Drugs in R&D
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Efaproxiral [RSR 13, GSJ 61, JP 4, KDD 86, RS 4] is a synthetic, small-molecule, radiation-sensitising agent being developed by Allos Therapeutics primarily for the treatment of cancer. It works by binding and allosterically stabilising deoxyhaemoglobin in hypoxic regions of tumour tissue. This increases oxygen uptake of the tumour tissue and restores its sensitivity to radiation therapy, making therapy potentially more successful. ⋯ To penetrate the non-oncology market in the US, the company will seek partnership with one or more pharmaceutical companies with direct sales forces and with established distribution systems. Allos is also hoping to secure an oncology marketing partner for non-North American territories. At the time, the company had been issued 21 patents in the US, Canada, Europe and Japan.
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Although oral nonsteroidal anti-inflammatory drugs (NSAIDs) are effective in the treatment of a variety of acute and chronic pain conditions, their use may be associated with serious systemic adverse effects, particularly gastrointestinal disorders. In order to minimise the incidence of systemic events related to such agents, topical NSAIDs have been developed. Topical NSAIDs, applied as gels, creams or sprays, penetrate the skin, subcutaneous fatty tissue and muscle in amounts that are sufficient to exert a therapeutic effect on peripheral and central mechanisms in the absence of high plasma concentrations. ⋯ Moreover, the topical ketoprofen patch was well tolerated; adverse events were primarily cutaneous in nature and occurred in a similar number of ketoprofen and placebo recipients suggesting that these events were related to the patch itself rather than the active ingredient. The incidence of gastrointestinal adverse events was low (<8% of all patients), and occurred in a similar proportion of patients receiving ketoprofen and placebo. Thus, the topical ketoprofen patch appears to be a simple, effective and safe therapeutic option for the treatment of local painful inflammation.
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Natalizumab [AN 100226, anti-alpha4 integrin monoclonal antibody, Antegren] is a humanised monoclonal antibody that blocks alpha4beta1 integrin-mediated leukocyte migration. Natalizumab is in phase III trials for the treatment of multiple sclerosis in North America and the UK, and for the treatment of Crohn's disease also in the UK. It may have potential in the treatment of other immune-related inflammatory disease. ⋯ He also predicted that Antegren could be on the market as early as 2003 for the indication of Crohn's disease and in 2004 for multiple sclerosis. The Journal stated that Biogen is under pressure to develop new drugs since its flagship product Avonex will be losing its US Orphan Drug Act protection in 2003. Antegren has a different mechanism to that of Avonex and could be used either alone or as a combination therapy.
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Exisulind [Aptosyn trade mark, FGN 1 trade mark, Prevatac trade mark, sulindac sulfone], the sulfone derivative of sulindac, is the lead compound in a series of selective apoptotic antineoplastic drugs (SAANDs) being developed by OSI Pharmaceuticals. The compounds were originally developed by Cell Pathways, which was acquired by, and integrated into, OSI Pharmaceuticals in June 2003. Exisulind inhibits the enzyme cyclic GMP phosphodiesterase (GMP-PDE), overexpressed in precancerous and cancerous colorectal cells, and induces apoptosis in such cells with minimal effects on normal cells. ⋯ The Eastern Cooperative Oncology Group (ECOG) initiated a phase II study in NSCLC patients in September 2002 that will investigate the effects of exisulind in combination with gemcitabine and carboplatin. The objectives of the two studies are to determine the 12-month survival rate and response rates following treatment with the combination regimens. Patents covering the mechanism of action of exisulind have been allowed in Europe and Japan, and extend to the methods of identifying compounds that selectively stimulate apoptosis in precancerous and cancerous cells.
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Gadofosveset [MS 325, MS 32520, Vasovist, ZK 236018], a gadolinium-based chelate, is an injectable angiography imaging agent for use in magnetic resonance imaging (MRI) scans. The agent is being developed by EPIX Medical (formerly Metasyn) for diagnostic imaging of blood vessels of the cardiovascular system. Gadofosveset has potential as an alternative to the range of x-ray, invasive, catheter-based angiograms and thallium stress tests currently used in the diagnosis of coronary artery disease. ⋯ However, under provision of the Hatch-Waxman Act, the terms of the patent may be extended following FDA approval. In its 2002 Annual Report, Schering predicted that gadofosveset has the potential to reach peak sales of EUR100 million, 3 years after launch - at the time, launch in the US was anticipated in 2005. Earlier, at an analyst presentation in Berlin in March 2002, the company stated that launch in the US was planned for 2004.