A Phase 1, Partially-Blinded, Placebo-Controlled, Randomized, Single Ascending Dose (SAD) With a Food Effect Cohort Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of TBI-223 in Healthy Adult Participants.
| Registry | NCT03758612 |
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| Status | Completed |
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| Phase | Phase 1 |
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| Study type | Interventional; randomized, parallel, masking: triple, treatment |
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| Enrollment | 86 (Actual) |
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| Sponsor | Global Alliance for TB Drug Development (Other) |
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| Conditions | Tuberculosis, Tuberculosis, Pulmonary |
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| Interventions | TBI-223 oral suspension, TBI-223 enteric capsule, TBI-223 SR Tablet Prototype 1, TBI-223 SR Tablet Prototype 2, TBI-223 SR Tablet Prototype 3, TBI-223 IR Tablet, Placebo suspension (Drug) |
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| Dates | start 2019-01-16, primary completion 2020-03-15, completion 2020-03-15, first posted 2018-11-29, last updated 2024-12-09 |
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| Locations | 1 site in United States |
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-Summary
Partially-Blinded, Placebo-Controlled, Randomized, Single Ascending Dose (SAD) with a Food Effect Cohort to Evaluate the Safety, Tolerability, and Pharmacokinetics of TBI-223 in Healthy Adults.
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+Detailed description
This study was a partially-blinded, placebo-controlled, randomized SAD study conducted at one study center. The primary objective of the study was to evaluate the safety and tolerability of single doses of TBI-223 oral suspension, TBI-223 oral enteric capsules, and TBI-223 tablet formulations in healthy adult subjects. The secondary objectives of the study were to determine the PK of TBI-223 and its metabolite M2 after single doses of TBI-223 oral suspension, TBI-223 oral enteric capsules, and TBI-223 tablet formulations in healthy adult subjects, and to compare the rate and extent of absorption of a single dose of TBI-223 oral suspension and TBI-223 tablet formulations when administered in healthy adult subjects either after a high-calorie, high-fat meal or in the fasting state.
Safety was assessed throughout the study for all subjects. Safety assessments included physical examinations, vital signs, serial ECGs, cardiac monitoring, adverse events (AEs), and clinical laboratory tests (including hematology, serum chemistry, coagulation, and urinalysis).
+Arms and interventions
| Arm | Type | Interventions | Description |
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| TBI-223 50 mg | Active comparator | Drug: TBI-223 oral suspension | Cohort 1, single dose of TBI-223 50 mg dosed under fasted conditions |
| TBI-223 100 mg | Active comparator | Drug: TBI-223 oral suspension | Cohort 2, single dose of TBI-223 100 mg dosed under fasted conditions |
| TBI-223 300 mg | Active comparator | Drug: TBI-223 oral suspension; Drug: TBI-223 enteric capsule | Cohort 3a, Period 1 - gave a single dose of TBI-223 300 mg oral suspension dosed under fasted conditions.
Cohort 3b, Period 2 - participants in cohort 3a were invited after a washout period to return for an additional single dose of TBI-223 300 mg enteric capsule dosed under fasted conditions |
| TBI-223 600 mg | Active comparator | Drug: TBI-223 oral suspension | Cohort 4, single dose of TBI-223 600 mg dosed under fasted conditions |
| TBI-223 1200 mg | Active comparator | Drug: TBI-223 oral suspension | Cohort 5, Period 1, single dose of TBI-223 1200 mg dosed under fasted conditions.
