• Title/Summary/Keyword: fosaprepitant

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Efficacy and Safety of an Increased-dose of Dexamethasone in Patients Receiving Fosaprepitant Chemotherapy in Japan

  • Kumagai, Hozumi;Kusaba, Hitoshi;Okumura, Yuta;Komoda, Masato;Nakano, Michitaka;Tamura, Shingo;Uchida, Mayako;Nagata, Kenichiro;Arita, Shuji;Ariyama, Hiroshi;Takaishi, Shigeo;Akashi, Koichi;Baba, Eishi
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.1
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    • pp.461-465
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    • 2014
  • Background: Antiemetic triplet therapy including dexamethasone (DEX) is widely used for patients receiving highly emetogenic chemotherapy (HEC). In Japan, the appropriate dose of DEX has not been established for this combination. Materials and Methods: To assess the efficacy and safety of increased-dose DEX, we retrospectively examined patients receiving HEC with antiemetic triplet therapy. Results: Twenty-four patients (fosaprepitant group) were given an increased-dose of DEX (average total dose: 45.8mg), fosaprepitant, and 5-HT3 antagonist. A lower-dose of DEX (33.6mg), oral aprepitant, and 5-HT3 antagonist were administered to the other 48 patients (aprepitant group). The vomiting control rates in the fosaprepitant and aprepitant groups were 100% and 85.4% in the acute phase, and were 75.0% and 64.6% in the delayed phase. The incidences of toxicity were similar comparing the two groups. Conclusions: Triplet therapy using an increased-dose of DEX is suggested to be safe and effective for patients receiving HEC.

Virtual screening, molecular docking studies and DFT calculations on JNK3

  • Priya, dharshini;Thirumurthy, Madhavan
    • Journal of Integrative Natural Science
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    • v.15 no.4
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    • pp.179-186
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    • 2022
  • The c-Jun N-terminal kinase (JNK3) play major role in neurodegenerative diseases like Alzheimer's disease, Parkinson's disease, cerebral ischemia and other Central Nervous System disorders. Since JNK3 is primarily stated in the brain and stimulated by stress-stimuli, this situation is conceivable that inhibiting JNK3 could be a possible treatment for the mechanisms underlying neurodegenerative diseases. In this study drugs from Zinc15 database were screened to identify the JNK3 inhibitors by Molecular docking and Density functional theory approach. Molecular docking was done by Autodock vina and the ligands were selected based on the binding affinity. Our results identified top ten novel ligands as potential inhibitors against JNK3. Molecular docking revealed that Venetoclax, Fosaprepitant and Avapritinib exhibited better binding affinity and interacting with proposed binding site residues of JNK3. Density functional theory was used to compute the values for energy gap, lowest unoccupied molecular orbital (LUMO), and highest occupied molecular orbital (HOMO). The results of Density functional theory study showed that Venetoclax, Fosaprepitant and Avapritinib serves as a lead compound for the development of JNK3 small molecule inhibitors.