Article(id=1209788326459077145, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1209788321396552074, articleNumber=null, orderNo=null, doi=10.16438/j.0513-4870.2021-1784, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=research-article, receivedDate=1639324800000, receivedDateStr=2021-12-13, revisedDate=1640707200000, revisedDateStr=2021-12-29, acceptedDate=null, acceptedDateStr=null, onlineDate=1766365613808, onlineDateStr=2025-12-22, pubDate=1644595200000, pubDateStr=2022-02-12, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1766365613808, onlineIssueDateStr=2025-12-22, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1766365613808, creator=13701087609, updateTime=1766365613808, updator=13701087609, issue=Issue{id=1209788321396552074, tenantId=1146029695717560320, journalId=1189982191388893191, year='2022', volume='57', issue='2', pageStart='251', pageEnd='546', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1766365612600, creator=13701087609, updateTime=1766370652531, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1209809460445451136, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1209788321396552074, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1209809460445451137, tenantId=1146029695717560320, journalId=1189982191388893191, issueId=1209788321396552074, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=251, endPage=264, ext={EN=ArticleExt(id=1209788326979170882, articleId=1209788326459077145, tenantId=1146029695717560320, journalId=1189982191388893191, language=EN, title=Drug discovery from viewpoint of medicinal chemists, columnId=1190335349059588909, journalTitle=Acta Pharmaceutica Sinica, columnName=Professionals Forum, runingTitle=null, highlight=null, articleAbstract=
Taking patient needs as the core and realizing clinical value as the guidance are the purpose and path of drug discovery. Whether the first-in-class drug or follow-on drugs are all to meet the demands of patients for drugs that are not treatable or more safe and effective. In order to realize clinical value, innovative drugs driven by basic biological research include three elements: understanding the molecular mechanism of pathogenesis; Grasping the microscopic features of the disease; clarifying the mechanism of action of drugs. The interrelation among the three is the translational medicine, and the medicinal chemistry plays an important role in the translations. That is, based on the results of basic research in biology/medicine, knowledge of the molecular mechanism of disease depends upon the establishment of various in vitro/in vivo models to find the key node and molecular regulation for the treatment of disease. Combined with the knowledge of gene deletion and variation, proteomics, epigenetics and other technologies, the molecular mechanism of disease provides multi-molecular information on the level of gene, proteins, enzymes, receptors, ion channels and signal transduction for molecular drug design. Insight into the microscopic characteristics of diseases would deepen the understanding of the molecular mechanism of the pathogenesis, as well as provide a feasible scientific path for the creation of new drugs. When the molecular mechanism of disease and the action mechanism of drugs are clarified, we have a deeper and wider understanding of the application of existing drugs (or active compounds), and may offer new ideas for drug design and application. In this translational process the medicinal chemistry plays a key role which requires medicinal chemists to break through the habitual thinking and working mode, backtracking (upstream) to basic research and its achievements and applying to the direction of creating new drugs in time, as well as paying attention to the clinical requirements (downstream) and implementing the specific content of the transformation process for the R&D of innovative drugs.
, correspAuthors=Zong-ru GUO, authorNote=null, correspAuthorsNote=null, copyrightStatement=Copyright ©2022 Acta Pharmaceutica Sinica. All rights reserved., copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, authorCompany=null, fund=null, authors=null, authorsList=Zong-ru GUO), CN=ArticleExt(id=1209788346222637758, articleId=1209788326459077145, tenantId=1146029695717560320, journalId=1189982191388893191, language=CN, title=药物化学视角的新药创制, columnId=1190335349206389552, journalTitle=药学学报, columnName=专家论坛, runingTitle=null, highlight=null, articleAbstract=
以患者需求为核心，实现临床价值为导向，是新药创制的宗旨和路径。无论首创性药物或是仿创性药物都是为了满足患者对无药可治或更加安全有效的药物需求。以生物学基础研究驱动的创新药物，为实现临床价值包含三个要素或环节，即理解致病的分子机制；把握疾病的微观特征；阐明药物的作用机制。这三者之间的相互关联，是贯穿其中的转化医学，药物化学扮演重要角色。即将生物学/医学的基础研究成果通过各种模型阐明疾病发生发展的分子机制，从分析分子调控过程中找到治疗疾病的关键节点。患者的症状、生化常规和影像特征等宏观表象，难以在分子水平上为药物分子设计提供信息，生物学的发展，得以在微观水平作分子生物学分析，例如基因缺失与变异、蛋白质组学、表观遗传学等技术，结合疾病的分子机制，可从多样本和大数据分析中归纳基因-蛋白（酶、受体、通道、信号分子等）与疾病的关系，对创制新药和疗法提供新的科学依据。洞察疾病的微观特征是上述发病的分子机制的延续和深化，为创制新药提供可行的科学路径。当阐明了疾病的分子机制和药物的作用机制，对既有药物（或活性物质）的应用就有了更深刻和广泛的认识，提供了药物设计和应用的新思路。构建新分子结构（NME）的药物化学是其中的重要环节，要求药物化学研究者扩展固有的靶标-设计-合成-评价的模式，从大视野的角度，上溯关注基础研究及其成果，及时向创制新药的方向转轨；向下游关注临床要求，结合疾病的微观特征，落实转化过程的具体内容，这对于首创性药物的研发是非常关键的步骤。本文从药物化学视角浅谈一些看法。
, correspAuthors=郭宗儒, authorNote=null, correspAuthorsNote=
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Ostrem JM ,
Peters U ,
Sos ML et al . K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions[J].
