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AJ302 is a first-in-class HDAC6 inhibitor under development for the prevention and/or treatment of chemotherapy-induced peripheral neuropathy. Phase 1 clinical trial of AJ302 will be initiated in early 2021.
AJ302 was selected among quinazolin-2,4-dione-based hydroxamic acids designed and synthesized by scientists at AnnJi for its HDAC6 inhibition activity in vitro and in vivo, its selectivity over other HDACs, its safety profile and its drug like physiochemical properties.
It is a highly selective inhibitor of HDAC6 which promotes neurite growth and branches. The selective inhibition of HDAC6 can substantially reduce drug toxicity while maintaining on target activity. In a rat CIPN model, AJ302 reversed paclitaxel-induced allodynia, and the pain relief was maintained for two weeks after dosing which suggests restoration of neurons. AJ302 may be useful in providing a much-needed drug for the treatment and/or prevention of CIPN in cancer patients receiving chemotherapy drugs.
AJ303 is a novel compound under development for the treatment of idiopathic pulmonary fibrosis (IPF). It decreased IPF-related inflammatory cytokines, such as IL-6, MCP1, and GM-CSF in vitro, that delays the progression of pulmonary fibrosis in bleomycin-induced pulmonary injury model in mice.
AJ303 has a favorable plasma to pulmonary ratio of tissue distribution after oral administration. Its potential efficacy in treating patients with IPF will be investigated clinically in 2021.
AJ502 is a novel, potent, and selective PDE4 inhibitor that has good skin permeating characteristics. Topically administered AJ502 showed efficacy in IMQ-induced psoriasis and PMA-induced atopic dermatitis in the animal models superior to that of marketed comparators. AJ502 is at IND-enabling stage.
AJ503 is an oral program of PDE4 inhibitor under candidate selection for the treatment for systemic inflammatory disorders such as psoriasis, rheumatoid arthritis, ankylosing spondylitis, and other inflammatory bowel disease (IBD).
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