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TG-2349 oral solution has been investigated in a phase I/IIa study (study number: TG-2349-01) in healthy volunteers and patients with chronic hepatitis C (CHC) infection. The study demonstrated that TG-2349 was safe and well-tolerated when given to healthy volunteers at single oral doses up to 800 mg, and at five-consecutive daily oral doses up to 600 mg. Co-administration of TG-2349 with food resulted in a significant increase in bioavailability, and therefore concomitant food intake with dosing is recommended.
To further advance the clinical development of TG-2349, a new capsule formulation was developed to replace the current TG-2349 oral solution. The objectives of this study (study number: TG-2349-02) are to evaluate the PK and relative bioavailability of TG-2349, given as a new capsule formulation and as the original formulation of oral solution, after a single oral dose of 400 mg under fed condition in healthy volunteers, and to evaluate the safety, tolerability, and ethnic differences of the TG-2349 capsule formulation.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| TG-2349 as the original formulation | Experimental | 400 mg, 2 syringes |
|
| TG-2349 as a new capsule formulation | Experimental | 400 mg, 4 capsules |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TG-2349 as the original formulation | Drug | single oral dose under fed condition |
|
| Measure | Description | Time Frame |
|---|---|---|
| Primary pharmacokinetic parameters: AUC0-t, AUC0-inf and Cmax | 120 hours after administration of study drug in each session |
| Measure | Description | Time Frame |
|---|---|---|
| Secondary pharmacokinetic parameters:Tmax, t1/2, CL/F, V/F and λz | 120 hours after administration of study drug in each session | |
| Urine pharmacokinetic parameters: Urine Ae% | 120 hours after administration of study drug in each session |
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Inclusion Criteria at Screening
(1)At least 1 year post menopausal, or (2)Surgically sterile, or (3)Willing to use a double-barrier method (intrauterine device [IUD] plus condom, spermicidal gel plus condom) of contraception from screening until 30 days after the last dose of study drug; 5.Males must be willing to use a reliable form of contraception (use of a condom or a partner fulfilling the above criteria) from screening until 30 days after the last dose of study drug 6.Willing to abstain from caffeine- or xanthine-containing beverages (including coffee and tea), alcohol, grapefruit juice, and Seville oranges during the stay-on-site period 7.Willing and able to provide written informed consent
Exclusion Criteria at Screening
Exclusion Criteria at the First Admission
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| Name | Affiliation | Role |
|---|---|---|
| Nicole Sims, DO | WCCT | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| WCCT | Cypress | California | 90630 | United States |
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| TG-2349 as a new capsule formulation | Drug | single oral dose under fed condition |
|
| Stool pharmacokinetic parameters: Stool Ae% | 120 hours after administration of study drug in each session |
| Safety parameters: Incidence and severity of AEs, changes from baseline in safety laboratory values, 12-lead ECG parameters, vital signs, and physical examination. | approximately 7 weeks |
| ID | Term |
|---|---|
| D004304 | Dosage Forms |
| ID | Term |
|---|---|
| D004364 | Pharmaceutical Preparations |
| D013678 | Technology, Pharmaceutical |
| D008919 | Investigative Techniques |
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