Nature,
2013,
503: 548-551., articleTitle=K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions, refAbstract=null), Reference(id=1209809070601663449, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1073/pnas.91.14.6374, pmid=null, pmcid=null, year=1994, volume=91, issue=null, pageStart=6374, pageEnd=6378, url=null, language=null, rfNumber=[2], rfOrder=1, authorNames=Kawamura M, McVicar DW, Johnston JA, journalName=Proc Natl Acad Sci U S A, refType=null, unstructuredReference=
Kawamura M ,
McVicar DW ,
Johnston JA et al . Molecular cloning of L-JAK, a Janus family protein-tyrosine kinase expressed in natural killer cells and activated leukocytes[J].
Proc Natl Acad Sci U S A,
1994,
91: 6374-6378., articleTitle=Molecular cloning of L-JAK, a Janus family protein-tyrosine kinase expressed in natural killer cells and activated leukocytes, refAbstract=null), Reference(id=1209809070761047018, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1126/science.1087061, pmid=null, pmcid=null, year=2003, volume=302, issue=null, pageStart=875, pageEnd=878, url=null, language=null, rfNumber=[3], rfOrder=2, authorNames=Changelian PS, Flanagan ME, Kent CR, journalName=Science, refType=null, unstructuredReference=
Changelian PS ,
Flanagan ME ,
Kent CR et al . Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor[J].
Science,
2003,
302: 875-878., articleTitle=Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor, refAbstract=null), Reference(id=1209809070933013495, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/jm1004286, pmid=null, pmcid=null, year=2010, volume=53, issue=null, pageStart=8468, pageEnd=8484, url=null, language=null, rfNumber=[4], rfOrder=3, authorNames=Flanagan ME, Blumenkopf TA, Brissette WH, journalName=J Med Chem, refType=null, unstructuredReference=
Flanagan ME ,
Blumenkopf TA ,
Brissette WH et al . Discovery of CP-690, 550:a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection[J].
J Med Chem,
2010,
53: 8468-8484., articleTitle=Discovery of CP-690, 550:a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection, refAbstract=null), Reference(id=1209809071109173252, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/jm800669s, pmid=null, pmcid=null, year=2008, volume=51, issue=null, pageStart=6902, pageEnd=6915, url=null, language=null, rfNumber=[5], rfOrder=4, authorNames=Park CM, Bruncko M, Adickes J, journalName=J Med Chem, refType=null, unstructuredReference=
Park CM ,
Bruncko M ,
Adickes J et al . Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins[J].
J Med Chem,
2008,
51: 6902-6915., articleTitle=Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins, refAbstract=null), Reference(id=1209809071306305559, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1002/advs.202100250, pmid=null, pmcid=null, year=2021, volume=8, issue=null, pageStart=2100250, pageEnd=null, url=null, language=null, rfNumber=[6], rfOrder=5, authorNames=Zhang BY, Zhang Y, Zhang JW, journalName=Adv Sci, refType=null, unstructuredReference=
Zhang BY ,
Zhang Y ,
Zhang JW et al . Focal adhesion kinase (FAK) inhibition synergizes with KRAS G12C inhibitors in treating cancer through the regulation of the FAK-YAP signaling[J].
Adv Sci,
2021,
8: 2100250., articleTitle=Focal adhesion kinase (FAK) inhibition synergizes with KRAS G12C inhibitors in treating cancer through the regulation of the FAK-YAP signaling, refAbstract=null), Reference(id=1209809071465689125, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/acsmedchemlett.6b00491, pmid=null, pmcid=null, year=2017, volume=8, issue=null, pageStart=321, pageEnd=326, url=null, language=null, rfNumber=[7], rfOrder=6, authorNames=Metcalf B, Chuang C, Dufu K, journalName=ACS Med Chem Lett, refType=null, unstructuredReference=
Metcalf B ,
Chuang C ,
Dufu K et al . Discovery of GBT440, an orally bioavailable Rstate stabilizer of sickle cell hemoglobin[J].
