A Relative Bioavailability and Food Effect Study of TYRA-300-B01 Capsule and Tablet Formulations in Healthy Adult Participants

A Phase 1, Multi-cohort, Open-label Study 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

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.

Study Overview

• Status: Active, not recruiting
• Conditions: Healthy
• Intervention / Treatment: Drug: TYRA-300-B01

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Estimated): 60
• Phase: Phase 1

Contacts and Locations

Study Locations

• Australia
  • Victoria
    • Melbourne, Victoria, Australia, 3004
      • Nucleus Network

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Males or females of non-childbearing potential, between 18 and 55 years of age
• In good health, determined by no clinically significant findings from medical history, 12-lead electrocardiogram (ECG), vital signs, and clinical laboratory assessments
• Body mass index (BMI) 18 to 32 kg/m^2 (inclusive)
• Cohorts 1 and 2 ethnicity requirements: none
• Cohort 3 ethnicity requirements: first- or second-generation Japanese participants

Exclusion Criteria:

• Significant history of any hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, immunologic, musculoskeletal disease, or allergic disease (as determined by the Investigator)
• Any ocular condition likely to increase the risk of eye toxicity
• Gastrointestinal disorders that will affect oral administration or absorption of TYRA-300-B01
• Females of child-bearing potential and males who plan to father a child while enrolled in this study

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Bioavailability Tablet vs Capsule Formulation; TYRA-300-B01 single oral dose of tablet or capsule crossover followed by twice-daily tablet dosing	Drug: TYRA-300-B01; TYRA-300 is an oral, novel potent FGFR 3-selective tyrosine kinase inhibitor that targets tumors that contain activating gene alterations of FGFR3.
Experimental: Food Effect Tablet Formulation; TYRA-300-B01 single oral dose of tablet in the fed and fasted state	Drug: TYRA-300-B01; TYRA-300 is an oral, novel potent FGFR 3-selective tyrosine kinase inhibitor that targets tumors that contain activating gene alterations of FGFR3.
Experimental: Pharmacokinetic Tablet Formulation; TYRA-300-B01 single oral dose	Drug: TYRA-300-B01; TYRA-300 is an oral, novel potent FGFR 3-selective tyrosine kinase inhibitor that targets tumors that contain activating gene alterations of FGFR3.
Experimental: Pharmacokinetic Mini-Tablet Formulation; TYRA-300-B01 multiple-dose mini-tablet formulation	Drug: TYRA-300-B01; TYRA-300 is an oral, novel potent FGFR 3-selective tyrosine kinase inhibitor that targets tumors that contain activating gene alterations of FGFR3.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	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
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

Secondary Outcome Measures

Outcome Measure	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	Frequency in changes in laboratory parameters and physical signs of toxicity	Initiation of study treatment up to 7-days post treatment

Collaborators and Investigators

• Sponsor: Tyra Biosciences, Inc
• Investigators: Study Chair: Doug Warner, M.D., Tyra Biosciences, Inc

Study record dates

Study Major Dates

• Study Start (Actual): October 16, 2023
• Primary Completion (Estimated): May 1, 2025
• Study Completion (Estimated): July 1, 2025

Study Registration Dates

• First Submitted: August 17, 2023
• First Submitted That Met QC Criteria: August 17, 2023
• First Posted (Actual): August 23, 2023

Study Record Updates

• Last Update Posted (Actual): March 26, 2025
• Last Update Submitted That Met QC Criteria: March 21, 2025
• Last Verified: March 1, 2025

More Information

Terms related to this study

• Other Study ID Numbers: TYR300-102

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No