Cohort 5, Period 2, participants were invited to return after a washout period to continue in period 2 and receive a single dose of TBI-223 1200 mg dosed under fed conditions |
| TBI-223 2000 mg | Active comparator | Drug: TBI-223 oral suspension | Cohort 6, single dose of TBI-223 2000 mg dosed under fasted conditions |
| TBI-223 2600 mg | Active comparator | Drug: TBI-223 oral suspension | Cohort 7, single dose of TBI-223 2600 mg dosed under fasted conditions |
| TBI-223 placebo | Placebo comparator | Drug: Placebo suspension | Period 1 Single dose matching placebo for TBI-223 under fasted conditions for cohorts 1 to 7
Period 2 Placebo participants in cohort 5 were invited to return after a washout period and were administered a single dose matching placebo for TBI-223 1200mg under fed conditions |
| TBI-223 3x600 mg SR-1 tablet | Active comparator | Drug: TBI-223 SR Tablet Prototype 1 | Cohort 8, arm 1 - Single dose TBI-223 of 1800 mg (3 x 600 mg) sustained release (SR) tablet formulation 1 under fed conditions |
| TBI-223 3x600 mg SR-2 tablet | Active comparator | Drug: TBI-223 SR Tablet Prototype 2 | Cohort 8, arm 2 - Single dose TBI-223 of 1800 mg (3 x 600 mg) sustained release (SR) tablet formulation 2 under fed conditions |
| TBI-223 2x900 mg SR-3 tablet | Active comparator | Drug: TBI-223 SR Tablet Prototype 3 | Cohort 8, arm 3 - Single dose TBI-223 of 1800 mg (2 x 900 mg) sustained release (SR) tablet formulation 3 under fed conditions |
| TBI-223 2x1000 mg IR tablet | Active comparator | Drug: TBI-223 IR Tablet | Cohort 8, arm 4 - Single dose TBI-223 of 2000 mg (2 x 1000 mg) immediate release (IR) tablet under fasted conditions
Cohort 9 - Participants from cohort 8 arm 4 were invited to return and were administered a single dose TBI-223 of 2000 mg (2 x 1000 mg) immediate release (IR) tablet under fed conditions |
- TBI-223 oral suspension (Drug): TBI-223 oral suspension, orally administered.
- TBI-223 enteric capsule (Drug): TBI-223 enteric capsules filled with 150 mg of TBI-223 powder, orally administered.
- TBI-223 SR Tablet Prototype 1 (Drug): TBI-223 600 mg sustained-release (SR) tablet Prototype 1, orally administered.
- TBI-223 SR Tablet Prototype 2 (Drug): TBI-223 600 mg SR tablet Prototype 2, orally administered.
- TBI-223 SR Tablet Prototype 3 (Drug): TBI-223 900 mg SR tablet Prototype 3, orally administered.
- TBI-223 IR Tablet (Drug): TBI-223 1000 mg immediate release (IR) tablet, orally administered
- Placebo suspension (Drug): Placebo for TBI-223 oral Suspension; orally administered.
+Outcome measures
Primary outcomes
- Number of Participants With Treatment-related Adverse Events [Day 1 - Day 11]: A treatment-related adverse event (AE) is defined for this study as any AE classified as possibly, probably or certainly related to the study drug. Adverse events (AEs) for participants who received at least one dose of study treatment were collected from the signing of informed consent till the end of study visit. An Investigator reviewed each AE collected and assessed its relationship to drug treatment based on all available information at the time of the completion of the study.
Secondary outcomes
- Area Under the Plasma Concentration-time- Curve From the Time of Dosing Extrapolated to Infinity (AUC0-inf) [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: AUC0-inf will be calculated from plasma concentrations of TBI-223 AND M2 and calculated as AUC0-inf = AUC0-t + Clast/λz, where λz is the apparent terminal elimination rate constant calculated by linear regression of the terminal linear portion of the log concentration versus time curve
- AUC0-t [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: AUC0-t will be calculated from plasma concentrations of TBI-223. Area under the plasma concentration-time curve from time-zero to the time of the last quantifiable concentration (Clast), as calculated by the linear trapezoidal rule.
- Maximum Plasma Concentration, Determined Directly From Individual Concentration-time- Data (Cmax) [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Cmax will be calculated from plasma concentrations of TBI-223. Cmax is calculated as the maximum plasma concentration, determined directly from individual concentration-time- data
- Time of the Maximum Plasma Concentrations (Tmax) [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Tmax will be calculated from plasma concentrations of TBI-223.
- The Observed Terminal Elimination Half-life (t1/2) [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: T1/2 will be calculated from plasma concentrations of TBI-223 and calculated as T½ = ln(2)/λz
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 300 mg TBI-223 in Capsule to Oral Suspension Formulations [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Geometric mean ratio of TBI-223 area under the (plasma concentration vs. time) curve and Cmax when administered as a Single 300 mg Dose of TBI-223 Capsule Formulation (Cohort 3 Repeat; Part 1; Test) and a Single 300 mg Dose of TBI-223 Oral Suspension (Cohort 3; Part 1; Reference).
