China’s Shenzhen Salubris Pharmaceuticals Co., Ltd (SHE: 002294) has announced receiving approval from the National Medical Products Administration (NMPA) to conduct a Phase I clinical study for its 3CL protease inhibitor SAL0133 in adult patients with mild to common COVID-19. This marks a significant step forward in the development of this innovative antiviral therapy.
Mechanism and Preclinical Profile
3CLpro plays a crucial role in the RNA replication of the novel coronavirus, particularly in the initial replication stage after the virus enters the host cell. By inhibiting the activity of 3CLpro protease, SAL0133 can effectively block virus replication and achieve antiviral effects. Preclinical studies have shown that SAL0133 demonstrates strong inhibitory activity against 3CLpro at the enzyme level and has potent antiviral activity against wild-type COVID-19 and five variants: Alpha (B.1), Beta, Delta, and Omicron BA.2 and BA.5. Notably, the EC90 value of antiviral activity against the Omicron BA.5 variant was 10 times higher than that of nirmatrelvir.
In animal models infected with COVID-19, SAL0133 significantly reduced viral load in lung tissue and markedly improved lung inflammation. The dose required to achieve significant viral load reduction was lower than that of nirmatrelvir. Nonclinical pharmacokinetic studies confirmed that SAL0133 exhibits good oral absorption characteristics, high oral bioavailability, a long half-life, good metabolic stability, and high oral exposure. The GLP toxicological study demonstrated that SAL0133 has good safety.
Future Outlook
The approval for the Phase I clinical study of SAL0133 underscores Salubris Pharmaceuticals’ commitment to advancing innovative treatments for COVID-19. With its demonstrated preclinical efficacy and safety profile, SAL0133 has the potential to make a significant impact on patient outcomes. Salubris’ ongoing efforts in clinical development highlight its dedication to improving treatment options and addressing significant unmet needs in the management of COVID-19.-Fineline Info & Tech
