The purpose of this study is to determine the appropriate dose of Ro 27-2441 (test drug) to be used in future studies, assess the efficacy and safety, and the anti-inflammatory action of the test drug in the treatment of asthmatic patients who are not currently receiving chronic therapy with corticosteroids. The research is being conducted at up to 80 clinical research sites in the US, Mexico, and Canada. Study participants will have a number of visits to a research site over approximately a 4-month period.

Start Date25 Oct 2002

Sponsor / Collaborator

Hoffmann-La Roche, Inc.

100 Clinical Results associated with Valategrast Hydrochloride

100 Translational Medicine associated with Valategrast Hydrochloride

100 Patents (Medical) associated with Valategrast Hydrochloride

Literatures (Medical) associated with Valategrast Hydrochloride

01 Dec 2020·Medicine in Drug Discovery

Protein-Driven Mechanism of Multiorgan Damage in COVID-19

Article

Author: Estrada, Ernesto

We propose a new plausible mechanism by mean of which SARS-CoV-2 produces extrapulmonary damages in severe COVID-19 patients. The mechanism consist on the existence of vulnerable proteins (VPs), which are (i) mainly expressed outside the lungs; (ii) their perturbations is known to produce human diseases; and (iii) can be perturbed directly or indirectly by SARS-CoV-2 proteins. These VPs are perturbed by other proteins, which are: (i) mainly expressed in the lungs, (ii) are targeted directly by SARS-CoV-2 proteins, (iii) can navigate outside the lungs as cargo of extracellular vesicles (EVs); and (iv) can activate VPs via subdiffusive processes inside the target organ. Using bioinformatic tools and mathematical modeling we identifies 26 VPs and their 38 perturbators, which predict extracellular damages in the immunologic endocrine, cardiovascular, circulatory, lymphatic, musculoskeletal, neurologic, dermatologic, hepatic, gastrointestinal, and metabolic systems, as well as in the eyes. The identification of these VPs and their perturbators allow us to identify 27 existing drugs which are candidates to be repurposed for treating extrapulmonary damage in severe COVID-19 patients. After removal of drugs having undesirable drug-drug interactions we select 7 drugs and one natural product: apabetalone, romidepsin, silmitasertib, ozanezumab, procaine, azacitidine, amlexanox, volociximab, and ellagic acid, whose combinations can palliate the organs and systems found to be damaged by COVID-19. We found that at least 4 drugs are needed to treat all the multiorgan damages, for instance: the combination of romidepsin, silmitasertib, apabetalone and azacitidine.

02 Dec 2018·Expert Opinion on Therapeutic PatentsQ2 · MEDICINE

α₄β₇ integrin inhibitors: a patent review

Q2 · MEDICINE

Review

Author: Wei, Ji-Fu ; Gu, Zhi-Chun ; Shi, Fang-Hong ; Huang, Shi-Ying ; Li, Hao ; Zhang, Shun-Guo

INTRODUCTIONThe α₄β₇ integrin is heterodimeric cell surface receptors expressed on most leukocytes. Mucosal addressing cell adhesion molecule 1(MAdCAM-1) is an exclusive ligand for α₄β₇ integrin. Areas covered: This article will highlight the progress that has been made in the discovery and development of α₄β₇ integrin inhibitors, and their use in the treatment of inflammatory bowel diseases, multiple sclerosis, asthma, hepatic disorders, human immunodeficiency virus, allergic conjunctivitis and type 1 diabetes. Expert opinion: α₄β₇ integrin inhibitors have attracted much interest for their clinical implication. Natalizumab and Vedolizumab are monoclonal antibodies (mAbs) successfully utilized clinically. Natalizumab is a mAbs of α₄-subunit blocking both α₄β₁ and α₄β₇ integrin. Vedolizumab selectively targets the α₄β₇ integrin. Several mAbs are still in the process of research and development. Among these mAbs, etrolizumab selectively against the β₇-subunit and AMG-181 specifically against the α₄β₇ integrin are the most promising anti-α₄β₇ integrin antibodies. Despite the unclear development stage of TR-14035 and R411, several low molecular compounds show bright future of further development, such as AJM300 and CDP323. In addition, results from laboratory data show that peptide inhibitors, such as peptide X, are effective α₄β₇ integrin inhibitors.

13 Feb 2014·ACS Medicinal Chemistry LettersQ3 · MEDICINE

Small Macrocycles As Highly Active Integrin α2β1 Antagonists

Q3 · MEDICINE

Article

Author: Kohlmann, Markus ; Lindenschmidt, Andreas ; Blum, Horst ; Buning, Christian ; Halland, Nis

Starting from clinical candidates Firategrast, Valategrast, and AJM-300, a series of novel macrocyclic platelet collagen receptor α2β1 antagonists were developed. The amino acid derived low molecular weight 14-18-membered macrocycles turned out to be highly active toward integrin α2β1 with IC50s in the low nanomolar range. The conformation of the macrocycles was found to be highly important for the activity, and an X-ray crystal structure was obtained to clarify this. Subsequent docking into the metal-ion-dependent adhesion site (MIDAS) of a β1 unit revealed a binding model indicating key binding features. Macrocycle 38 was selected for further in vitro and in vivo profiling.

100 Deals associated with Valategrast Hydrochloride

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	Australia	Hoffmann-La Roche, Inc.	25 Oct 2002
Asthma	Phase 2	Puerto Rico	Hoffmann-La Roche, Inc.	25 Oct 2002
Asthma	Phase 2	United States	Hoffmann-La Roche, Inc.	25 Oct 2002
Asthma	Phase 2	Mexico	Hoffmann-La Roche, Inc.	25 Oct 2002
Asthma	Phase 2	Canada	Hoffmann-La Roche, Inc.	25 Oct 2002
Multiple Sclerosis	Phase 2	United States	-	-
Multiple Sclerosis	Phase 2	United States	-	-
Multiple Sclerosis	Phase 2	-	F. Hoffmann-La Roche Ltd.	-
Multiple Sclerosis	Phase 2	-	F. Hoffmann-La Roche Ltd.	-

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