Oral presentation at ECCO highlights MORF-057 as a potent, selective and orally available small molecule development candidate
Mechanism of action demonstrated in in vitro and in vivo models
WALTHAM, MA, USA I February 14, 2020 IMorphic Therapeutic (NASDAQ: MORF), a biopharmaceutical company developing a new generation of oral integrin therapies for the treatment of serious chronic diseases, announced an oral presentation today highlighting Morphic’s product candidate MORF-057 at the 15th Congress of the European Crohn’s and Colitis Organisation (ECCO). MORF-057 is in development as an oral inhibitor of the α4β7 integrin, a clinically proven target for the treatment of inflammatory bowel diseases (IBD).
“The approved antibody therapeutic vedolizumab has provided validation of α4β7 as an effective target for the treatment of inflammatory bowel disease. However, a significant opportunity remains to address IBD with an orally administered therapeutic,” commented Bruce Rogers, Ph.D., chief scientific officer of Morphic Therapeutic. “We are highly encouraged that the data presented at ECCO demonstrate MORF-057’s favorable in vitro pharmacodynamic characteristics and these results are reinforced by the positive outcomes in in vivo models using oral administration of MORF-057. These data further strengthen our conviction to move MORF-057 forward into clinical studies as planned.”
MORF-057 was specifically designed to inhibit α4β7-mediated migration of α4β7-expressing lymphocytes to the gut, which is a fundamental contributor to IBD. The data presented at ECCO support MORF-057 as a potent, selective and orally bioavailable small molecule inhibitor of the α4β7 integrin. In the studies presented, MORF-057 showed greater than 41,600-fold selectivity for α4β7 over α4β1.1 High specificity for α4β7 over α4β1 is necessary to avoid inhibiting α4β1, which enables potentially pathological migration of lymphocytes to the central nervous system. Further, the data demonstrate that MORF-057 acts through its intended mechanism of action, by blocking the migration of α4β7-high-expressing lymphocytes. Notably, these results were replicated in both murine and primate models, with MORF-057 activity being equivalent to the murine equivalent of vedolizumab.
Details of the Oral Presentation at ECCO 2020:
Session: Current and novel targets for IBD agents
Title: Discovery of highly selective small molecule oral inhibitors of integrin α4β7 for the treatment of inflammatory bowel diseases
Presenter: Dr. Jamie Wong, Ph.D.
Contributors: Matthew Bursavich, Natalia Blanco, Adam Camblin, Laura Cappellucci, Rhianna Cohen, Dan Cui, Megan Krumpoch, Cheng Zhong, Kristopher Hahn, Dooyoung Lee, Blaise Lippa, Fu-Yang Lin, Alex Lugovskoy, Molly McShea, Siavash Mostafavi, Terence Moy, Andrew Sullivan, Dawn Troast, Liangsu Wang, Bruce Rogers
Presentation number: DOP64
This ECCO presentation will be available on the Morphic website in the Investors section.
About MORF-057
Morphic is developing MORF-057 as a selective, oral small molecule inhibitor of the α4β7 integrin, a target for the treatment of inflammatory bowel diseases (IBD) that has been clinically validated by the success of the approved antibody therapeutic vedolizumab. α4β7 inhibition is intended to block the interactions between α4β7 on the surface of lymphocytes and the gut cell ligand MAdCAM-1, preventing lymphocyte migration from the bloodstream into intestinal mucosal tissues and causing inflammation. Morphic believes an approved oral α4β7 inhibitor has significant potential as a best-in-class medication for some types of IBD, and may offer therapeutic opportunity earlier in disease progression as a way of changing the course of disease for many patients.
About Morphic Therapeutic
Morphic Therapeutic is a biopharmaceutical company developing a new generation of oral integrin therapies for the treatment of serious chronic diseases, including autoimmune, cardiovascular and metabolic diseases, fibrosis and cancer. In collaboration with AbbVie, Janssen and Schrödinger, Morphic is advancing its pipeline and discovery activities using its proprietary MInT technology platform which leverages the Company’s unique understanding of integrin structure and biology. For more information, visit www.morphictx.com.
- ECCO presentation Wong, et al 2/14/20: selectivity was determined by comparing potency against α4β7 and α4β1 in RPMI8866 and Jurkat cell lines, respectively.
