AR-12

AR-12 is an orally available small molecule drug developed as a targeted therapy for cancer and infectious diseases. It is a celecoxib derivative that does not inhibit cyclooxygenase activity but instead acts primarily by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1), leading to downregulation of the PI3K/Akt signaling pathway involved in cell growth and proliferation[2][3][1]. This inhibition results in reduced tumor cell proliferation and induction of apoptosis. In addition to its anticancer effects, AR-12 has demonstrated broad-spectrum antifungal activity by inhibiting fungal acetyl coenzyme A synthetase and inducing autophagy[5][7]. It also exhibits antiviral properties against various viruses including HIV, Influenza A, Chikungunya, Ebola, Lassa virus, and SARS-CoV-2[8][4][3]. The drug has completed Phase 1 clinical trials for cancer indications and has received orphan drug designations in Europe for cryptococcosis and tularaemia[6]. Preclinical studies have shown efficacy against a wide range of solid tumors (breast, lung, prostate, pancreatic) as well as hematological malignancies both as monotherapy and in combination with other agents[1].

Other names

PDK1 inhibitor AR-12PDK-1 inhibitor AR-12PDK 1 inhibitor AR-12celecoxib derivative kinase inhibitor AR-12AR-12 hydrochlorideAR12 hydrochlorideAR 12 hydrochloride