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The purpose of this study is to assess the safety, tolerability and pharmacokinetics of multiple doses of PNU-100480 given for 14 or 28 days. Killing activity against the bacterium that causes tuberculosis (TB) will also be measured. The effect of adding an additional tuberculosis (TB) agent (given for 2 days) in addition to PNU-100480 will be evaluated. Linezolid open label to determine activity in whole blood assay (WBA).
Evaluate safety, tolerability, pharmacokinetics and whole blood activity (WBA) of PNU-100480 given for 14 or 28 days; evaluate WBA of PNU with pyrazinamide; evaluate WBA of linezolid
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1 | Experimental |
| |
| Cohort 2 | Experimental |
| |
| Cohort 3 | Experimental |
| |
| Cohort 4 | Experimental |
| |
| Cohort 5 | Experimental |
| |
| Cohort 6 (optional) | Experimental |
| |
| Linezolid Cohort | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PNU-100480 | Drug | 100 mg BID for 14 days |
| |
| Placebo |
| Measure | Description | Time Frame |
|---|---|---|
| To evaluate the safety and tolerability of ascending oral doses of PNU-100480 administered as extemporaneously prepared suspension (EPS) over 14 and 28 days in healthy adult volunteers. | Monitor adverse events daily; safety eval pre-dose, specified times , discharge, follow-up/as needed |
| Measure | Description | Time Frame |
|---|---|---|
| To characterize the single dose and steady state pharmacokinetics of ascending oral doses of PNU-100480 administered over 14 and 28 days in healthy adult volunteers with regard to the parent drug and its metabolites. | Full and sparse PK sampling from Day 1 through final day of dosing | |
| To characterize the bactericidal activity in blood of orally administered PNU-100480 against intracellular M. tuberculosis in relation to blood concentrations ofPNU-100480 and its metabolites. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Lisa Beth Ferstenberg, M.D. | Sequella, Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pfizer Investigational Site | New Haven | Connecticut | 06511 | United States |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 20629533 | Derived | Wallis RS, Jakubiec WM, Kumar V, Silvia AM, Paige D, Dimitrova D, Li X, Ladutko L, Campbell S, Friedland G, Mitton-Fry M, Miller PF. Pharmacokinetics and whole-blood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers. J Infect Dis. 2010 Sep 1;202(5):745-51. doi: 10.1086/655471. |
| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| Drug |
to match 100 mg BID for 14 days |
|
| PNU-100480 | Drug | 300 mg BID for 14 days |
|
| Placebo | Drug | to match 300 mg BID for 14 days |
|
| PNU-100480 | Drug | 600 mg BID for 14 days |
|
| Placebo | Drug | to match 600 mg BID for 14 days |
|
| PNU-100480 | Drug | 1200 mg QD for 14 days |
|
| Placebo | Drug | to match 1200 mg QD for 14 days |
|
| PNU-100480 | Drug | 600 mg BID for 28 days with pyrazinamide (25 mg/kg up to 2 g) QD on Days 27-28 |
|
| Placebo | Drug | placebo to match 600 mg BID for 28 days with pyrazinamide (25 mg/kg up to 2 g) QD on Days 27-28 |
|
| PNU-100480 | Drug | PNU-100480 dose up to total of 1200 mg daily for 28 days with pyrazinamide (25 mg/kg up to 2 g) QD on Days 27-28 |
|
| Placebo | Drug | placebo to match dose up to total of 1200 mg daily for 28 days with pyrazinamide (25 mg/kg up to 2 g) QD on Days 27-28 |
|
| Linezolid | Drug | 300 mg QD for 4 days (open label) |
|
| Full and sparse sampling from Day 1 through final day of dosing |
| To characterize the effect of once a day administration of pyrazinamide for 2 days on the pharmacokinetics and bactericidal activity in blood of orally administered PNU-100480 against intracellular M. tuberculosis (Cohorts 5 and 6, Days 27-28 only). | Days 27-28 as applicable |
| To characterize pharmacokinetics and bactericidal activity in blood of orally administered linezolid against intracellular M. tuberculosis following 4 days of QD dosing. | As applicable up to Day 4 |
| ID | Term |
|---|---|
| D014376 | Tuberculosis |
| ID | Term |
|---|---|
| D009164 | Mycobacterium Infections |
| D000193 | Actinomycetales Infections |
| D016908 | Gram-Positive Bacterial Infections |
| D001424 | Bacterial Infections |
| D001423 | Bacterial Infections and Mycoses |
| D007239 | Infections |
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| ID | Term |
|---|---|
| C543015 | PNU-100480 |
| D000069349 | Linezolid |
| ID | Term |
|---|---|
| D000081 | Acetamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D000085 | Acetates |
| D000144 | Acids, Acyclic |
| D002264 | Carboxylic Acids |
| D023303 | Oxazolidinones |
| D010080 | Oxazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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