Osalmid

Osalmid is an inhibitor of ribonucleoside-diphosphate reductase subunit M2 (RRM2; IC₅₀ = 8.2 µM).¹ It decreases hepatitis B virus (HBV) DNA replication in infected HepG2 2.2.15 cells (EC₅₀ = 45.8 µM) and reduces HBV DNA levels in the supernatant and lysates of infected HepG2 2.2.15 cells (EC₅₀s = 11.1 and 16.5 µM, respectively). Osalmid inhibits the replication of HBV resistant to the nucleoside reverse transcriptase inhibitor 3TC (lamivudine; Item No. 18514) in infected HepG2 cells (EC₅₀ = 19.8 µM). It reduces the proliferation of HepG2, Huh7, and HCCLM3 cells in a concentration-dependent manner and decreases the proliferation of a variety of esophageal squamous cell carcinoma cells (IC₅₀s = 144.8-182.3 µM).^2,3 Osalmid (400 mg/kg per day) reduces HBV DNA levels in serum and liver tissues in a transgenic mouse model of HBV infection. Intragastric administration of osalmid (200 mg/kg per day), in combination with radiation, reduces tumor growth in radiation-sensitive and -resistant KYSE-150 esophageal squamous cell carcinoma mouse xenograft models.³

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1. Liu, X., Xu, Z., Hou, C., et al. Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochem. Pharmacol. 103, 118-128 (2016).

2. Wu, Z., Zhan, Y., Wang, L., et al. Identification of osalmid metabolic profile and active metabolites with anti-tumor activity in human hepatocellular carcinoma cells. Biomed. Pharmacother. 130, 110556 (2020).

3. Tang, Q., Wu, L., Xu, M., et al. Osalmid, a novel identified RRM2 inhibitor, enhances radiosensitivity of esophageal cancer. Int. J. Radiat. Oncol. Biol. Phys. 108(5), 1368-1379 (2020).