Background: Rheumatoid arthritis (RA) is a chronic, systemic, inflammatory disease that affects approximately 0.5 – 1% of adults worldwide and commonly results in joint destruction and significant impairment in the quality of life. RA is considered an autoimmune disease with unknown etiology. Many pathogenic pathways of RA have been revealed recently, which has led to development of various novel therapies. Objective: The current treatments for RA fall into four categories: non-steroidal anti-inflammatory drugs, glucocorticoids, non-biological, disease-modifying antirheumatic drugs (DMARDs) and biological DMARDs. In this review, we discuss some of the most recent development in antirheumatic therapies. Methods: Using SciFinder Scholar and PubMed as our main search tools, we evaluated various newly developed therapies for RA. In each drug category, emphases are placed on the mode of action, limitations and new drug candidates from the patent search. Those therapies that are well-established are reviewed on...

The Development of Novel Therapies for Rheumatoid Arthritis.

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

Chemosensory receptor ligand-based therapies

A suspension formulation of an insulinotropic peptide (e.g., glucagon-like peptide- 1 (GLP-1) or exenatide) is described. The suspension formulation comprises (i) a non¬ aqueous, single-phase vehicle, comprising one or more polymer and one or more one solvent, wherein the vehicle exhibits viscous fluid characteristics, and (ii) a particle formulation comprising the insulinotropic peptide, wherein the peptide is dispersed in the vehicle. The particle formulation further includes a stabilizing component comprising one or more stabilizers, for example, carbohydrates, antioxidants, amino acids, and buffers. Devices for delivering the suspension formulations and methods of use are also described.

Suspension formulations of insulinotropic peptides and uses thereof

The huge increase in type 2 diabetes is a burden worldwide. Many marketed compounds do not address relevant aspects of the disease; they may already compensate for defects in insulin secretion and insulin action, but loss of secreting cells (β-cell destruction), hyperglucagonemia, gastric emptying, enzyme activation/inhibition in insulin-sensitive cells, substitution or antagonizing of physiological hormones and pathways, finally leading to secondary complications of diabetes, are not sufficiently addressed. In addition, side effects for established therapies such as hypoglycemias and weight gain have to be diminished. At present, nearly 1000 compounds have been described, and approximately 180 of these are going to be developed (already in clinical studies), some of them directly influencing enzyme activity, influencing pathophysiological pathways, and some using G-protein-coupled receptors. In addition, immunological approaches and antisense strategies are going to be developed. Many compounds are derived from physiological compounds (hormones) aiming at improving their kinetics and selectivity, and others are chemical compounds that were obtained by screening for a newly identified target in the physiological or pathophysiological machinery. In some areas, great progress is observed (e.g., incretin area); in others, no great progress is obvious (e.g., glucokinase activators), and other areas are not recommended for further research. For all scientific areas, conclusions with respect to their impact on diabetes are given. Potential targets for which no chemical compound has yet been identified as a ligand (agonist or antagonist) are also described.

Novel Pharmacological Approaches to the Treatment of Type 2 Diabetes

Implantable medical devices having anti-restenotic coatings are disclosed. Specifically, implantable medical devices having coatings of certain antiproliferative agents, particularly certain protein farnesyl transferase inhibitors, are disclosed. The anti-restenotic protein farnesyl transferase inhibitors are tipifarnib, lonafarnib, and pharmaceutically acceptable derivatives thereof. The anti-restenotic medial devices include stents, catheters, micro-particles, probes and vascular grafts. Intravascular stents are preferred medical devices. The medical devices can be coated using any method known in the art including compounding the protein farnesyl transferase inhibitor with a biocompatible polymer prior to applying the coating. Moreover, medical devices composed entirely of biocompatible polymer-protein farnesyl transferase inhibitor blends are disclosed. Additionally, medical devices having a coating comprising at least one protein farnesyl transferase inhibitor in combination with at least one additional therapeutic agent are also disclosed. Furthermore, related methods of using and making the anti-restenotic implantable devices are also disclosed.

Medical devices to treat or inhibit restenosis

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects.

Controlled release pharmaceutical compositions comprising a fumaric acid ester

The present invention relates to novel amino acid salts of fumaric acid monoalkylesters. The salts are suitable for use as active substances in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders.

Novel salts of fumaric acid monoalkylesters and their pharmaceutical use

Compounds and pharmaceutical compositions for use in the treatment and/or prophylaxis of cartilage and/or bone conditions and for methods of treating such condition. The compounds are salts of strontium that have a water-solubility of from about 1 g/l to about 100 g/l at room temperature, especially amino acid salts of strontium or dicarboxylic acid salts of strontium. Examples of novel water-soluble strontium salts are e.g. strontium glutamate and strontium alpha-ketoglutarate. The present invention also relates to an improved method for preparing the strontium salt of glutamic acid.

Water-soluble strontium salts for use in treatment of cartilage and/or bone conditions

Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and/or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors/antagonists of IL-1, inhibitors/antagonists of TNF-α, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors/antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and/or prophylactically active substance as defined above.

Treatments comprising strontium for rheumatic and arthritic diseases and pain

The present invention relates to novel glucofuranose esters and glucopyranose esters of alkyl-fumarates. The esters are suitable for use as active substances in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders.

Henrik Nilsson

Papers

Controlled release pharmaceutical compositions comprising a fumaric acid ester

Novel salts of fumaric acid monoalkylesters and their pharmaceutical use

Water-soluble strontium salts for use in treatment of cartilage and/or bone conditions

Treatments comprising strontium for rheumatic and arthritic diseases and pain

Novel glucopyranose esters and glucofuranose esters of alkyl- fumarates and their pharmaceutical use