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Glioma is the most common type of central nervous system tumor reported worldwide. Current imaging technologies have limitations in the diagnosis and assessment of glioma. The present study aimed to confirm the diagnostic efficacy and safety of anti-1-amino-3-[18F]fluorocyclobutane carboxylic acid (18F-fluciclovine; anti-[18F]FACBC) as a radiotracer for patients undergoing combined positron emission tomography and computed tomography (PET/CT) for suspected glioma. Combined data from two multicenter, open-label phase III clinical trials were evaluated for this study. The two trials enrolled patients with suspected high- or low-grade glioma on the basis of clinical symptoms, clinical course, and magnetic resonance imaging findings, and who were scheduled for tumor resection surgery. Patients fasted for ≥ 4 h and received 2 mL of 18F-fluciclovine (radioactivity dose 78.3–297.0 MBq), followed by a 10-min PET scan 10–50 min after injection. The primary efficacy endpoint was the positive predictive value (PPV) of the gadolinium contrast-enhanced T1-weighted image negative [Gd (–)] and 18F-fluciclovine PET-positive [PET ( +)] area of the scans, using the histopathological diagnosis of the tissue sampled from that area as the standard of truth. All adverse events reported during the study were recorded for safety analysis. A total of 45 patients aged 23–89 years underwent 18F-fluciclovine PET; 31/45 patients (68.9%) were male, and 30/45 patients (66.7%) were suspected to have high-grade glioma. The PPV of 18F-fluciclovine PET in the Gd (–) PET ( +) area was 88.0% (22/25 areas, 95% confidence interval: 70.0–95.8). The extent of planned tumor resection was modified in 47.2% (17/36 cases) after 18F-fluciclovine PET scan, with an extension of area in 30.6% (11/36 cases) and reduction in 16.7% (6/36 cases). Furthermore, tissue samples collected from PET ( +) areas tended to have a higher malignancy grade compared with those from PET (–) areas. Overall, 18F-fluciclovine was well tolerated. 18F-fluciclovine PET/CT is useful for determining the extent of tumor resection at surgical planning, and may serve as a safe and effective diagnostic tool for patients with suspected glioma. These trials were registered in the Japan Pharmaceutical Information Center Clinical Trials Information (JapicCTI-152986, JapicCTI-152985).

Glioma is the most common type of central nervous system tumor reported worldwide. Current imaging technologies have limitations in the diagnosis and assessment of glioma. The present study aimed to confirm the diagnostic efficacy and safety of anti-1-amino-3-[Combined data from two multicenter, open-label phase III clinical trials were evaluated for this study. The two trials enrolled patients with suspected high- or low-grade glioma on the basis of clinical symptoms, clinical course, and magnetic resonance imaging findings, and who were scheduled for tumor resection surgery. Patients fasted for ≥ 4 h and received 2 mL ofA total of 45 patients aged 23-89 years underwentThese trials were registered in the Japan Pharmaceutical Information Center Clinical Trials Information (JapicCTI-152986, JapicCTI-152985).

A furan-fused 3-sulfolene 4H,6H-thieno[3,4-c]furan 5,5-dioxide 1, can be used as a bis-diene, reacting sequentially with a variety of dienophiles to construct four types of skeleton, depending on the dienophile and the reaction conditions. The 3-sulfolene moiety of the furansulfolene not only functions as the s-cis-diene part in Diels–Alder reactions, but also extends the range of the Diels–Alder reactions of the furan moiety with various dienophiles through its desulfonylation to form the s-cis-diene.

核磁気共鳴を用いた断層診断法(MAgnetic Resonance Imaging, 以下MRIと略記する)における第二世代の造影剤として,血管内に滞留性を有するガドリニウム化合物についての検討を行った。本目的のために多糖誘導体を骨格とし,二官能性キレート剤を介したガドリニウム化合物を合成した。多糖誘導体は分子量7×103のデンプンおよび3×103のアミロースを酸化開裂した化合物を合成した。二官能性キレート剤としては,N-[2-bis(carboxymethyl)aminoethyl]-N[2-bis(carboxymethyl)amlno-2-(p-benzyl)ethyl]glycineおよび環状骨格を有する新規化合物10-[1Y-(2-アミノエチル)カルバモイル]メチル-α,α',α"-トリメチル-1,4,7,10-テトラアザシクロドデカン-1,4,7-三酢酸を合成した。各化合物についてMRI用薬剤の基礎検討として,磁場強度0.5Tおよび1.5Tにおける緩和時間の測定,111In標識体を用いた体内分布の検討および疾患動物を用いたin vivoでの造影実験を行った。いずれの化合物も血管内滞留性が認められ,また速やかに尿中に排泄された。さらに多糖誘導体に結合させることにより緩和効果の向上が認められた。以上の結果から本化合物は第二世代のMRI用造影剤として,有望であることが明らかとなった。

The preparation of the hitherto unknown 4,6-dihydrothieno[3,4-c]furan S,S-dioxide 1 and its intermolecular Diels–Alder reactions with typical dienophiles are described.

At high pressure, the furansulfolene, 4H,6H-thieno[3,4-c]furan 5,5- dioxide (1), whose furan and 3-sulfolene moieties could be used as diene components in Diels-Alder reactions, reacted with the dienophiles at its furan moiety selectively