Pipeline
A portfolio focused on proven immunology targets
We are advancing a suite of small molecule inhibitors against clinically validated inflammation and immunology targets.
AREA
Immunology & Inflammation (I & I)
I & I
I & I
AREA
Solid Tumors
Solid Tumors
Programs
STAT6: in development for atopic dermatitis, asthma, and other indications
IL-14 and IL-13 are cytokines that orchestrate the cardinal features of Type 2 inflammation, a specific immune system activation primarily driven by T helper 2 (Th2) cells, type 2 innate lymphoid cells (ILC2s) and eosinophils. The excessive Type 2 inflammation triggers an inflammatory cascade causing various allergic and inflammatory conditions. Blocking IL-4 and IL-13, by antibodies like Dupilumab, has been shown to effectively treat many inflammatory diseases, such as asthma, atopic dermatitis, allergic rhinitis, and nasal polyps.
Both IL-4 and IL-13 signals converge on STAT6, a key transcription factor driving Th2 cell differentiation, B cell activation, IgE antibody production, eosinophils activation, and tissue inflammation. Inhibition of STAT6 can block the overactive type 2 inflammation with potential of Dupilumab-like efficacy in multiple Type 2 inflammatory diseases. Our STAT6 lead candidate is a highly potent small molecule that can selectively block STAT6 activation. This candidate combines biologic-like efficacy with the advantage of oral small molecule therapy, and has the potential to bring relief and convenience to millions of patients worldwide.
TNFα: in development for rheumatoid arthritis (RA) and other indications
TNFα is implicated in multiple diseases and is a validated target in autoimmune conditions such as RA. While current biologics are effective, they have limitations. Oral TNFa small molecule inhibitors offer significant advantages over biologics, including ease of administration and reduced immunogenicity.
Our lead candidate is an oral small molecule TNFα inhibitor in development for the treatment of RA, with the potential for broader autoimmune applications. Our candidate has demonstrated a best-in-class small molecule profile and was well-tolerated in preclinical studies.
Interleukin 17 (IL-17) AA + AF: in discovery for the treatment of psoriasis and other indications
IL-17 serves as a critical mediator in the inflammatory cascade of psoriasis. IL-17 AA + AF are validated targets for psoriasis, with several therapies on the market.
While existing IL-17 inhibitors are effective for many, efficacy is not universal due to the complexity of psoriasis, antidrug antibodies, and individual variations in disease mechanisms.
Our candidate is a dual oral small molecule IL-17 AA + AF inhibitor in development for the treatment of psoriasis, with the potential for broader autoimmune applications. Our in vivo lead compounds show superior potency versus competitor small molecules and demonstrate significant suppression of arthritis in rat CIA models.
STAT6: in discovery for asthma and other indications
STAT6 is a key modulator in type 2 inflammation diseases such as asthma and atopic dermatitis. Injectable anti-IL-4/IL-13 antibodies have demonstrated clinical benefits by suppressing STAT6 activation in multiple type 2 inflammation diseases. However, biologics have limited patient coverage due to the route of administration. Oral STAT6 inhibitors should provide unique advantages with ease of administration and biologic-like activity.
Our lead STAT6 small molecule inhibitors exhibited high potency and selectivity in both biochemical and cellular assays. Future activities are focused on the optimization of pharmacokinetic properties leading to an oral small molecule candidate for clinical development.
