Galecto Announces First Patient Treated in Phase 2a Trial of the Oral LOXL2 Inhibitor GB2064 in Myelofibrosis (the MYLOX-1 Trial)
The open label MYLOX-1 trial is designed to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of orally administered GB2064 in 16 patients over 9 months. The trial will also assess impact on fibrosis and quantification of the tissue targeting of GB2064, as well as other aspects of clinical response in myelofibrosis.
“We are very pleased to start this Phase 2a trial with GB2064 in myelofibrosis, which marks a further important milestone in the development of Galecto’s exciting clinical pipeline. There is a significant unmet need in myelofibrosis, with very few therapeutic alternatives. Fibrosis in the tumor micro-environment remains unaddressed and LOXL2 inhibition could be disease modifying,” said Dr. Hans Schambye, CEO of
The current standard of care for myelofibrosis is JAK inhibitors, but questions remain regarding side effects caused by the mechanism of action. LOXL-2 is an attractive target, as it is upregulated in myelofibrosis fibrotic tissue and plays a key role in fibrosis and disease progression in the tumor micro-environment. Focused inhibition of LOXL-2 is believed to be inherently safer than pan-inhibition of all LOX enzymes because some of the iso-enzymes potentially carry important liabilities.
Professor Srdan Verstovsek, MD, PhD of the
The MYLOX-1 Trial
The MYLOX-1 trial is an open label trial focusing on safety in patients who are intolerant to or ineligible for JAK1 inhibitor therapy. The trial will include safety measures as per the state of the art MRI for spleen size and bone marrow sampling for measurement of fibrosis and of drug presence.
GB2064 is a pseudo-irreversible inhibitor of the LOXL2 enzyme, which means that high plasma concentrations will cancel the enzyme for a disproportionately longer time than the presence of the drug in plasma. This may mean that the risk of potential side effects due to drug remaining in the system could be avoided. GB2064 has been tested in healthy volunteers without finding dose limiting or dose-related tolerability issues.
LOXL2 is an extracellular enzyme, which carries out cross-linking of collagen and elastin fibrils and thus contributes to building and strengthening of the fibrous matrix that is exaggerated in fibrotic disease.
Myelofibrosis is a blood cancer where the normal bone marrow loses its ability to produce life preserving blood cells like erythrocytes, platelets and white blood cells. The bone marrow is destroyed by fibrotic tissue and hence the name Myelofibrosis (myelo- means marrow). Bone marrow transplantation may be possible, but these patients are older and the risks of non-success is high. Therefore, medicines which can help patients to become transfusion free and live longer are needed.
Certain statements in this press release are forward-looking statements that involve a number of risks and uncertainties. Such forward-looking statements include statements about the planned design of the MYLOX-1 trial, the future myelofibrosis market and Galecto’s focus, plans for clinical development, product candidates and pipeline. The words “may,” “will,” “could,” “would,” “should,” “expect,” “plan,” “anticipate,” “intend,” “believe,” “estimate,” “predict,” “project,” “potential,” “continue,” “target” and similar expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words. For such statements,
For more information, contact:
|Hans Schambye, CEO
|+45 70 70 52 10|
|+1 617 430 7577||+41 78 680 0538|
Source: Galecto, Inc.