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The study objectives are to define the safety and tolerability profile of oral, single ascending dose (SAD) levels of HOPO 14-1 capsules in cohorts of healthy participants and to assess the pharmacokinetic (PK) and excretion profile of HOPO 14-1. The study hypothesis is that a single dose of HOPO 14-1 will be safe and tolerable up to 7500 mg.
The currently available therapy for radionuclide internal contamination is suboptimal. Pharmacological and toxicological data support the clinical development of HOPO 14-1 for decorporation of radionuclides.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1: 100 mg | Experimental | Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1. |
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| Cohort 2: 200 mg | Experimental | Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1. |
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| Cohort 3: 500 mg | Experimental | Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1. |
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| Cohort 4: 1200 mg | Experimental | Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1. |
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| Cohort 5: 2500 mg | Experimental | Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1. |
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| Cohort 6: 5000 mg | Experimental |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| HOPO 14-1 | Drug | HOPO 14-1 contains the active pharmaceutical ingredient (API) 3, 4, 3-LI(1, 2-HOPO) formulated with a permeability enhancer, sodium oleate, in capsule form. |
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| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants with One or More Adverse Events | Up to 14 days | |
| Number of Participants with One or More Drug-Related Adverse Events | Up to 14 days | |
| Number of Participants with One or More Adverse Events by Maximum Severity | Up to 14 days | |
| Number of Participants with One or More Serious Adverse Events | Up to 14 days |
| Measure | Description | Time Frame |
|---|---|---|
| Observed Maximum Plasma Concentration (Cmax) | Up to Day 7 | |
| Observed Time to Reach Cmax (Tmax) | Up to Day 7 | |
| Area Under the Plasma Concentration Time Curve up to the Last Blood Collection Time with a Measurable Concentration (AUClast) |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| SRI International Clinical Trials Unit | Plymouth | Michigan | 48170 | United States |
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Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1.
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| Cohort 7: 7500 mg | Experimental | Participants receive an oral single dose of HOPO 14-1 in the fasted condition on Day 1. |
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| Up to Day 7 |
| Extrapolated to Infinity (AUC0-inf) | Up to Day 7 |
| Terminal Half-Life (t 1/2) | Up to Day 7 |
| Apparent Volume of Distribution after Oral Administration (V/F) | Up to Day 7 |
| Oral Systemic Clearance Rate (CL/F) | Up to Day 7 |
| Cumulative Amount Excreted in Urine | Up to Day 7 |
| Cumulative Amount Excreted in Feces | Up to Day 7 |