An Open-Label Randomized Pilot Study of Safety and Preliminary Efficacy of TG100801 in Patients With Choroidal Neovascularization Due to Age-Related Macular Degeneration

Wet age-related macular degeneration (AMD) is caused by the formation and growth of abnormal blood vessels (angiogenesis) in the retina. The new blood vessels have fragile walls and can leak fluid into the retina. The build-up of fluid (edema) under the macula can distort vision or cause vision loss. TG100801 is a topical (eye drop) therapy that has been shown to inhibit ocular angiogenesis, vascular leak, and inflammation in laboratory studies. The primary purpose of this pilot study is to evaluate the ability of topical administration of TG100801 to reduce the amount of fluid in the retina in patients with AMD following 30 days of treatment. An additional objective is to evaluate the safety of TG100801 in patients with AMD.

Start Date01 Jul 2007

Sponsor / Collaborator

TargeGen, Inc.

NCT00414999

/ CompletedPhase 1

A Phase 1, Double-Masked, Placebo-Controlled, Dose-Escalation Study (in Two Parts) of TG100801 and a Colored Vehicle in Adult Healthy Volunteers

The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, age-related macular degeneration (AMD), which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. TG100801 is a new drug that inhibits ocular angiogenesis, vascular leak, and inflammation in laboratory studies, and may have great utility in the treatment of diseases such as AMD.
The purpose of this study is to assess the safety, ocular tolerability, and blood pharmacokinetics of TG100801 at escalating doses in healthy volunteers.

Start Date01 Nov 2006

Sponsor / Collaborator

TargeGen, Inc.

100 Clinical Results associated with TG-100801

100 Translational Medicine associated with TG-100801

100 Patents (Medical) associated with TG-100801

Literatures (Medical) associated with TG-100801

03 Apr 2022·AutoimmunityQ4 · MEDICINE

Drug repurposing for rheumatoid arthritis: Identification of new drug candidates via bioinformatics and text mining analysis

Q4 · MEDICINE

Article

Author: Unal, Ulku ; Gov, Esra ; Comertpay, Betul ; Demirtas, Talip Yasir

Rheumatoid arthritis (RA) is an autoimmune disease that results in the destruction of tissue by attacks on the patient by his or her own immune system. Current treatment strategies are not sufficient to overcome RA. In the present study, various transcriptomic data from synovial fluids, synovial fluid-derived macrophages, and blood samples from patients with RA were analysed using bioinformatics approaches to identify tissue-specific repurposing drug candidates for RA. Differentially expressed genes (DEGs) were identified by integrating datasets for each tissue and comparing diseased to healthy samples. Tissue-specific protein-protein interaction (PPI) networks were generated and topologically prominent proteins were selected. Transcription-regulating biomolecules for each tissue type were determined from protein-DNA interaction data. Common DEGs and reporter biomolecules were used to identify drug candidates for repurposing using the hypergeometric test. As a result of bioinformatic analyses, 19 drugs were identified as repurposing candidates for RA, and text mining analyses supported our findings. We hypothesize that the FDA-approved drugs momelotinib, ibrutinib, and sodium butyrate may be promising candidates for RA. In addition, CHEMBL306380, Compound 19a (CHEMBL3116050), ME-344, XL-019, TG100801, JNJ-26483327, and NV-128 were identified as novel repurposing candidates for the treatment of RA. Preclinical and further validation of these drugs may provide new treatment options for RA.

01 Dec 2017·Science (New York, N.Y.)Q1 · CROSS-FIELD

The target landscape of clinical kinase drugs

Q1 · CROSS-FIELD

Article

Author: Wu, Zhixiang ; Reiter, Katrin ; Ruprecht, Benjamin ; Schmidt, Tobias ; Heinzlmeir, Stephanie ; Schneider, Sabine ; Meng, Chen ; Garz, Anne-Kathrin ; Qiao, Huichao ; Vooder, Tonu ; Canevari, Giulia ; Vick, Binje ; Schoof, Melanie ; Feuchtinger, Annette ; Ehrlich, Hans-Christian ; Helm, Dominic ; Tõnisson, Neeme ; Koch, Heiner ; Klaeger, Susan ; Huenges, Jan ; Polzer, Harald ; Greif, Philipp A. ; Kramer, Karl ; Spiekermann, Karsten ; Zolg, Daniel Paul ; Walch, Axel ; Casale, Elena ; Schlegl, Judith ; Zecha, Jana ; Becker, Wilhelm ; Kuster, Bernhard ; Aiche, Stephan ; Ruland, Juergen ; Petzoldt, Svenja ; Depaolini, Stefania Re ; Jeremias, Irmela ; Reinecke, Maria ; Wilhelm, Mathias ; Preissner, Robert ; Bassermann, Florian ; Koenig, Paul-Albert ; Médard, Guillaume ; Kayser, Gian ; Götze, Katharina ; Hahne, Hannes ; Felder, Eduard Rudolf ; Gohlke, Bjoern-Oliver ; Rueckert, Lars

Kinase inhibitors are important cancer therapeutics. Polypharmacology is commonly observed, requiring thorough target deconvolution to understand drug mechanism of action. Using chemical proteomics, we analyzed the target spectrum of 243 clinically evaluated kinase drugs. The data revealed previously unknown targets for established drugs, offered a perspective on the "druggable" kinome, highlighted (non)kinase off-targets, and suggested potential therapeutic applications. Integration of phosphoproteomic data refined drug-affected pathways, identified response markers, and strengthened rationale for combination treatments. We exemplify translational value by discovering SIK2 (salt-inducible kinase 2) inhibitors that modulate cytokine production in primary cells, by identifying drugs against the lung cancer survival marker MELK (maternal embryonic leucine zipper kinase), and by repurposing cabozantinib to treat FLT3-ITD-positive acute myeloid leukemia. This resource, available via the ProteomicsDB database, should facilitate basic, clinical, and drug discovery research and aid clinical decision-making.

