Abstract: Described here are TRPV1 agonist compounds and their methods of synthesis and use. In addition to specifically identified compounds, capsaicin prodrugs, gemini dimers, and mutual prodrugs are also described. Formulations of the TRPV1 agonist compounds may be in the form of a liquid, tablets, capsules, gel, cream, emulsion, a patch, or the like. Methods for treating medical conditions using the compounds, compositions, or prodrugs described, are also provided.

Abstract: Oils of capsaicinoids and methods of making and using them are described. In some variations, the oils of capsaicinoids comprise at least 40% w/w capsaicinoid and a solvent capable of solubilizing the capsaicinoid, wherein the oil of capsaicinoid is substantially free of capsaicinoid crystals or capsaicinoid precipitates. In other variations, the oils of capsaicinoids consist essentially of at least 40% w/w capsaicinoid and a solvent capable of solubilizing the capsaicinoid. The solvent may be a semi-volatile solvent, a non-volatile solvent, or a volatile solvent, and the oil may comprise at least 50% w/w capsaicinoid, 60% w/w capsaicinoid, 70% w/w capsaicinoid, 80% w/w capsaicinoid, 90% w/w capsaicinoid, or 95% w/w capsaicinoid. The oil of capsaicinoid may also include a crystallization inhibitor.

Abstract: Described here are patches and methods for treating neuropathic pain. In some variations, the neuropathic pain-relieving patch comprises capsaicin or a capsaicin analog, wherein the concentration of the capsaicin or capsaicin analog is less than 1% by weight, and a penetration enhancer, wherein the patch is capable of relieving neuropathic pain over a sustained period of time. The penetration enhancer may be any suitable penetration enhancer. The patches may also include oils, viscosity increasing agents, and the like. In some variations, the pain-relieving patches comprise capsaicin, or an, wherein the concentration of the capsaicin or analog is less than 1%, and a penetration enhancer, whereby delivery of capsaicin from the patch continues for at least an hour, and whereby a single use of the patch provides a therapeutic benefit for at least one month, two months, or three months. Methods for treating neuropathic pain are also described.

Abstract: The invention provides compositions, methods and kits for the removal of harmful or irritating substances from bodily surfaces. Kits may include a composition containing capsaicin and a capsaicin-cleaning composition, e.g., a composition in which capsaicin is soluble.

Abstract: Described here are drug delivery devices including an occlusive backing layer and a drug depot containing a TRPV1 agonist and a non-hydrophilic solvent. The drug depot may take various forms, such as an adhesive polymeric matrix, liquid reservoir, or microreservoir droplets. Methods of making and using the drug delivery devices are also described.

Abstract: The invention provides compositions, methods and kits for the removal of harmful or irritating substances from bodily surfaces. Kits may include a composition containing capsaicin and a capsaicin-cleansing composition, e.g., a composition in which capsaicin is soluble.

Abstract: Compositions are provided that contain a TRPV1 agonist, such as capsaicin, and a solvent system. Topical application of the composition results in rapid delivery of agonist to the dermis and epidermis. Method of using the compositions for reducing nociceptive nerve fiber function in subjects, and for treatment of capsaicin-responsive conditions are also provided.

Abstract: Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R1, R2, A and X are as defined herein. Also disclosed are compounds and related compositions.