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This will be a Phase I, open-label, nonrandomized, single-dose study in healthy male subjects.
Potential subjects will be screened to assess their eligibility to enter the study within 28 days prior to the dose administration. Subjects will be admitted into the Clinical Research Unit (CRU) on Day -1 and be confined to the CRU until at least Day 8. On Day 1, subjects will receive a single oral dose of [14C]-saroglitazar magnesium. Subjects will be discharged if the following discharge criteria are met: plasma radioactivity levels below the limit of quantitation for 2 consecutive collections and ≥ 90% mass balance recovery, or ≤ 1% of the total radioactive dose is recovered in combined excreta (urine and feces) in 3 consecutive 24-hour periods in which both are collected. If discharge criteria are not met by Day 8, subjects will remain in the CRU up to Day 12.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Study Treatment | Experimental | 4 mg [14C]-saroglitazar magnesium (approximately 100 μCi) oral suspension |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Saroglitazar magnesium | Drug | On Day 1, subjects will receive a single oral dose of [14C]-saroglitazar magnesium |
|
| Measure | Description | Time Frame |
|---|---|---|
| AUC from time zero to infinity (AUC0-∞) | Area under the time curve from time zero to infinity will be calculated for saroglitazar and saroglitazar sulfoxide in plasma, and total radioactivity in whole blood and plasma | At predose to maximum up to Day 12 |
| AUC from time zero to the last quantifiable concentration (AUC0-t) administration of [14C]-saroglitazar magnesium | Area under the time curve from time zero to the last quantifiable concentration will be calculated for saroglitazar and saroglitazar sulfoxide in plasma, and total radioactivity in whole blood and plasma | At predose to maximum up to Day 12 |
| Cmax | Maximum observed concentration will be calculated for saroglitazar and saroglitazar sulfoxide in plasma, and total radioactivity in whole blood and plasma | At predose to maximum up to Day 12 |
| Tmax | Time to reach maximum observed concentration will be calculated for saroglitazar and saroglitazar sulfoxide in plasma, and total radioactivity in whole blood and plasma | At predose to maximum up to Day 12 |
| t1/2 | Apparent terminal elimination half-life will be calculated for saroglitazar and saroglitazar sulfoxide in plasma, and total radioactivity in whole blood and plasma | At predose to maximum up to Day 12 |
| Apparent total clearance (CL/F) | The apparent total clearance (CL/F) will be determined for saroglitazar | At predose to maximum up to Day 12 |
| Measure | Description | Time Frame |
|---|---|---|
| Metabolic profile/ identifications of metabolites and probable structure elucidation for saroglitazar in plasma, urine, and feces | Metabolic profile/ identifications of metabolites and probable structure elucidation for saroglitazar in different matrices like plasma, urine, and feces will be performed and reported | Maximum up to Day 12 |
| Measure | Description | Time Frame |
|---|---|---|
| Amount of Saroglitazar excreted in feces | Amount of Saroglitazar in Fecal samples will be calculated. | At predose to maximum up to Day 12 |
| Percentage of Saroglitazar excreted in feces | Percentage of Saroglitazar excreted in Fecal samples will be calculated. |
Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| John E. Blanchard, MD | Covance | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Covance Clinical Research Unit Inc. | Madison | Wisconsin | 53704 | United States |
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| ID | Term |
|---|---|
| C000588741 | saroglitazar |
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| Apparent volume of distribution (Vz/F) during the terminal elimination phase | The Apparent volume of distribution (Vz/F) during the terminal elimination phase will be determined for saroglitazar | At predose to maximum up to Day 12 |
| AUC0-∞ of plasma saroglitazar relative to AUC0-∞ of plasma total radioactivity (AUC0-∞ Plasma saroglitazar/Total Radioactivity Ratio) | AUC0-∞ of plasma saroglitazar relative to AUC0-∞ of plasma total radioactivity (AUC0-∞ Plasma saroglitazar/Total Radioactivity Ratio) will be calculated | At predose to maximum up to Day 12 |
| AUC0-∞ of whole blood total radioactivity to AUC0-∞ of plasma total radioactivity (AUC0 ∞ Blood/Plasma Ratio) | AUC0-∞ of whole blood total radioactivity to AUC0-∞ of plasma total radioactivity (AUC0 ∞ Blood/Plasma Ratio) will be calculated | At predose to maximum up to Day 12 |
| Mean residence time | Mean residence time for saroglitazar and saroglitazar sulfoxide will be calculated | At predose to maximum up to Day 12 |
| Total radioactivity amount excreted in urine and feces | Amount of radioactivity excreted in urine and Feces will be calculated. | At predose to maximum up to Day 12 |
| Percentage radioactivity excreted in urine and feces | Percentage radioactivity excreted in urine and Feces will be calculated. | At predose to maximum up to Day 12 |
| Renal clearance (CLR) | Renal clearance for saroglitazar and saroglitazar sulfoxide will be determined | At predose to maximum up to Day 12 |
| Number of Participants with Adverse Events (AEs) as a Measure of Safety and Tolerability |
Incidence and severity of AEs as a measure of safety and tolerability will be measured and reported |
| Maximum up to Day 12 |
| At predose to maximum up to Day 12 |