Teglarinad chloride (GMX-1777 chloride) is a potent inhibitor of NAMPT, the precursor of GMX1778.Teglarinad chloride has antitumor activity and acts by interfering with DNA repair and inhibiting angiogenesis.

In the IM-9 model, small-cell lung cancer (SHP-77) model, and colon carcinoma (HCT-116) model, GMX1777 (75 mg/kg; 24 h intravenous infusion) induces tumor regression[2].For both FaDu and C666-1 tumors in vivo, GMX1777 (50-100 mg/kg/day, intramuscular for 5 days), with or without local tumor radiotherapy, proves to be effective[1].Upon intravenous infusion (25-400 mg/kg; 24 h), GMX1777 is rapidly converted to GMX1778 in the plasma of mice, with a half-life of GMX1777 less than 0.7 h[1].