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Safety and pharmaco...
Safety and pharmacokinetics of GB1211, an oral galectin-3 inhibitor : a single- and multiple-dose first-in-human study in healthy participants
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- Aslanis, Vassilios (författare)
- Galecto Biotech ApS, Denmark
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- Slack, Robert J. (författare)
- Galecto Biotech ApS, Denmark
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- MacKinnon, Alison C. (författare)
- Galecto Biotech ApS, Denmark
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- McClinton, Catherine (författare)
- Galecto Biotech ApS, Denmark
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- Tantawi, Susan (författare)
- Galecto Biotech ApS, Denmark
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- Gravelle, Lise (författare)
- Galecto Biotech ApS, Denmark
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- Nilsson, Ulf J. (författare)
- Lund University,Lunds universitet,Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Leffler, Hakon (författare)
- Lund University,Lunds universitet,Avdelningen för mikrobiologi, immunologi och glykobiologi - MIG,Institutionen för laboratoriemedicin,Medicinska fakulteten,LUCC: Lunds universitets cancercentrum,Övriga starka forskningsmiljöer,Division of Microbiology, Immunology and Glycobiology - MIG,Department of Laboratory Medicine,Faculty of Medicine,LUCC: Lund University Cancer Centre,Other Strong Research Environments
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- Brooks, Ashley (författare)
- Covance Clinical Research Unit Ltd.
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- Khindri, Sanjeev K. (författare)
- Galecto Biotech ApS, Denmark
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- Marshall, Richard P. (författare)
- Galecto Biotech ApS, Denmark
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- Pedersen, Anders (författare)
- Galecto Biotech ApS, Denmark
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- Schambye, Hans (författare)
- Galecto Biotech ApS, Denmark
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- Zetterberg, Fredrik (författare)
- Galecto Biotech ApS, Denmark
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(creator_code:org_t)
- 2023-03-13
- 2023
- Engelska 14 s.
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Ingår i: Cancer Chemotherapy and Pharmacology. - : Springer Science and Business Media LLC. - 0344-5704 .- 1432-0843. ; 91:3, s. 267-280
- Relaterad länk:
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http://dx.doi.org/10... (free)
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https://lup.lub.lu.s...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 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 ClinicalTrials.gov (identifier: NCT03809052).
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- Humans
- Administration, Oral
- Area Under Curve
- Dose-Response Relationship, Drug
- Double-Blind Method
- Galectin 3/antagonists & inhibitors
- Healthy Volunteers
Publikations- och innehållstyp
- art (ämneskategori)
- ref (ämneskategori)
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Aslanis, Vassili ...
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Slack, Robert J.
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MacKinnon, Aliso ...
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McClinton, Cathe ...
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Tantawi, Susan
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Gravelle, Lise
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visa fler...
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Nilsson, Ulf J.
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Leffler, Hakon
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Brooks, Ashley
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Khindri, Sanjeev ...
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Marshall, Richar ...
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Pedersen, Anders
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Schambye, Hans
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Zetterberg, Fred ...
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