• Journal of Pharmaceutical Investigation
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• 제35권1호
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• pp.57-63
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• 2005

Numerous drugs are chiral because they possess one or more chiral centers. Enantiomers may differ in their pharmacokinetic, pharmacological and toxicological properties. However, the significance of stereochemistry of drugs in their therapeutic uses has received relatively little attention until recently. The US FDA issued a guideline on stereoisomeric drugs in 1992, and the European agency describes tests for new drug substances which are optically active in an ICH(International Conference of Harmonization) guideline. According to the guidance, enantiomers may differ in their pharmacokinetic, pharmacological and toxicological properties. Therefore, in this paper, we examined the recently published Canadian guidance, stereochemical issues in chiral drug development, which will be references to make a guidance on stereochemical issues in chiral drug development in Korea.

• 한국응용과학기술학회지
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• 제25권4호
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• pp.539-555
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• 2008

It is well understood that developing new drugs is one of the highest value-added businesses in a country; however, the current governments' spending in pharmaceutical research and development(R&D) is minimal in Korea. This paper suggests that different governmental bodies should take in charge of different stages of the R&D process in order to maximize the use of limited government research funding. First, during the initial phase of the drug development, including clinical trials, the Ministry of Education, Science and Technology is the most appropriate governmental organization to support the research. For later procedures such as supporting the industries for exporting developed drugs, legislative approvals, and building infrastructure for future clinical trials should be supported by the Ministry of Knowledge and Economy and the Ministry of Health and Welfare along with the Korea Food and Drug Administration(KFDA). The KFDA, which is the main governmental agency approving newly developed drugs in the market, will need to take a crucial responsibility in the initial phase of the pharmaceutical R&D by guiding the industries with timely and proper information. As a first step, it is recommended to set up and operate a center for supporting new drugs, so that the industries can facilitate the development of marketable drugs which meet customers' needs. Later, in order to expedite the process of exporting and getting approvals of the newly developed drugs from foreign countries, it is necessary to develop new approval system, which includes introduction of the Good Manufacturing Practice (GMP), mandatory validation system, and education program for supporting expertise. Lastly, the KFDA needs to take an active role in developing Korean pharmaceutical industries by communicating with other foreign governments with regards to the globalization of the Korean pharmaceutical industries. For example, as a follow up after the Free Trade Agreement(FTA), active discussion on GLP of Mutual Recognition Agreement(MRA) with the United States of America, should be seriously considered.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2003년도 춘계학술대회 논문집
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• pp.75-75
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• 2003

Silica has been known to be a factor in acute cell injury and chronic pulmonary fibrosis. In Rat2 fibroblasts, silica induced the activation of NFkB, which plays a crucial role in regulating the expression of many genes involved in the subsequent inflammatory response. In addition, we observed that TAK1 and NIK were involved in silica-mediated NF-kB activation in Rat2 cells. (omitted)

• Journal of Interdisciplinary Genomics
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• 제3권2호
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• pp.25-29
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• 2021

Myotonic muscular dystrophy is a disease characterized by progressive muscle weakness with myotonia and multiorgan involvement. Two subtypes have been recognized; each subtype is caused by nucleotide repeat expansion. So far, there has been no cure for myotonic muscular dystrophy. In this article, we introduce ongoing clinical trials for new drugs to modify disease course by correcting genetic derangement or its downstream in myotonic dystrophy type 1.

• Biomolecules & Therapeutics
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• 제29권1호
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• pp.41-51
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• 2021

Src family kinases (SFKs), an important group of non-receptor tyrosine kinases, are suggested to be excessively activated during various types of tissue fibrosis. The present study investigated the effect of KF-1607, an orally active and a newly synthesized Src kinase inhibitor (SKI) with proposed low toxicity, in preventing the progression of renal interstitial fibrosis. Unilateral ureteral obstruction (UUO) surgery was performed in 6-week-old male C57BL/6 mice to induce renal interstitial fibrosis. Either KF-1607 (30 mg/kg, oral gavage) or PP2 (2 mg/kg, intraperitoneal injection), a common experimental SKI, was administered to mice for seven days, started one day prior to surgery. UUO injury-induced SFK expression, including Src, Fyn, and Lyn kinase. SFK inhibition by KF-1607 prevented the progression of tubular injury in UUO mice, as indicated by decreases in albuminuria, urinary KIM-1 excretion, and kidney NGAL protein expression. Renal tubulointerstitial fibrosis was attenuated in response to KF-1607, as shown by decreases in α-SMA, collagen I and IV protein expression, along with reduced Masson's trichrome and collagen-I staining in kidneys. KF-1607 also inhibited inflammation in the UUO kidney, as exhibited by reductions in F4/80 positive-staining and protein expression of p-NFκB and ICAM. Importantly, the observed effects of KF-1607 were similar to those of PP2. A new pan Src kinase inhibitor, KF-1607, is a potential pharmaceutical agent to prevent the progression of renal interstitial fibrosis.

• 통합자연과학논문집
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• 제5권4호
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• pp.229-232
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• 2012

The pharmaceutical industry has an ongoing need for new, safe medicines with genuine biomedical effects. Most of the candidate molecules are far from becomes a drug, because of their pharmacokinetic and pharmacodynamic properties. The introduction of bioisostere to improve properties of molecules and to obtain new class of compound is currently increased. Silicon substitution of carbon of existing drugs is an attractive strategy to search a new candidate with improved biological and physicochemical properties. The fundamental differences between carbon and silicon can lead to improved profile of the silicon containing candidate, and could be exploited to get further benefit in drug design process.

