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GSK835726 is an orally bioavailable small molecule that acts as a dual antagonist of the histamine H1 and H3 receptors. Developed by GSK, it was primarily investigated for the treatment of seasonal allergic rhinitis (SAR). The rationale for the dual H1/H3 mechanism was to combine the established anti-allergic effects of H1 antagonism (addressing sneezing, itching, and runny nose) with the potential of H3 antagonism to alleviate nasal congestion, a symptom often poorly controlled by standard antihistamines. The drug underwent Phase 1 safety and pharmacokinetic testing and Phase 2 efficacy evaluations in environmental challenge chambers, but development was ultimately discontinued.
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