Ipsen announced the results of phase-I and phase-IIa clinical studies for its BIM23A760 designed and developed by Ipsen's research team using its validated peptide engineering platform. BIM23A760 is a first-inclass innovative 'chimeric' compound that bears within a single molecule two pharmacological moieties, that is a somatostatin analog and a dopamine agonist. This molecule targets two of the most commonly patho-physiological pathways associated with pituitary tumours: growth hormone and prolactin. The design of BIM23A760 is based on a novel concept in molecular biology regarding the amplification of intracellular signalling when engaging simultaneously two receptors with their respective ligands.
In the phase-I trial, the exposure to BIM23A760 in healthy volunteers showed a pharmacokinetic profile consistent with sustained release compatible with a once-weekly dosing. BIM23A760 treatment potently suppressed prolactin levels at all tested doses after single dosing, with a decrease in prolactin sustained for at least 4 weeks after repeated dosing. In addition, statistically significant reductions in IGF-1 levels were observed after repeated dosing.
In the phase-IIa study, the exposure to BIM23A760 in acromegalic patients, exhibited a pharmacological activity as evidenced by a 66 to 74 per cent mean maximum reduction in growth hormone (GH) levels compared to baseline. A dose dependent tendancy for a more pronounced and longer GH inhibition was also observed. Additionally, a reduction in IGF-1 levels was seen in both dosage (1 mg and 4 mg). The pharmacokinetic profile of BIM23A760 among patients with acromegaly was similar to the profile observed among healthy participants in the phase-I study. BIM 23A760 was well tolerated at both dosages.
Jacques-Pierre Moreau, executive vice-president, chief scientific officer said, "The phase-I and phase-IIa results for BIM23A760 show encouraging signs of efficacy with the markers of bioactivity pointing in the right direction. BIM23A760's original design might represent a true advance in the therapy of pituitary adenomas. This compound is at the very heart of Ipsen's endocrinology focus and expertise on homeostasis, namely restoring the hormonal imbalance induced by pituitary disorders."
BIM23A760 is a new chimeric compound that contains structural elements of both somatostatin analogues and dopamine agonists and acts synergistically by inducing an interaction between these receptors in disorders such as acromegaly and neuroendocrine tumours.
Ipsen is an innovation-driven international specialty pharmaceutical group with over 20 products on the market and a total worldwide staff of nearly 4,200.