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 1200 mg Oral Suspension Under Fasted to Fed Conditions [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Geometric mean ratio of TBI-223 area under the (plasma concentration vs. time) curve and Cmax when administered as a Single 1200 mg Dose of TBI-223 Oral Suspension under Fed (Test) and Fasted (Reference) Conditions (Part 1; Cohort 5)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 2000 mg of Immediate Release (IR) Tablets Under Fed to Fasted Conditions. [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Geometric mean ratio of TBI-223 area under the (plasma concentration vs. time) curve and Cmax when administered as IR tablets, 2000 mg (2 x 1000 mg TBI-223 tablets) under Fed Conditions (Cohort 9; Test) and IR tablets, 2000 mg (2 x1000 mg TBI-223 tablets) under Fasted Conditions (Cohort 8; Reference)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of TBI-223 1800 mg Sustained Release (SR) Tablets Under Fed Conditions to 2000 mg IR Tablets Under Fasted Conditions [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Geometric mean ratio of TBI-223 area under the (plasma concentration vs. time) curve and Cmax when administered as SR (Prototypes 1, 2, and 3) under Fed Conditions (Cohort 8; Test) and IR, 2000 mg (2 x 1000 mg TBI-223 tablets) under Fasted Conditions (Cohort 8; Reference)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 1800 mg SR Tablets (Prototypes 1, 2, 3,) to 2000 mg IR Tablets Under Fed Conditions [predose (0 hour) and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, 24, 30, 36, 42, 48, and 72 hours after administration of the investigational product]: Geometric mean ratio of TBI-223 area under the (plasma concentration vs. time) curve and Cmax when administered as TBI-223 after 1800 mg SR tablets (Prototypes 1, 2, 3,) under Fed Conditions (Cohort 8; Test) and 2000 mg IR tablets (2 x 1000 mg TBI-223 tablets) under Fed Conditions (Cohort 8; Reference)
+Eligibility
Sex: All, ages: 19 Years to 50 Years, accepts healthy volunteers
Key Inclusion Criteria:
All volunteers must satisfy the following criteria to be considered for study participation:
1. Is a healthy adult male or female, 19 to 50 years of age (inclusive) at the time of screening.
2. Has a body mass index (BMI) ≥18.5 and ≤32.0 (kg/m2) and a body weight of no less than 50.0 kg.
3. Is medically healthy with no clinically significant screening results (e.g., laboratory profiles normal or up to Grade 1 per Division of Microbiology and Infectious Diseases Toxicity Tables), as deemed by the Investigator.
4. Has not used tobacco- or nicotine-containing products (including smoking cessation products), for a minimum of 6 months before dosing.
5. If assigned to receive study drug under fed conditions, is willing and able to consume the entire high-calorie, high-fat breakfast meal in the timeframe required.
Key Exclusion Criteria:
1. History or presence of clinically significant cardiovascular (heart murmur), pulmonary, hepatic, renal, hematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, psychiatric disease or any other condition that, in the opinion of the Investigator, would jeopardize the safety of the subject or the validity of the study results.
2. Any presence of musculoskeletal toxicity (severe tenderness with marked impairment of activity, or frank necrosis).
3. Has a positive test for hepatitis B surface antigen, hepatitis C antibody, or HIV at screening.
4. QTcF interval >450 msec for males or >470 msec for females at screening, Day -1, or Day 1 (predose), or history of prolonged QT syndrome. For the triplicate 12-lead ECGs taken at screening and on Day -1, the average QTcF interval of the three 12-lead ECG recordings were used to determine qualification.
5. Family history of long-QT syndrome or sudden death without a preceding diagnosis of a condition that was causative of sudden death (such as known coronary artery disease, congestive heart failure, or terminal cancer).
6. History of any of the following:
* Serotonin syndrome
* Seizures or seizure disorders, other than childhood febrile seizures
* Brain surgery
* History of head injury in the last 5 years
* Any serious disorder of the nervous system particularly one that lowered the seizure threshold.
