Additional Relevant Details
In the Phase 1 SAD trial, MORF-057 was well tolerated in all 5 cohorts receiving MORF-057 in single doses ranging from 25 mg to 400 mg with no serious adverse events (SAEs) and no significant lab abnormalities in any subject. In the study, MORF-057 exhibited a generally dose proportional and predictable pharmacokinetic profile. The key pharmacodynamic measurement in the trial was receptor occupancy (RO), which indicated the percentage of α4β7 bound by MORF-057 12 hours after the dose. MORF-057 achieved greater than 95% mean α4β7 RO across the three highest dose cohorts, including the observation of >99% RO in subjects in each cohort above 25mg. These single dose data demonstrate the potential that MORF-057 will be able to maintain saturating levels of receptor occupancy following twice daily oral administration. MORF-057 was specifically designed to be highly selective for α4β7 and not α4β1, a related integrin. Notably, we did not observe quantifiable levels of α4β1 RO in the study.