• Title/Summary/Keyword: Olmutinib

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Crystal Form of Olmutinib

  • Lee, Chang-Yeob;Sohn, Young-Taek
    • Journal of the Korean Chemical Society
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    • v.63 no.1
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    • pp.7-11
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    • 2019
  • Olmutinib, N-[3-({2-[4-(4-methylpiperazine-1-yl)aniline]thieno[3,2-d]Pyrimidin-4-yl}oxy)phenyl]prop-2-enamide dihydrochloride monohydrate, $Olita^{TM}$ is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that was developed by Boehringer Ingelheim and Hanmi Pharmaceutical Co. Ltd for the treatment of non-small cell lung cancer (NSCLC). The aim of this work was to investigate the existence of polymorphs and pseudopolymorphs of olmutinib. Three crystal forms of olmutinib have been isolated by recrystallization and characterized by differential scanning calorimetry (DSC), thermogravimetric (TG) analysis and powder X-ray diffractometry (PXRD). From the DSC and TG data it was confirmed that Form 1 is monohydrate, Form 2 is dihydrate, Form 3 is 1.5 hydrate. The PXRD patterns of three crystal forms were different respectively. After storage of 1 month at $2^{\circ}C$, 24% RH (Relative Humidity), Form 1, Form 2, and Form 3 were not transformed.

A Case of Non-Small Cell Lung Carcinoma Patient Who Improved Skin Rash Due to Olmutinib by Administration of Nobongsangki-Jeong (노봉상기정을 투여하여 Olmutinib으로 인한 피부염이 호전된 4기 비소세포성 폐암 환자 1례)

  • Choi, You-Na;Kim, Jeehye;Bae, Kyeore;Cho, Chong-kwan;Yoo, Hwa-Seung
    • Journal of Korean Traditional Oncology
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    • v.22 no.1
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    • pp.13-22
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    • 2017
  • Objective: The purpose of this study is to report the effect of Nobongsangki-Jeong on skin rash caused by Olmutinib. Methods: A female Non-Small cell lung carcinoma patient (Adenocarcinoma, Stage IV, Epidermal Growth Factor Receptor positive) suffered from skin rash due to the side effect of Olmutinib administration. She was treated with Nobongsangki-Jeong for the symptom management for 14 days. The clinical outcomes were measured by numeric rating scale (NRS) and National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 4.03. Results: After treatment, skin rash was improved from NRS 5 to 1. Pruritus and pain of skin were improved from NCI-CTCAE grade 2 to 1. Conclusion: This case study suggests that Nobongsangki-Jeong may have the efficacy for the treatment of skin rash caused by Olmutinib.