7. Lactose intolerant.
8. History of sensitivity or contraindication to use of linezolid, tedizolid, or any study investigational products
+Posted results
Participant flow
| Milestone | TBI-223 50 mg | TBI-223 100 mg | TBI-223 300 mg | TBI-223 600 mg | TBI-223 1200 mg | TBI-223 2000 mg | TBI-223 2600 mg | TBI-223 Placebo | TBI-223 3x600 mg SR-1 Tablet | TBI-223 3x600 mg SR-2 Tablet | TBI-223 2x900 mg SR-3 Tablet | TBI-223 2x1000 mg IR Tablet |
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| Started | 6 | 6 | 6 | 6 | 8 | 6 | 8 | 14 | 6 | 6 | 6 | 6 |
| Completed | 6 | 6 | 6 | 6 | 8 | 6 | 8 | 14 | 6 | 6 | 6 | 6 |
| Not completed | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Outcome results
- Number of Participants With Treatment-related Adverse Events (Primary), Count of participants, Participants: TBI-223 Placebo 0; TBI-223 50 mg 1; TBI-223 100 mg 1; TBI-223 300 mg Oral Suspension 0; TBI-223 300 mg Oral Enteric Capsules 0; TBI-223 600 mg 0; TBI-223 1200 mg Fasted 0; TBI-223 1200 mg Fed 1; TBI-223 2000 mg 2; TBI-223 2600 mg 3; TBI-223 3x600 mg SR-1 Tablet 1; TBI-223 3x600 mg SR-2 Tablet 0; TBI-223 2x900 mg SR-3 Tablet 0; TBI-223 2x1000 mg IR Tablet Fasted 3; TBI-223 2x1000 mg IR Tablet Fed 2
- Area Under the Plasma Concentration-time- Curve From the Time of Dosing Extrapolated to Infinity (AUC0-inf) (Secondary), Mean, h*ng/mL: TBI-223 50 mg 1640 +/- 344; TBI-223 100 mg 2730 +/- 628; TBI-223 300 mg Oral Suspension 10700 +/- 2100; TBI-223 300 mg Oral Enteric Capsules 8690 +/- 1690; TBI-223 600 mg 25500 +/- 9580; TBI-223 1200 mg Fasted 45000 +/- 13800; TBI-223 1200 mg Fed 47700 +/- 14300; TBI-223 2000 mg 107000 +/- 17800; TBI-223 2600 mg 127000 +/- 37800; TBI-223 3x600 mg SR-1 Tablet 71300 +/- 18800; TBI-223 3x600 mg SR-2 Tablet 69500 +/- 16000; TBI-223 2x900 mg SR-3 Tablet 82600 +/- 19400; TBI-223 2x1000 mg IR Tablet Fasted 86400 +/- 21200; TBI-223 2x1000 mg IR Tablet Fed 100000 +/- 27300
- AUC0-t (Secondary), Mean, h*ng/mL: TBI-223 50 mg 1620 +/- 343; TBI-223 100 mg 2730 +/- 631; TBI-223 300 mg Oral Suspension 10700 +/- 2090; TBI-223 300 mg Oral Enteric Capsules 8640 +/- 1690; TBI-223 600 mg 25500 +/- 9560; TBI-223 1200 mg Fasted 45900 +/- 13000; TBI-223 1200 mg Fed 47600 +/- 14300; TBI-223 2000 mg 107000 +/- 17800; TBI-223 2600 mg 127000 +/- 37700; TBI-223 3x600 mg SR-1 Tablet 71000 +/- 18900; TBI-223 3x600 mg SR-2 Tablet 69400 +/- 16000; TBI-223 2x900 mg SR-3 Tablet 82600 +/- 19400; TBI-223 2x1000 mg IR Tablet Fasted 86300 +/- 21200; TBI-223 2x1000 mg IR Tablet Fed 100000 +/- 27300
- Maximum Plasma Concentration, Determined Directly From Individual Concentration-time- Data (Cmax) (Secondary), Mean, ng/mL: TBI-223 50 mg 506 +/- 156; TBI-223 100 mg 811 +/- 201; TBI-223 300 mg Oral Suspension 3090 +/- 664; TBI-223 300 mg Oral Enteric Capsules 1360 +/- 610; TBI-223 600 mg 5800 +/- 2400; TBI-223 1200 mg Fasted 8530 +/- 1030; TBI-223 1200 mg Fed 9150 +/- 2740; TBI-223 2000 mg 14800 +/- 2650; TBI-223 2600 mg 16200 +/- 4640; TBI-223 3x600 mg SR-1 Tablet 7040 +/- 2010; TBI-223 3x600 mg SR-2 Tablet 9580 +/- 3390; TBI-223 2x900 mg SR-3 Tablet 8490 +/- 1670; TBI-223 2x1000 mg IR Tablet Fasted 12800 +/- 2320; TBI-223 2x1000 mg IR Tablet Fed 19700 +/- 5640
