FX125L
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FX125L is the lead, orally available BSCI, currently in Phase I clinical trials in the USA.
The potent anti-inflammatory activity of FX125L following oral administration has been clearly demonstrated in a wide range of animal models of disease in vivo, including rodent models of allergic asthma, RA and atherosclerosis, while the regulatory preclinical studies with FX125L suggested a very favourable safety profile and a wide therapeutic range. FX125L has optimal CMC characteristics and is obtained by a straightforward 3-step chemical synthesis with an extremely low cost of goods. GMP production has been established and stability is excellent. |
Different immunological challenges (e.g. cantharidin-induced skin blister challenge) have been incorporated in the Phase I studies with FX125L in healthy subjects, yielding a series of biomarkers of the inflammatory response that could provide an early indication of the biological activity of FX125L in man. FX125L was well tolerated in doses up to 30-fold the presumed therapeutic dose after single administration in man and its pharmacokinetics were linear with an elimination half life of about 25h. The clinical indications targeted with FX125L include respiratory disorders such as asthma and COPD, supported by numerous studies in a wide range of animal models, which consistently suggested that FX125L may have in the clinic similar efficacy but better safety than corticosteroids and superior efficacy than montelukast. |
