CD51 antagonists(Integrin alpha-V antagonists), αvβ3 antagonists(Integrin alpha-V/beta-3 antagonists), αvβ5 antagonists(Integrin alpha-V/beta-5 antagonists)

Therapeutic Areas

Cardiovascular DiseasesCongenital DisordersEndocrinology and Metabolic Disease+ [1]

Active Indication-

Inactive Indication

Originator Organization

Johnson & Johnson Pharmaceutical Research & Development LLC

Active Organization-

Inactive Organization

Johnson & Johnson Pharmaceutical Research & Development LLC

Neuromed Pharmaceuticals Ltd.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with JNJ-26076713

100 Translational Medicine associated with JNJ-26076713

100 Patents (Medical) associated with JNJ-26076713

Literatures (Medical) associated with JNJ-26076713

01 Sep 2020·Expert Opinion on Investigational DrugsQ2 · MEDICINE

Anti-integrin therapy for retinovascular diseases

Q2 · MEDICINE

Review

Author: Ciulla, Thomas ; Luo, Qianyi ; Bhatwadekar, Ashay D. ; Kansara, Viral

INTRODUCTIONIntegrins are a family of multi-functional cell-adhesion molecules, heterodimeric receptors that connect extracellular matrix (ECM) to actin cytoskeleton in the cell cortex, thus regulating cellular adhesion, migration, proliferation, invasion, survival, and apoptosis. Consequently, integrins play a role in inflammation, angiogenesis and fibrosis.AREAS COVEREDThis review examines individual anti-integrin agents in terms of their chemical nature, route of administration, and anti-integrin action. It also provides a summary of preclinical and clinical studies. Current clinical candidates include risuteganib, THR-687, and SF-0166, which have shown promise in treating diabetic macular edema (DME) and/or age-related macular degeneration (AMD) in early clinical studies. Preclinical candidates include SB-267268, AXT-107, JNJ-26076713, Cilengitide and Lebecetin, which exhibit a decrease in retinal permeability, angiogenesis and/or choroidal neovascularization (CNV).EXPERT OPINIONAnti-integrin therapies show potential in treating retinal diseases. Anti-integrin agents tackle the multi-factorial nature of diabetic retinopathy (DR) and AMD and show promise as injectable and topical agents in preclinical and early clinical studies. Integrin inhibition has potential to serve as primary therapy, adjunctive therapy to anti-vascular endothelial growth factor agents, or secondary therapy in refractory cases.

01 Mar 2008·The Journal of Pharmacology and Experimental TherapeuticsQ3 · MEDICINE

Studies with an Orally Bioavailable αV Integrin Antagonist in Animal Models of Ocular Vasculopathy: Retinal Neovascularization in Mice and Retinal Vascular Permeability in Diabetic Rats

Q3 · MEDICINE

Article

Author: Liu, Li ; Shaw, Lynn C. ; Tuman, Robert W. A. ; Huebert, Norman ; Grant, Maria B. ; Ghosh, Shyamali ; Kinney, William A. ; Maryanoff, Bruce E. ; Zhou, Zhao ; Santulli, Rosemary J. ; Mousa, Shaker A. ; Damiano, Bruce P. ; Johnson, Dana L. ; Bursell, Sven E. ; Clermont, Alan C. ; DeCorte, Bart L. ; Galemmo, Robert A. Jr.