- Time of the Maximum Plasma Concentrations (Tmax) (Secondary), Median, hours: TBI-223 50 mg 1.0 (0.500 to 1.00); TBI-223 100 mg 1.50 (1.00 to 2.00); TBI-223 300 mg Oral Suspension 1.37 (1.00 to 1.53); TBI-223 300 mg Oral Enteric Capsules 5.00 (3.00 to 16.0); TBI-223 600 mg 1.75 (1.00 to 4.00); TBI-223 1200 mg Fasted 1.50 (1.00 to 3.02); TBI-223 1200 mg Fed 1.50 (0.500 to 3.00); TBI-223 2000 mg 1.52 (1.00 to 3.05); TBI-223 2600 mg 2.25 (1.50 to 5.00); TBI-223 3x600 mg SR-1 Tablet 7.00 (6.00 to 16.0); TBI-223 3x600 mg SR-2 Tablet 6.50 (4.00 to 8.00); TBI-223 2x900 mg SR-3 Tablet 7.50 (5.00 to 20.0); TBI-223 2x1000 mg IR Tablet Fasted 2.00 (1.00 to 3.00); TBI-223 2x1000 mg IR Tablet Fed 3.00 (1.00 to 4.00)
- The Observed Terminal Elimination Half-life (t1/2) (Secondary), Mean, hours: TBI-223 50 mg 2.19 +/- 0.239; TBI-223 100 mg 1.96 +/- 0.165; TBI-223 300 mg Oral Suspension 1.94 +/- 0.238; TBI-223 300 mg Oral Enteric Capsules 3.43 +/- 1.02; TBI-223 600 mg 2.63 +/- 0.693; TBI-223 1200 mg Fasted 2.93 +/- 0.706; TBI-223 1200 mg Fed 2.32 +/- 0.158; TBI-223 2000 mg 3.81 +/- 0.870; TBI-223 2600 mg 2.93 +/- 0.534; TBI-223 3x600 mg SR-1 Tablet 3.70 +/- 0.271; TBI-223 3x600 mg SR-2 Tablet 2.32 +/- 0.581; TBI-223 2x900 mg SR-3 Tablet 3.08 +/- 0.784; TBI-223 2x1000 mg IR Tablet Fasted 2.80 +/- 0.604; TBI-223 2x1000 mg IR Tablet Fed 2.38 +/- 0.101
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 300 mg TBI-223 in Capsule to Oral Suspension Formulations (Secondary), Geometric mean, ratio (%): TBI-223 Ratio (%) 42.46 (31.57 to 57.10)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 1200 mg Oral Suspension Under Fasted to Fed Conditions (Secondary), Geometric mean, ratio (%): TBI-223 Ratio (%) 103.34 (87.00 to 122.75)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 2000 mg of Immediate Release (IR) Tablets Under Fed to Fasted Conditions. (Secondary), Geometric mean, ratio (%): TBI-223 Ratio (%) 151.24 (127.91 to 178.82)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of TBI-223 1800 mg Sustained Release (SR) Tablets Under Fed Conditions to 2000 mg IR Tablets Under Fasted Conditions (Secondary), Geometric mean, ratio (%): TBI-223 Ratio (%), SR-1 Fed vs IR Fasted 53.53 (40.10 to 71.45); TBI-223 Ratio (%), SR-2 Fed vs IR Fasted 71.70 (53.71 to 95.71); TBI-223 Ratio (%), SR-3 Fed vs IR Fasted 66.31 (49.67 to 88.53)
- Geometric Mean Ratio and 90% Confidence Interval (CI) of Cmax, AUC0-t and AUC 0-inf of 1800 mg SR Tablets (Prototypes 1, 2, 3,) to 2000 mg IR Tablets Under Fed Conditions (Secondary), Geometric mean, ratio (%): TBI-223 Ratio (%), SR-1 Fed vs IR Fed 35.39 (26.04 to 48.10); TBI-223 Ratio (%), SR-2 Fed vs IR Fed 47.41 (34.88 to 64.43); TBI-223 Ratio (%), SR-3 Fed vs IR Fed 43.85 (32.26 to 59.59)
Adverse events
Time frame: Day 1 - Day 11
| Arm | Deaths | Serious adverse events | Other adverse events |
|---|
| TBI-223 Placebo | 0/14 (0.0%) | 0/14 (0.0%) | 4/14 (28.6%) |
| TBI-223 50 mg | 0/6 (0.0%) | 0/6 (0.0%) | 1/6 (16.7%) |
| TBI-223 100 mg | 0/6 (0.0%) | 0/6 (0.0%) | 2/6 (33.3%) |
| TBI-223 300 mg Oral Suspension | 0/6 (0.0%) | 0/6 (0.0%) | 1/6 (16.7%) |
| TBI-223 300 mg Oral Enteric Capsules | 0/6 (0.0%) | 0/6 (0.0%) | 0/6 (0.0%) |
| TBI-223 600 mg | 0/6 (0.0%) | 0/6 (0.0%) | 0/6 (0.0%) |
| TBI-223 1200 mg Fasted | 0/8 (0.0%) | 0/8 (0.0%) | 0/8 (0.0%) |
| TBI-223 1200 mg Fed | 0/7 (0.0%) | 0/7 (0.0%) | 1/7 (14.3%) |
| TBI-223 2000 mg | 0/6 (0.0%) | 0/6 (0.0%) | 3/6 (50.0%) |
| TBI-223 2600 mg | 0/8 (0.0%) | 0/8 (0.0%) | 3/8 (37.5%) |
| TBI-223 3x600 mg SR-1 Tablet | 0/6 (0.0%) | 0/6 (0.0%) | 1/6 (16.7%) |
| TBI-223 3x600 mg SR-2 Tablet | 0/6 (0.0%) | 0/6 (0.0%) | 2/6 (33.3%) |
| TBI-223 2x900 mg SR-3 Tablet | 0/6 (0.0%) | 0/6 (0.0%) | 2/6 (33.3%) |
| TBI-223 2x1000 mg IR Tablet Fasted | 0/6 (0.0%) | 0/6 (0.0%) | 3/6 (50.0%) |
| TBI-223 2x1000 mg IR Tablet Fed | 0/6 (0.0%) | 0/6 (0.0%) | 2/6 (33.3%) |
