Obecure is a clinical stage company developing Histalean®, a first-in-class pro-histaminic drug to improve the overall health and quality of life of patients in need of antipsychotic drug treatment for mental disorders such as schizophrenia, bipolar disease and major depression. Treatment with antipsychotic medications can relieve many of the devastating symptoms of such diseases. However, in the vast majority of patients, it is accompanied by side effects that seriously impact their lives, such as excessive somnolence and a dramatic weight gain that exposes them to serious health hazards, such as obesity, diabetes and cardiovascular disease. Unlike the antipsychotic effects of these drugs that are mediated by their dopaminergic and serotonergic inhibition, their side effects are mainly attributable to their anti-histaminic activity. Indeed, proof-of-concept clinical trials conducted by the Company demonstrate that Histalean® has a distinct capacity to significantly attenuate the side effects associated with Zyprexa® (olanzapine), a leading antipsychotic drug, with annual sales of more than $5 billion.
The company was founded in 2005 by Bio-Light Life Science Investments Ltd, publically traded on the Tel Aviv Stock Exchange (TASE:BOLT) and holds an exclusive license for the technology from Mor Research Applications Ltd, the technology transfer arm of Clalit Health Services (Israel's leading HMO).
Histalean® is a novel dosage form of betahistine dihydrochloride, a prescription drug used worldwide for over 40 years to treat Meniere's disease (vertigo). In the U.S., the drug was approved for marketing in 1967 but, although there were no concerns regarding safety, queries regarding its efficacy led the FDA to its withdrawal in 1972. The drug has a remarkable safety record, as evidenced in a post-marketing surveillance review, reporting that after more than 130 million patient exposures, only about 550 adverse event reports were filed.1
Betahistine’s pharmacological action involves the activation of the histaminergic system in the brain, required for multiple functions including the control of eating, sleeping, attention and cognition. It has a unique dual-action mechanism, activating the major receptor for histamine signal mediation, the H1 receptor, and antagonizing the negative feedback by the H3 autoregulatory receptor. This double barrel activity may thus be clinically translated to improvement of histamine signaling for reducing eating and improving general alertness. In particular, it may be beneficial when histaminergic activity is impaired, in patients who take medications that have undesirable antihistaminic activities leading to weight gain and somnolence. These include many of the most beneficial antipsychotic drugs such as Zyprexa®, Risperdal®(risperidone) and Seroquel® (quetiapine).
Obecure has conducted several controlled clinical studies, investigating the clinical benefit of Histalean® for promoting weight-loss in obesity and for reduction of olanzapine-induced weight gain and somnolence. Study results to date suggest that Histalean's benefits in mitigating antipsychotic drug side effects greatly outweigh its potential as an overall anti-obesity agent. In fact, co-administration with olanzapine, resulted in a clinically and statistically significant reduction of about 40% of the weight gain and about 60% of the somnolence induced by the antipsychotic treatment.2 3Moreover, treatment with Histalean in conjunction with olanzapine in schizophrenia patients for four months, suggested a favorable antipsychotic therapeutic benefit, as compared to patients treated with placebo and olanzapine alone, although statistical significance was not reached.4
Based on these preliminary findings, Obecure is focusing on the development of Histalean®as adjunctive to olanzapine therapy. The company has embarked on a clinical program designed to optimize the efficacy profile of Histalean® by exploring novel formulations, doses and regimens of administration, and is currently seeking investments and/or partnerships to further accelerate its development towards this lucrative market.
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