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Japanese cedar (JC) pollinosis is a common allergic rhinitis in Japan. The JC pollen sublingual immunotherapy (SLIT) tablet was developed using the highest concentration of JC pollen extract.This was a randomized, double-blind, placebo-controlled phase II/III trial to investigate the optimal dose of the JC pollen SLIT tablet and examine long-term efficacy and safety for 3 years with the selected dose, and 2-year follow-up.A total of 1042 patients with JC pollinosis (aged 5-64 years) were equally randomized into 4 groups and received daily treatment with 2,000, 5,000, or 10,000 Japanese allergy unit (JAU) or placebo. The primary end point was the total nasal symptom and medication score (TNSMS) during the peak symptom period in the first season. Key secondary end points were TNSMS for the JC pollen dispersion season and total nasal and ocular symptom and medication score for the peak symptom period and JC pollen dispersion season.For the primary end point, absolute reductions and relative mean reductions in TNSMS compared with placebo were 1.50 and 21.4%, 2.24 and 32.1%, and 2.18 and 31.2% for 2,000, 5,000, and 10,000 JAU, respectively (P.001 in all groups). For all key secondary end points, efficacy was confirmed for all doses (P.001 in all groups). The treatment was well tolerated. Long-term efficacy of 5,000 JAU was shown over the 3 years.The optimal dose of the JC pollen SLIT tablet was 5,000 JAU, with good efficacy and safety over a 3-year treatment period. This sustained effect was dependent on treatment duration.

A novel linker possessing selenocyanate and masked carboxylic acid was developed for the solid-phase synthesis of dehydropeptides. This linker was used to demonstrate the synthesis of the model compound of RGD-conjugated dehydropeptide.

Beta-Amyloid peptide (Abeta) is the main protein component of neuritic plaques in the brain of patients of Alzheimer's disease (AD), and its neurotoxicity would be exposed by the formation of aggregates. The aggregation inhibitors composed of an Abeta recognition element (KLVFF) and a hydrophilic moiety are evaluated by a novel fluorescence assay. These compounds inhibit growth of the model aggregates on the KLVFF immobilized surface. In addition, some compounds also possess disrupting activities of preformed aggregates. These compounds could be a key candidate for therapeutic drugs for AD by their novel molecular mechanisms.

The cyclic dehydrodepsipeptide, AM-toxin II, was efficiently synthesized by a solid-phase method using a novel selenyl linker. The cleavage from the resin with formation of a double bond is successfully achieved under mild oxidative conditions with TBHP.