01 Jun 2010·BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapyQ3 · MEDICINE

Current Status of Vascular Endothelial Growth Factor Inhibition in Age-Related Macular Degeneration

Q3 · MEDICINE

Review

Author: Shaker A. Mousa ; Shaymaa S. Mousa

Angiogenesis, the process by which new vessels are created from pre-existing vasculature, has become the subject of intense research in recent years. Increased rates of angiogenesis are associated with several disease states, including cancer, age-related macular degeneration (AMD), psoriasis, rheumatoid arthritis, and diabetic retinopathy. Vascular endothelial growth factor (VEGF) is an important modulator of angiogenesis, and has been implicated in the pathology of a number of conditions, including AMD, diabetic retinopathy, and cancer. AMD is a progressive disease of the macula and the third major cause of blindness worldwide. If not treated appropriately, AMD can progress to involve both eyes. Until recently, the treatment options for AMD have been limited, with photodynamic therapy (PDT) the mainstay of treatment. Although PDT is effective at slowing disease progression, it rarely results in improved vision. Several therapies have been or are now being developed for neovascular AMD, with the goal of inhibiting VEGF. These VEGF inhibitors include the RNA aptamer pegaptanib, partial and full-length antibodies ranibizumab and bevacizumab, the VEGF receptor decoy aflibercept, small interfering RNA-based therapies bevasiranib and AGN 211745, sirolimus, and tyrosine kinase inhibitors, including vatalanib, pazopanib, TG 100801, TG 101095, AG 013958, and AL 39324. At present, established therapies have met with great success in reducing the vision loss associated with neovascular AMD, whereas those still under investigation offer the potential for further advances. In AMD patients, these therapies slow the rate of vision loss and in some cases increase visual acuity. Although VEGF-inhibitor therapies are a milestone in the treatment of these disease states, several concerns need to be addressed before their impact can be fully realized.

News (Medical) associated with TG-100801

30 Jul 2007

·www.biospace.com

TargeGen, Inc. Initiates Multi-Center Phase II Clinical Trial Of TG100801, a Topically Applied Kinase Inhibitor In Macular Degeneration Patients

SAN DIEGO, July 30 /PRNewswire/ -- TargeGen, Inc. today announced that the Company has initiated a multi-center Phase II clinical trial of topically applied TG100801 in patients with age-related macular degeneration (AMD). (Logo: ) AMD is the leading cause of blindness in adults with more than 3.5 million estimated patients worldwide. Currently approved treatments for macular degeneration require repeated injection into the eye and act primarily by reducing VEGF mediated retinal leakage. TG100801 is administered non-invasively as an eye drop and is designed to suppress VEGF mediated leakage and additional kinase targets associated with inflammation, edema, and angiogenesis which are the pathological hallmarks of AMD and other back of the eye diseases including diabetic macular edema and proliferative diabetic retinopathy. "The initiation of this trial is a significant milestone for TargeGen," stated Peter G. Ulrich, President, CEO and Co-Founder of TargeGen. "TG100801 is an important drug candidate that potentially addresses the leading causes of debilitating vision loss in adults in a more comprehensive way and may eliminate or reduce the requirement for repeated injections into the eye." In addition to TG100801, TargeGen is developing TG101348, an oral Jak2 inhibitor for the potential treatment of myeloproliferative diseases and TG100115, a PI3K inhibitor for the potential treatment of certain inflammatory disorders. A second topically applied compound for eye disease, TG100948, is in early development. About TargeGen, Inc. TargeGen, Inc. is a privately held vascular biology-focused biopharmaceutical company based in San Diego, CA. TargeGen primarily develops small molecule kinase inhibitors that target vascular leakage (edema), vascular proliferation (angiogenesis) and inflammation. Edema, angiogenesis and inflammation are involved in the pathology of many major human diseases. TargeGen initiated operations in 2002 and has raised capital from top tier venture capital sources. Current investors include VantagePoint Venture Partners, Forward Ventures, Enterprise Partners, Chicago Growth Partners, BB BIOTECH, Innovis Investments, H&Q Capital Management, Pappas Ventures and other investors. Photo: NewsCom: AP Archive: PRN Photo Desk, photodesk@prnewswire.comTargeGen, Inc. CONTACT: TargeGen, Inc., +1-858-678-0760, fax, +1-858-678-0160,info@targegen.com Web site:

Small molecular drug

100 Deals associated with TG-100801

External Link

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Age Related Macular Degeneration	Phase 2	United States	TargeGen, Inc.	01 Jul 2007
Choroidal Neovascularization	Phase 2	United States	TargeGen, Inc.	01 Jul 2007
Glycogen Storage Disease Type II	Phase 2	United States	TargeGen, Inc.	01 Jul 2007
Diabetic Retinopathy	Phase 1	United States	TargeGen, Inc.	01 Nov 2006
Diabetic macular oedema	Preclinical	United States	TargeGen, Inc.	01 May 2006
Diabetic macular oedema	Preclinical	United States	The Scripps Research Institute	01 May 2006

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ARVO2006	Not Applicable	-	-	TG100572	thsyocupie(xxhndeznyv) = phogvzsyud imikqkdggj (taxtszznlf )	-	01 May 2006