The alpha(V) integrins are key receptors involved in mediating cell migration and angiogenesis. In age-related macular degeneration (AMD) and diabetic retinopathy, angiogenesis plays a critical role in the loss of vision. These ocular vasculopathies might be treatable with a suitable alpha(V) antagonist, and an oral drug would offer a distinct advantage over current therapies. (3,S,beta,S)-1,2,3,4-Tetrahydro-beta-[[1-[1-oxo-3-(1,5,6,7-tetrahydro-1,8-naphthyridin-2-yl)propyl]-4-piperidinyl]methyl]-3-quinolinepropanoic acid (JNJ-26076713) is a potent, orally bioavailable, nonpeptide alpha(V) antagonist derived from the arginine-glycine-asparagine binding motif in the matrix protein ligands (e.g., vitronectin). This compound inhibits alpha(V)beta(3) and alpha(V)beta(5) binding to vitronectin in the low nanomolar range, it has excellent selectivity over integrins alpha(IIb)beta(3) and alpha(5)beta(1), and it prevents adhesion to human, rat, and mouse endothelial cells. JNJ-26076713 blocks cell migration induced by vascular endothelial growth factor, fibroblast growth factor (FGF), and serum, and angiogenesis induced by FGF in the chick chorioallantoic membrane model. JNJ-26076713 is the first alpha(V) antagonist reported to inhibit retinal neovascularization in an oxygen-induced model of retinopathy of prematurity after oral administration. In diabetic rats, orally administered JNJ-26076713 markedly inhibits retinal vascular permeability, a key early event in diabetic macular edema and AMD. Given this profile, JNJ-26076713 represents a potential therapeutic candidate for the treatment of age-related macular degeneration, macular edema, and proliferative diabetic retinopathy.

01 Mar 2008·The Journal of Organic ChemistryQ2 · CHEMISTRY

Suzuki−Miyaura Approach to JNJ-26076713, an Orally Active Tetrahydroquinoline-Containing α_Vβ₃/α_Vβ₅ Integrin Antagonist. Enantioselective Synthesis and Stereochemical Studies

Q2 · CHEMISTRY

Article

Author: Ballentine, Scott ; Santulli, Rosemary J. ; Schubert, Carsten ; Teleha, Christopher A. ; Thompson, Andrew S. ; Mahan, Andrew ; Zanotti-Gerosa, Antonio ; Hansen, Ryan ; McComsey, David F. ; Zhou, Yong ; Kinney, William A. ; Ghosh, Shyamali ; Grasa, Gabriela ; Newport, Maria ; Leo, Gregory C. ; Dingenen, Jules ; Maryanoff, Bruce E.

An improved scale-up synthesis was required for the alpha(V)beta(3)/alpha(V)beta(5) integrin antagonist 1, which had demonstrated oral efficacy in eye disease models of angiogenesis and vascular permeability. A stereodefined, quinoline-substituted, unsaturated ester was conveniently prepared by a Suzuki-Miyaura coupling to facilitate exploration of multiple methods of asymmetric reduction. The catalytic chiral hydrogenation of the corresponding unsaturated acid (Z-5b) with a ruthenium-based metal precursor and the (R)-XylPhanePhos ligand proved particularly efficient and economical. The resulting (3S)-quinoline-containing intermediate was reduced to an equal mixture of tetrahydroquinoline diastereomers. The undesired diastereomer could be recycled to the desired one by an oxidation/reduction protocol. The absolute stereochemistry of 1 was established as 3S,3'S by a combination of X-ray diffraction and chemical means.

100 Deals associated with JNJ-26076713

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Age Related Macular Degeneration	Preclinical	United States	Johnson & Johnson Pharmaceutical Research & Development LLC	14 Dec 2007
Age Related Macular Degeneration	Preclinical	Canada	Neuromed Pharmaceuticals Ltd.	14 Dec 2007
Diabetic macular oedema	Preclinical	United States	Johnson & Johnson Pharmaceutical Research & Development LLC	14 Dec 2007
Diabetic macular oedema	Preclinical	Canada	Neuromed Pharmaceuticals Ltd.	14 Dec 2007
Proliferative retinopathy with diabetes mellitus	Preclinical	United States	Johnson & Johnson Pharmaceutical Research & Development LLC	14 Dec 2007
Proliferative retinopathy with diabetes mellitus	Preclinical	Canada	Neuromed Pharmaceuticals Ltd.	14 Dec 2007

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