Relative bioavailability and food effect of the galectin-3 inhibitor selvigaltin (GB1211) administered as a tablet in healthy participants (GALBA-1)

Relative bioavailability and food effect of the galectin-3 inhibitor selvigaltin (GB1211) administered as a tablet in healthy participants (GALBA-1)

Purpose Overexpression of galectin-3, a β-galactoside-binding lectin, is associated with fibrotic diseases and cancer. Selvigaltin is an oral galectin-3 inhibitor, previously administered as a 50 mg capsule. This study aimed to evaluate the relative bioavailability and food effect of selvigaltin as...

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Published in:Cancer chemotherapy and pharmacology Vol. 94; no. 5; pp. 707 - 720
Main Authors: Aslanis, Vassilios, Abd-Elaziz, Khalid, Slack, Robert J., Brinch, Anne, Gravelle, Lise, Morley, Wayne, Phung, De, Herman, Kimberly, Holyer, Ian, Poulsen, Karen Killerup, Dogterom, Peter, Tantawi, Susan, Zetterberg, Fredrik R., Jacoby, Brian, Schambye, Hans, Lindmark, Bertil
Format: Journal Article
Language:English
Published: Berlin/Heidelberg Springer Berlin Heidelberg 01-11-2024
Springer Nature B.V
Subjects:
Adverse events
Bioavailability
Cancer Research
Food
Galectin-3
Medicine
Medicine & Public Health
NCT
NCT05747573
Oncology
Original Article
Pharmacokinetics
Pharmacology/Toxicology
Selvigaltin
Tablet formulation
Food effect
Bioavailability
Galectin-3
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Summary:Purpose Overexpression of galectin-3, a β-galactoside-binding lectin, is associated with fibrotic diseases and cancer. Selvigaltin is an oral galectin-3 inhibitor, previously administered as a 50 mg capsule. This study aimed to evaluate the relative bioavailability and food effect of selvigaltin as a 100 mg tablet in healthy volunteers. Methods In this single-dose, randomized, three-period, crossover study (GALBA-1; NCT05747573), participants received selvigaltin as a 100 mg tablet (under fasted and fed conditions) or as two 50 mg capsules (under fasted conditions). Primary endpoints included plasma and urine pharmacokinetic (PK) parameters. Secondary endpoints were safety and tolerability. Results Of the 13 enrolled participants, 12 completed the study. Under fasted conditions, geometric mean maximum observed plasma concentration (C max ) and systemic exposure (AUC 0─inf ) of selvigaltin were 161.0% and 84.0% higher, respectively, after administration of a tablet vs. capsules. Under fed vs. fasted conditions, geometric mean C max of the selvigaltin tablet was 20.0% lower, whereas AUC 0─inf was unaffected. Geometric mean percentage of total dose of selvigaltin excreted in urine over 0─96 h was 30.3% and 35.9% for the tablet under fasted and fed conditions, respectively, and 14.5% for the capsules. No treatment-emergent severe or serious adverse events or study discontinuations due to a treatment-emergent adverse event were reported. Conclusion The tablet formulation of selvigaltin displayed higher bioavailability vs. the capsule formulation, with minimal effect of food on PK. Selvigaltin was well-tolerated during all treatments. These findings warrant further clinical development of the tablet formulation of selvigaltin without specific food restrictions. Clinical trial registration NCT05747573; February 28, 2023.
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ISSN:0344-5704
1432-0843
1432-0843
DOI:10.1007/s00280-024-04710-3