SOURCE: Morphic Therapeutic
Post Views: 46
Oral presentation at ECCO highlights MORF-057 as a potent, selective and orally available small molecule development candidate
Mechanism of action demonstrated in in vitro and in vivo models
WALTHAM, MA, USA I February 14, 2020 IMorphic Therapeutic (NASDAQ: MORF), a biopharmaceutical company developing a new generation of oral integrin therapies for the treatment of serious chronic diseases, announced an oral presentation today highlighting Morphic’s product candidate MORF-057 at the 15th Congress of the European Crohn’s and Colitis Organisation (ECCO). MORF-057 is in development as an oral inhibitor of the α4β7 integrin, a clinically proven target for the treatment of inflammatory bowel diseases (IBD).
“The approved antibody therapeutic vedolizumab has provided validation of α4β7 as an effective target for the treatment of inflammatory bowel disease. However, a significant opportunity remains to address IBD with an orally administered therapeutic,” commented Bruce Rogers, Ph.D., chief scientific officer of Morphic Therapeutic. “We are highly encouraged that the data presented at ECCO demonstrate MORF-057’s favorable in vitro pharmacodynamic characteristics and these results are reinforced by the positive outcomes in in vivo models using oral administration of MORF-057. These data further strengthen our conviction to move MORF-057 forward into clinical studies as planned.”
MORF-057 was specifically designed to inhibit α4β7-mediated migration of α4β7-expressing lymphocytes to the gut, which is a fundamental contributor to IBD. The data presented at ECCO support MORF-057 as a potent, selective and orally bioavailable small molecule inhibitor of the α4β7 integrin. In the studies presented, MORF-057 showed greater than 41,600-fold selectivity for α4β7 over α4β1.1 High specificity for α4β7 over α4β1 is necessary to avoid inhibiting α4β1, which enables potentially pathological migration of lymphocytes to the central nervous system. Further, the data demonstrate that MORF-057 acts through its intended mechanism of action, by blocking the migration of α4β7-high-expressing lymphocytes. Notably, these results were replicated in both murine and primate models, with MORF-057 activity being equivalent to the murine equivalent of vedolizumab.
Details of the Oral Presentation at ECCO 2020:
Session: Current and novel targets for IBD agents
Title: Discovery of highly selective small molecule oral inhibitors of integrin α4β7 for the treatment of inflammatory bowel diseases
Presenter: Dr. Jamie Wong, Ph.D.
Contributors: Matthew Bursavich, Natalia Blanco, Adam Camblin, Laura Cappellucci, Rhianna Cohen, Dan Cui, Megan Krumpoch, Cheng Zhong, Kristopher Hahn, Dooyoung Lee, Blaise Lippa, Fu-Yang Lin, Alex Lugovskoy, Molly McShea, Siavash Mostafavi, Terence Moy, Andrew Sullivan, Dawn Troast, Liangsu Wang, Bruce Rogers
Presentation number: DOP64
This ECCO presentation will be available on the Morphic website in the Investors section.
About MORF-057
Morphic is developing MORF-057 as a selective, oral small molecule inhibitor of the α4β7 integrin, a target for the treatment of inflammatory bowel diseases (IBD) that has been clinically validated by the success of the approved antibody therapeutic vedolizumab. α4β7 inhibition is intended to block the interactions between α4β7 on the surface of lymphocytes and the gut cell ligand MAdCAM-1, preventing lymphocyte migration from the bloodstream into intestinal mucosal tissues and causing inflammation. Morphic believes an approved oral α4β7 inhibitor has significant potential as a best-in-class medication for some types of IBD, and may offer therapeutic opportunity earlier in disease progression as a way of changing the course of disease for many patients.
About Morphic Therapeutic
Morphic Therapeutic is a biopharmaceutical company developing a new generation of oral integrin therapies for the treatment of serious chronic diseases, including autoimmune, cardiovascular and metabolic diseases, fibrosis and cancer. In collaboration with AbbVie, Janssen and Schrödinger, Morphic is advancing its pipeline and discovery activities using its proprietary MInT technology platform which leverages the Company’s unique understanding of integrin structure and biology. For more information, visit www.morphictx.com.
- ECCO presentation Wong, et al 2/14/20: selectivity was determined by comparing potency against α4β7 and α4β1 in RPMI8866 and Jurkat cell lines, respectively.
SOURCE: Morphic Therapeutic
Post Views: 46
