Safety and pharmacokinetics of GB1211, an oral galectin-3 inhibitor: a single- and multiple-dose first-in-human study in healthy participants

Vassilios Aslanis, Robert J. Slack, Alison C. MacKinnon, Catherine McClinton, Susan Tantawi, Lise Gravelle, Ulf J. Nilsson, Hakon Leffler, Ashley Brooks, Sanjeev K. Khindri, Richard P. Marshall, Anders Pedersen, Hans Schambye, Fredrik Zetterberg

Research output: Contribution to journalArticlepeer-review


PURPOSE: Galectin-3, a β-galactoside-binding lectin, plays a key role in several cellular pathways involved in chronic inflammation, heart disease and cancer. GB1211 is an orally bioavailable galectin-3 inhibitor, developed to be systemically active. We report safety and pharmacokinetics (PK) of GB1211 in healthy participants.

METHODS: This phase 1, double-blind, placebo-controlled, first-in-human study (NCT03809052) included a single ascending-dose phase (with a food-effect cohort) where participants across seven sequential cohorts were randomized 3:1 to receive oral GB1211 (5, 20, 50, 100, 200 or 400 mg) or placebo. In the multiple ascending-dose phase, participants received 50 or 100 mg GB1211 or placebo twice daily for 10 days. All doses were administered in the fasted state except in the food-effect cohort where doses were given 30 min after a high-fat meal.

RESULTS: All 78 participants received at least one GB1211 dose (n = 58) or placebo (n = 20) and completed the study. No safety concerns were identified. Following single and multiple oral doses under fasted conditions, maximum GB1211 plasma concentrations were reached at 1.75-4 h (median) post-dose; mean half-life was 11-16 h. There was a ~ twofold GB1211 accumulation in plasma with multiple dosing, with steady-state reached within 3 days; 30% of the administered dose was excreted in urine as unchanged drug. Absorption in the fed state was delayed by 2 h but systemic exposure was unaffected.

CONCLUSION: GB1211 was well tolerated, rapidly absorbed, and displayed favorable PK, indicating a potential to treat multiple disease types. These findings support further clinical development of GB1211.

CLINICAL TRIAL REGISTRATION: The study was registered with (identifier: NCT03809052).

Original languageEnglish
Pages (from-to)267-280
Number of pages14
JournalCancer Chemotherapy and Pharmacology
Issue number3
Publication statusPublished - 2023 Mar

Subject classification (UKÄ)

  • Pharmacology and Toxicology

Free keywords

  • Humans
  • Administration, Oral
  • Area Under Curve
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Galectin 3/antagonists & inhibitors
  • Healthy Volunteers


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