• 생명과학회지
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• 제33권8호
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• pp.663-679
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• 2023

본 리뷰 논문은 2010년부터 2022년까지의 인공지능을 활용한 신약개발 관련 연구동향을 분석하여 정리하였다. 이러한 분석을 통해 2,421개 연구의 초록을 코퍼스로 구성하고, 전처리를 거쳐 빈도가 높고 연결 중심성이 높은 단어를 추출하였다. 분석 결과 2010-201년과 2020-2022년 단어빈도 추이는 비슷한 것으로 구분되어 나타났다. 연구 방법으로는 2010년부터 2020년까지 머신 러닝을 활용한 연구가 많이 진행되었고, 2021년부터는 딥러닝을 활용한 연구가 증가하고 있다. 이러한 연구를 통해 이루어지고 있는 인공지능 활용연구 동향에 대해 분야별로 살펴보고 관련 연구의 장점, 문제점, 도전과제 등을 살펴보았다. 파악되어진 연구 동향은 2021년 이후로 약물의 재배치를 인공지능 활용 연구, 항암제 개발을 위한 컴퓨터 활용 연구, 임상시험에 인공지능 적용 연구 등과 같이 인공지능 적용 분야가 확대되고 있다는 점이다. 이러한 과정을 통해 향후 이루어질 것으로 예상되는 인공지능 활용 신약개발 연구의 전망에 대해 간략히 제시하였다. 위의 인공지능 기술 발전과 함께 바이오와 의료데이터의 신뢰성과 안전성이 확보되어진다면 인공지능 활용 신약개발의 방향이 개인 맞춤형 의료와 정밀의료 분야로 진행되어질 것으로 판단하기에 이에 대한 지속적인 노력이 필요하리라 본다.

• 벤처창업연구
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• 제14권1호
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• pp.151-166
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• 2019

신약개발은 기초연구${\rightarrow}$전임상${\rightarrow}$임상${\rightarrow}$품목허가${\rightarrow}$판매에 이르기까지 10~15년의 긴 시간과 10억불 이상의 막대한 자금을 필요로 한다. 많은 신약개발 바이오벤처기업은 증권시장 상장을 통해 확보한 자금으로 신약개발을 지속적으로 추진하고자 한다. 본 연구는 증권시장 상장이 신약개발 바이오벤처기업에 미치는 영향에 주목하여, 상장 시점(D) 및 상장 후 2년 시점(D+2년)에서 등록특허, 전임상, 임상, 기술이 전계약의 증가 여부로 증권시장 상장에 의한 신약개발 바이오벤처기업의 기술사업화 성과를 분석하였다. 또한 상장 및 상장 후 2년 시점에서 등록특허, 전임상 및 임상이 기술이전계약에 유의미한 영향을 미치는지 분석하였다. 분석결과는 다음과 같다. 첫째, 한국의 신약개발 바이오벤처기업은 상장 시점과 상장 후 2년 시점을 비교하면, 등록특허는 증가했으나 전임상, 임상 및 기술이전계약은 증가하지 않았다. 둘째, 상장 시점과 상장 후 2년 시점에 전임상은 한국기술이전계약에 유의한 영향을 주고 있고 해외기술이전계약에 부분적으로 유의한 영향을 주고 있지만, 등록특허 및 임상은 기술이전계약에 유의한 영향을 주지 않았다. 한국의 신약개발 바이오벤처기업은 증권시장 상장에도 불구하고 특허는 증가했지만, 전임상, 임상 및 기술이전계약은 증가하지 못했음을 알 수 있다. 향후 신약개발 바이오벤처기업의 기술사업화를 강화하기 위해서는 IPO 공모자금의 효율적 사용을 위한 R&D전략 수립, 산 학 연 연계 강화를 통한 오픈 이노베이션, 보다 정교한 전임상 및 임상 전략 수립 등이 요청되고 있다.

• 전자통신동향분석
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• 제38권3호
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• pp.38-46
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• 2023

The value of living a long and healthy life without suffering has increased owing to aging populations, transition to welfare societies, and global interest in health deriving from the novel coronavirus disease pandemic. New drug development has gained attention as both a tool to improve the quality of life and high-value market, with blockbuster drugs potentially generating over 10 billion dollars in annual revenue. However, for newly discovered substances to be used as drugs, various properties must be verified over a long period in a time-consuming and costly process. Recently, the development of artificial intelligence technologies, such as deep and reinforcement learning, has led to significant changes in drug development by enabling the effective identification of drug candidates that satisfy desired properties. We explore and discuss trends in artificial intelligence for de novo drug design.

• 한국컴퓨터정보학회논문지
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• 제21권3호
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• pp.65-71
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• 2016

To reduce the expenses for development a novel drug, systems biology has been studied actively. Target prediction, a part of systems biology, contributes to finding a new purpose for FDA(Food and Drug Administration) approved drugs and development novel drugs. In this paper, we propose a classification model for predicting novel target genes based on relation between target genes and disease related genes. After collecting known target genes from TTD(Therapeutic Target Database) and disease related genes from OMIM(Online Mendelian Inheritance in Man), we analyzed the effect of target genes on disease related genes based on PPI(Protein-Protein Interactions) network. We focused on the distinguishing characteristics between known target genes and random target genes, and used the characteristics as features for building a classifier. Because our model is constructed using information about only a disease and its known targets, the model can be applied to unusual diseases without similar drugs and diseases, while existing models for finding new drug-disease associations are based on drug-drug similarity and disease-disease similarity. We validated accuracy of the model using LOOCV of ten times and the AUCs were 0.74 on Alzheimer's disease and 0.71 on Breast cancer.