmune diseases.
The compound is currently in clinical Phase 2a where the compound is tested as an add-on to methotrexate treatment in previous methotrexate naïve patients with active Rheumatoid Arthritis.
- AP1189 is biased agonist to the MC1r and MCr3, ie the compound mediates its effect though EKR 1/2 phosphorylation, but not cAMP within the target cells. One beneficial effect of the biased agonism is that AP1189 compared to all other known MC1r agonists does not stimulate melanocytes and thereby unwanted skin pigmentation.
- AP1189 is developed for once daily oral administration – other MCr stimulating compounds including the ACTHAR Gel (on the US market) are given as injections
- In contrast to ACTHAR gel and other compound where ACTH is the active ingredient, AP1189 does not stimulate the MC2r receptors, which mean that AP1189 does not induce a number of MC2r mediated unwanted and often treatment limiting side effects
- AP1189 induce resolution of inflammation, ie a combination of anti-inflammatory and pro-resolving effect that compared to most other treatments aimed for inflammatory and autoimmune diseases does not induce immuno-suppression, which in many cases in to be considered an un-wanted and often treatment limiting adverse effect.
- The current development program is aimed to show Proof of concept in relevant inflammatory and autoimmune diseases, with focus on Rheumatoid Arthritis and Nephrotic Syndrome
- The aim is to continue development beyond Clinical Phase 2a in collaboration with a pharmaceutical partner better fitted to take responsibility for larger Clinical trials including Phase 3 development, marked authorisation and marketing