HCV-IN-7

HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity[1].

Signaling Pathways >> Anti-infection >> HCV

Research Areas >> Infection

IC50: 3-47 pM (genotypic HCV NS5A)[1]

HCV-IN-7 inhibits GT1b (IC50=12 pM), GT2a (IC50=5 pM), GT1a (IC50=27 pM), GT3a (IC50=47 pM), GT4a (IC50=3 pM), GT6a (IC50=28 pM)[1]. HCV-IN-7 (10 µM) has 12%, 42%, 12% inhibition for CYP2D6, CYP2C9, CYP3A4, respectively[1]. HCV-IN-7 (10 µM) has cytotoxicity of 14%, 22%, 36% in Huh7, HepG2 and HEK cells, respectively[1]. HCV-IN-7 has a less complex central tricyclic core as novel and potent pan-genotypic NS5A inhibitors with good pharmacokinetic profile[1].

HCV-IN-7 (iv; 1 mg/kg) has a T1/2 of 2 hours, CL of 11 mL/min/kg, and a Vss of 2 L/kg for rats[1]. HCV-IN-7 (po; 10 mg/kg) has a Cmax of 1 μM and an AUClast of 6 μM for rats[1]. HCV-IN-7 (iv; 1 mg/kg) has a T1/2 of 4 hours, CL of 6 mL/min/kg, and a Vss of 2 L/kg for dog[1]. HCV-IN-7 (po; 10 mg/kg) has a Cmax of 5 μM and an AUClast of 49 μM for dog[1].

[1]. Ramdas V, et al. Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate. J Med Chem. 2019 Dec 12;62(23):10563-10582.