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Structures of ferroportin in complex with its specific inhibitor vamifeport.
Lehmann EF, Liziczai M, Drożdżyk K, Altermatt P, Langini C, Manolova V, Sundstrom H, Dürrenberger F, Dutzler R, Manatschal C. Lehmann EF, et al. Elife. 2023 Mar 21;12:e83053. doi: 10.7554/eLife.83053. Elife. 2023. PMID: 36943194 Free PMC article.
Here, we describe the cryo-electron microscopy structures of human FPN in complex with synthetic nanobodies and vamifeport (VIT-2763), the first clinical-stage oral FPN inhibitor. Vamifeport competes with hepcidin for FPN binding and is currently in clinical develop …
Here, we describe the cryo-electron microscopy structures of human FPN in complex with synthetic nanobodies and vamifeport (VIT-27 …
The oral ferroportin inhibitor vamifeport improves hemodynamics in a mouse model of sickle cell disease.
Nyffenegger N, Zennadi R, Kalleda N, Flace A, Ingoglia G, Buzzi RM, Doucerain C, Buehler PW, Schaer DJ, Dürrenberger F, Manolova V. Nyffenegger N, et al. Blood. 2022 Aug 18;140(7):769-781. doi: 10.1182/blood.2021014716. Blood. 2022. PMID: 35714304 Free PMC article.
We hypothesized that iron restriction via blocking ferroportin, the unique iron transporter in mammals, might reduce HbS concentration in RBCs, thereby decreasing hemolysis, improving blood flow, and preventing vaso-occlusive events. Indeed, vamifeport (also known as VIT- …
We hypothesized that iron restriction via blocking ferroportin, the unique iron transporter in mammals, might reduce HbS concentration in RB …
β-Thalassemia: evolving treatment options beyond transfusion and iron chelation.
Langer AL, Esrick EB. Langer AL, et al. Hematology Am Soc Hematol Educ Program. 2021 Dec 10;2021(1):600-606. doi: 10.1182/hematology.2021000313. Hematology Am Soc Hematol Educ Program. 2021. PMID: 34889443 Free PMC article. Review.
Another group of agents seeks to ameliorate ineffective erythropoiesis and improve anemia by targeting abnormal iron metabolism in thalassemia: apotransferrin, VIT-2763 (a ferroportin inhibitor), PTG-300 (a hepcidin mimetic), and an erythroferrone antibody in early …
Another group of agents seeks to ameliorate ineffective erythropoiesis and improve anemia by targeting abnormal iron metabolism in thalassem …
Oral ferroportin inhibitor vamifeport for improving iron homeostasis and erythropoiesis in β-thalassemia: current evidence and future clinical development.
Porter J, Taher A, Viprakasit V, Kattamis A, Coates TD, Garbowski M, Dürrenberger F, Manolova V, Richard F, Cappellini MD. Porter J, et al. Expert Rev Hematol. 2021 Jul;14(7):633-644. doi: 10.1080/17474086.2021.1935854. Epub 2021 Jul 29. Expert Rev Hematol. 2021. PMID: 34324404 Review.
AREAS COVERED: The preclinical and clinical development of vamifeport (VIT-2763), a novel ferroportin inhibitor, was reviewed. PubMed, EMBASE and ClinicalTrials.gov were searched using the search term 'VIT-2763'. ...
AREAS COVERED: The preclinical and clinical development of vamifeport (VIT-2763), a novel ferroportin inhibitor, was reviewed. …
Novel Therapeutic Advances in β-Thalassemia.
Makis A, Voskaridou E, Papassotiriou I, Hatzimichael E. Makis A, et al. Biology (Basel). 2021 Jun 18;10(6):546. doi: 10.3390/biology10060546. Biology (Basel). 2021. PMID: 34207028 Free PMC article. Review.
Another therapeutic approach is to target the dysregulation of iron homeostasis, using, for example, hepcidin agonists (inhibitors of TMPRSS6 and minihepcidins) or ferroportin inhibitors (VIT-2763). This review provides an update on the novel therapeutic options tha …
Another therapeutic approach is to target the dysregulation of iron homeostasis, using, for example, hepcidin agonists (inhibitors of TMPRSS …
The Oral Ferroportin Inhibitor VIT-2763 Improves Erythropoiesis without Interfering with Iron Chelation Therapy in a Mouse Model of beta-Thalassemia.
Nyffenegger N, Flace A, Doucerain C, Dürrenberger F, Manolova V. Nyffenegger N, et al. Int J Mol Sci. 2021 Jan 16;22(2):873. doi: 10.3390/ijms22020873. Int J Mol Sci. 2021. PMID: 33467196 Free PMC article.
Mice were treated with VIT-2763 or DFX alone or with the combination of both drugs once daily for three weeks. VIT-2763 alone or in combination with DFX improved anemia and erythropoiesis. ...
Mice were treated with VIT-2763 or DFX alone or with the combination of both drugs once daily for three weeks. VIT-2 …
Oral ferroportin inhibitor VIT-2763: First-in-human, phase 1 study in healthy volunteers.
Richard F, van Lier JJ, Roubert B, Haboubi T, Göhring UM, Dürrenberger F. Richard F, et al. Am J Hematol. 2020 Jan;95(1):68-77. doi: 10.1002/ajh.25670. Epub 2019 Nov 19. Am J Hematol. 2020. PMID: 31674058 Free PMC article. Clinical Trial.
This first-in-human, Phase I study (https://www.clinicaltrialsregister.eu; EudraCT no. 2017-003395-31) assessed the safety, tolerability, pharmacokinetics and pharmacodynamics of single- and multiple-ascending doses (SAD and MAD) of the oral ferroportin inhibitor, VIT-2 …
This first-in-human, Phase I study (https://www.clinicaltrialsregister.eu; EudraCT no. 2017-003395-31) assessed the safety, tolerability, ph …
Oral ferroportin inhibitor ameliorates ineffective erythropoiesis in a model of β-thalassemia.
Manolova V, Nyffenegger N, Flace A, Altermatt P, Varol A, Doucerain C, Sundstrom H, Dürrenberger F. Manolova V, et al. J Clin Invest. 2019 Dec 9;130(1):491-506. doi: 10.1172/JCI129382. J Clin Invest. 2019. PMID: 31638596 Free PMC article.
VIT-2763 not only improved erythropoiesis but also corrected the proportions of myeloid precursors in spleens of Hbbth3/+ mice. VIT-2763 is currently being developed as an oral drug targeting ferroportin for the treatment of beta-thalassemia....
VIT-2763 not only improved erythropoiesis but also corrected the proportions of myeloid precursors in spleens of Hbbth3/+ mice …