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This is a randomized, double-blind study to evaluate the safety, tolerability and PK of single and multiple ascending oral doses of RP7214. The relative bioavailability in fed and fasting conditions will also be evaluated for RP7214. The study comprises three parts; Part 1: Single ascending dose, Part 2: Multiple ascending dose and Part 3: Food effect.
There are three escalating cohorts in SAD part and two escalating cohorts in MAD part. In each cohort, six eligible healthy volunteers will be randomized to receive either RP7214 or placebo in 2:1 ratio. Within each cohort, two sentinel subjects (RP7214 and Placebo) will be dosed first for assessment of safety and tolerability. The safety data of at least 48 hrs will be reviewed to confirm safety of sentinel subjects after which the remaining four subjects will be dosed. Food effect study is a randomized, 2-treatment, 2-period, 2-sequence, crossover study in 12 HVs.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| RP7214, Single and multiple doses | Experimental | In Part 1 up to 3 cohorts with single ascending doses of RP7214 at 100 mg QD, 200 mg QD and 400 mg QD. In Part 2 up to 2 cohorts with multiple ascending doses of RP7214 at 200 mg BID, 400 mg BID. |
|
| Placebo, Single and multiple doses | Placebo Comparator | In Part 1 up to 3 cohorts and in Part 2 up to 2 cohorts with matching placebo to RP7214 tablet |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| RP7214 | Drug | Participants will receive single and multiple ascending doses of RP7214 |
|
| Measure | Description | Time Frame |
|---|---|---|
| Assessments of Adverse Events (AEs) | Day1 - day15 |
| Measure | Description | Time Frame |
|---|---|---|
| RP7214 Cmax | Maximum Observed Plasma Concentration | 0, 0.25, 0.5, 1, 2, 4, 6, 8 and 12 hrs post dose |
| RP7214 Tmax | Time for maximum plasma concentration |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Rhizen Investigational Site | Las Vegas | Nevada | 89121 | United States | ||
| Rhizen Investigational Site |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 36217901 | Derived | Nair A, Barde PJ, Routhu KV, Viswanadha S, Veeraraghavan S, Pak S, Peterson JA, Vakkalanka S. A first in man study to evaluate the safety, pharmacokinetics and pharmacodynamics of RP7214, a dihydroorotate dehydrogenase inhibitor in healthy subjects. Br J Clin Pharmacol. 2023 Mar;89(3):1127-1138. doi: 10.1111/bcp.15562. Epub 2022 Nov 1. |
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| ID | Term |
|---|---|
| C000718746 | RP7214 |
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| Placebo | Drug | Participants will receive single and multiple ascending doses of matching placebo |
|
| 0, 0.25, 0.5, 1, 2, 4, 6, 8 and 12 hrs post dose |
| RP7214 t½ | Terminal half-life | 0, 0.25, 0.5, 1, 2, 4, 6, 8 and 12 hrs post dose |
| RP7214 AUC0-inf | Area under the plasma concentration time curve from zero extrapolated to infinite time | 0, 0.25, 0.5, 1, 2, 4, 6, 8 and 12 hrs post dose |
| Fargo |
| North Dakota |
| 58104 |
| United States |