Sorrento Successfully Completes Phase 1 Study and Is Proceeding to Implement Global Registrational Trials with STI-1558, an Oral Mpro Inhibitor as a Standalone Oral Treatment and Prevention of COVID-19 without the Need for a Ritonavir Booster
- Phase 1 Study (with 58 healthy volunteers) of STI-1558 was completed in
Australiawith 300 mg, 600 mg, 1,200 mg and 2,000 mg doses in the single ascending dose (SAD) portion of the study and 300 mg, 600 mg and 800 mg BID (twice a day) daily for 7.5 days in the multiple ascending dose (MAD) portion of the study.
- The pharmacokinetics (PK) were dose proportional in the SAD study. In the MAD study, the 600 mg BID dose cohort achieved trough concentrations (Ctrough) significantly above the EC90 value for viral inhibition by STI-1558 and no accumulation was seen in the subjects, supporting a 600 mg twice daily dose for 5 days as the recommended dose for standalone treatment without ritonavir as booster.
- There were no serious adverse events (SAEs) or severe treatment emergent adverse events (TEAEs) and the maximum tolerated dose (MTD) was not reached in either the SAD (up to 2000 mg) or the MAD (up to 800 mg BID daily for 7.5 days) portions of the study.
- Global registrational Phase 2/3 trials of STI-1558 as a standalone treatment of COVID-19 are proceeding and are expected to be implemented rapidly in the US,
Mexico, China, Australiaand other regions.
The Phase 1 safety and PK study in healthy volunteers was conducted in
The preliminary blinded safety and PK data from the SAD and MAD portions of the study are available. Overall, there were no changes in vital signs, physical examinations, ECGs or safety clinical labs resulting from study participation. The preliminary summary of treatment-emergent adverse events (TEAEs) showed that there were no serious AEs (SAEs) or severe TEAEs and the maximum tolerated dose was not reached in either the SAD or MAD portions of the study. No dose limiting toxicities were noted and there were no premature terminations from the study post-treatment.
The linear and semi-log plots for doses from 300 mg to 2000 mg (Cohorts 1-4) are proportional in the SAD portion. In the 600 mg BID dose cohort of the MAD portion, the trough concentration (Ctrough) was significantly above the EC90 value of predicted value for viral inhibition and no accumulation was seen, supporting a 600 mg twice-daily dose as a recommended dose for standalone treatment without ritonavir booster. In preclinical study, STI-1558 has shown sufficient lung tissue penetration and dual inhibition of Mpro for viral replication and cathepsin L for viral entry to host cells, indicating a potential robust antiviral activity in COVID-19 patients.
A phase 1 trial in participants infected with SARS-CoV-2 has been initiated in
A large Phase 2 registrational study is planned in
“The successful completion of the Phase 1 in
About Sorrento Therapeutics, Inc.
Sorrento is a clinical and commercial stage biopharmaceutical company developing new therapies to treat cancer, pain (non-opioid treatments), autoimmune disease and COVID-19. Sorrento's multimodal, multipronged approach to fighting cancer is made possible by its extensive immuno-oncology platforms, including key assets such as next-generation tyrosine kinase inhibitors (“TKIs”), fully human antibodies (“G-MAB™ library”), immuno-cellular therapies (“DAR-T™”), antibody-drug conjugates (“ADCs”), and oncolytic virus (“Seprehvec™”). Sorrento is also developing potential antiviral therapies and vaccines against coronaviruses, including STI-1558, COVISHIELD™ and COVIDROPS™; and diagnostic test solutions, including COVIMARK™.
Sorrento's commitment to life-enhancing therapies for patients is also demonstrated by our effort to advance a TRPV1 agonist, non-opioid pain management small molecule, resiniferatoxin (“RTX”), and SP-102 (10 mg, dexamethasone sodium phosphate viscous gel) (SEMDEXA™), a novel, viscous gel formulation of a widely used corticosteroid for epidural injections to treat lumbosacral radicular pain, or sciatica, and to commercialize ZTlido® (lidocaine topical system) 1.8% for the treatment of postherpetic neuralgia (PHN). RTX has been cleared for a Phase II trial for intractable pain associated with cancer and a Phase II trial in osteoarthritis patients. Positive final results from the Phase III Pivotal Trial C.L.E.A.R. Program for SEMDEXA™, its novel, non-opioid product for the treatment of lumbosacral radicular pain (sciatica), were announced in
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Source: Sorrento Therapeutics, Inc.