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The purpose of this study is to evaluate the relative bioavailability of capsule and tablet formulations of TYRA-300-B01, and to evaluate the safety, tolerability, and food effect of TYRA-300-B01 tablets in healthy adult participants.
This is a Phase 1, multi-cohort trial studying TYRA-300-B01, a novel, potent fibroblast growth factor receptor (FGFR) 3-selective tyrosine kinase inhibitor, in healthy, adult participants. The purpose of this study is to evaluate the relative bioavailability of capsule and tablet formulations of TYRA-300-B01, and to evaluate the safety, tolerability, and food effect of TYRA-300-B01 tablets in healthy adult participants.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Bioavailability Tablet vs Capsule Formulation | Experimental | TYRA-300-B01 single oral dose of tablet or capsule crossover followed by twice-daily tablet dosing |
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| Food Effect Tablet Formulation | Experimental | TYRA-300-B01 single oral dose of tablet in the fed and fasted state |
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| Pharmacokinetic Tablet Formulation | Experimental | TYRA-300-B01 single oral dose |
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| Pharmacokinetic Mini-Tablet Formulation | Experimental | TYRA-300-B01 multiple-dose mini-tablet formulation |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TYRA-300-B01 | Drug | TYRA-300 is an oral, novel potent FGFR 3-selective tyrosine kinase inhibitor that targets tumors that contain activating gene alterations of FGFR3. |
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| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics single-dose Cmax | maximum plasma concentration (Cmax) | Up to 48 hours post-dose |
| Pharmacokinetics multiple-dose Cmax | maximum steady-state plasma concentration (Cmax) | Up to 24 hours post-dose |
| Pharmacokinetics multiple-dose Cmin | average steady-state trough plasma concentration (Cmin) | Up to 24 hours post-dose |
| Pharmacokinetics single dose Tmax | time to reach maximum plasma concentration (Tmax) | Up to 48 hours post-dose |
| Pharmacokinetics single and multiple dose AUC | area under the plasma concentration-time curve (AUC) | Up to 48 hours post-dose |
| Pharmacokinetics single dose CL/F | apparent total clearance (CL/F) | Up to 48 hours post-dose |
| Pharmacokinetics single dose Vz/F | apparent volume of distribution (Vz/F) | Up to 48 hours post-dose |
| Pharmacokinetics single dose t1/2 | half-life of TYRA-300 | Up to 48 hours post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| Safety and tolerability | number of participants with adverse events (AEs), serious adverse events (SAEs), adverse events of special interest (AESIs) as a measure of safety and tolerability | Initiation of study treatment up to 7-days post treatment |
| Safety and tolerability |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Doug Warner, M.D. | Tyra Biosciences, Inc | Study Chair |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Nucleus Network | Melbourne | Victoria | 3004 | Australia |
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| Pharmacokinetics multiple-dose RCmax | accumulation ratio for Cmax (RCmax) | Up to 24 hours post-dose |
| Pharmacokinetics multiple-dose RAUC | accumulation ratio for AUC | Up to 24 hours post-dose |
Frequency in changes in laboratory parameters and physical signs of toxicity |
| Initiation of study treatment up to 7-days post treatment |