Other adverse events by term
| Term | Organ system | TBI-223 Placebo | TBI-223 50 mg | TBI-223 100 mg | TBI-223 300 mg Oral Suspension | TBI-223 300 mg Oral Enteric Capsules | TBI-223 600 mg | TBI-223 1200 mg Fasted | TBI-223 1200 mg Fed | TBI-223 2000 mg | TBI-223 2600 mg | TBI-223 3x600 mg SR-1 Tablet | TBI-223 3x600 mg SR-2 Tablet | TBI-223 2x900 mg SR-3 Tablet | TBI-223 2x1000 mg IR Tablet Fasted | TBI-223 2x1000 mg IR Tablet Fed |
|---|
| Nausea | Gastrointestinal disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 2/6 | 3/8 | 0/6 | 0/6 | 0/6 | 1/6 | 0/6 |
| Vomiting | Gastrointestinal disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 2/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Dizziness | Nervous system disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 1/7 | 1/6 | 2/8 | 0/6 | 0/6 | 0/6 | 2/6 | 1/6 |
| Headache | Nervous system disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 1/8 | 1/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Tachycardia | Cardiac disorders | 0/14 | 0/6 | 1/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 1/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Energy Increased | General disorders | 0/14 | 0/6 | 1/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Medical device site reaction | General disorders | 0/14 | 0/6 | 1/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Skin discolouration | Skin and subcutaneous tissue disorders | 1/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Urticaria | Skin and subcutaneous tissue disorders | 0/14 | 1/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Hypotension | Vascular disorders | 1/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Neutropenia | Blood and lymphatic system disorders | 1/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Hypersensitivity | Immune system disorders | 1/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Blood bilirubin increased | Investigations | 0/14 | 0/6 | 0/6 | 1/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Back pain | Musculoskeletal and connective tissue disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 1/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 |
| Vessel puncture site inflammation | General disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 2/6 | 0/6 | 1/6 | 0/6 |
| Chest discomfort | General disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 1/6 | 0/6 |
| Vessel puncture site pain | General disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 1/6 | 0/6 | 0/6 |
| Vessel puncture site reaction | General disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 1/6 | 0/6 | 0/6 |
| Vessel puncture site swelling | General disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 1/6 | 0/6 | 0/6 |
| Disturbance in attention | Nervous system disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 1/6 | 0/6 |
| Abdominal Pain | Gastrointestinal disorders | 0/14 | 0/6 | 0/6 | 0/6 | 0/6 | 0/6 | 0/8 | 0/7 | 0/6 | 0/8 | 0/6 | 0/6 | 0/6 | 0/6 | 1/6 |
+Locations (1)
| Facility | City | Country | Status |
|---|
| Worldwide Clinical Trials (WCT) | San Antonio, Texas | United States | |
+Publications
- Results publication: Lombardi A, Pappas F, Bruinenberg P, Nedelman J, Taneja R, Hickman D, Beumont M, Sun E. Pharmacokinetics, tolerability, and safety of TBI-223, a novel oxazolidinone, in healthy participants. Antimicrob Agents Chemother. 2025 Apr 2;69(4):e0154224. doi: 10.1128/aac.01542-24. Epub 2025 Mar 11. PMID 40067046
+Study documents
+Investigators