ACS Med Chem Lett,
2017,
8: 321-326., articleTitle=Discovery of GBT440, an orally bioavailable Rstate stabilizer of sickle cell hemoglobin, refAbstract=null), Reference(id=1209809071587323953, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1016/j.canlet.2015.11.015, pmid=null, pmcid=null, year=2016, volume=370, issue=null, pageStart=332, pageEnd=344, url=null, language=null, rfNumber=[8], rfOrder=7, authorNames=Li Z, Jiang K, Zhu X, journalName=Cancer Lett, refType=null, unstructuredReference=
Li Z ,
Jiang K ,
Zhu X et al . Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells[J].
Cancer Lett,
2016,
370: 332-344., articleTitle=Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells, refAbstract=null), Reference(id=1209809071725736000, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1172/JCI66343, pmid=null, pmcid=null, year=2013, volume=123, issue=null, pageStart=2551, pageEnd=2563, url=null, language=null, rfNumber=[9], rfOrder=8, authorNames=Serra V, Eichhorn PJA, García-García C, journalName=J Clin Invest, refType=null, unstructuredReference=
Serra V ,
Eichhorn PJA ,
García-García C et al . RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer[J].
J Clin Invest,
2013,
123: 2551-2563., articleTitle=RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer, refAbstract=null), Reference(id=1209809071830593615, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=null, pmid=null, pmcid=null, year=2005, volume=40, issue=null, pageStart=967, pageEnd=969, url=null, language=null, rfNumber=[10], rfOrder=9, authorNames=Guo ZR, journalName=Acta Pharm Sin (药学学报), refType=null, unstructuredReference=
Guo ZR . Innovation of anti-inflammatory drugs-strategy of moderate inhibition of cyclooxygenases[J].
Acta Pharm Sin (药学学报),
2005,
40: 967-969., articleTitle=Innovation of anti-inflammatory drugs-strategy of moderate inhibition of cyclooxygenases, refAbstract=null), Reference(id=1209809071956422750, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1038/s41422-018-0055-1, pmid=null, pmcid=null, year=2018, volume=28, issue=null, pageStart=779, pageEnd=781, url=null, language=null, rfNumber=[11], rfOrder=10, authorNames=Sun YH, Zhao XW, Ding N, journalName=Cell Res, refType=null, unstructuredReference=
Sun YH ,
Zhao XW ,
Ding N et al . PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies[J].
Cell Res,
2018,
28: 779-781., articleTitle=PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies, refAbstract=null), Reference(id=1209809072161943668, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/acs.jmedchem.9b01566, pmid=null, pmcid=null, year=2020, volume=63, issue=null, pageStart=1216, pageEnd=1232, url=null, language=null, rfNumber=[12], rfOrder=11, authorNames=Cheng M, Yu XF, Lu K, journalName=J Med Chem, refType=null, unstructuredReference=
Cheng M ,
Yu XF ,
Lu K et al . Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders[J].
J Med Chem,
2020,
63: 1216-1232., articleTitle=Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders, refAbstract=null), Reference(id=1209809072350687367, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1016/j.chembiol.2015.05.009, pmid=null, pmcid=null, year=2015, volume=22, issue=null, pageStart=755, pageEnd=763, url=null, language=null, rfNumber=[13], rfOrder=12, authorNames=Lu J, Qian Y, Altieri M, journalName=Chem Biol, refType=null, unstructuredReference=
Lu J ,
Qian Y ,
Altieri M et al . Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4[J].
Chem Biol,
2015,
22: 755-763., articleTitle=Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4, refAbstract=null), Reference(id=1209809072510070940, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/acs.jmedchem.8b01631, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=941, pageEnd=964, url=null, language=null, rfNumber=[14], rfOrder=13, authorNames=Han X, Wang C, Qin C, journalName=J Med Chem, refType=null, unstructuredReference=
Han X ,
Wang C ,
Qin C et al . Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer[J].
J Med Chem,
2019,
62: 941-964., articleTitle=Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer, refAbstract=null), Reference(id=1209809072644288681, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/acs.jmedchem.9b01393, pmid=null, pmcid=null, year=2019, volume=62, issue=null, pageStart=11218, pageEnd=11231, url=null, language=null, rfNumber=[15], rfOrder=14, authorNames=Han X, Zhao LJ, Xiang WG, journalName=J Med Chem, refType=null, unstructuredReference=
Han X ,
Zhao LJ ,
Xiang WG et al . Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands[J].
J Med Chem,
2019,
62: 11218-11231., articleTitle=Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands, refAbstract=null), Reference(id=1209809072791089331, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1073/pnas.89.18.8641, pmid=null, pmcid=null, year=1992, volume=89, issue=null, pageStart=8641, pageEnd=8645, url=null, language=null, rfNumber=[16], rfOrder=15, authorNames=Thorens B, journalName=Proc Natl Acad Sci U S A, refType=null, unstructuredReference=
Thorens B . Expression cloning of the pancreatic
β-cell receptor for the gluco-incretin hormone glucagon-like peptide 1[J].
Proc Natl Acad Sci U S A,
1992,
89: 8641-8645., articleTitle=Expression cloning of the pancreatic
β-cell receptor for the gluco-incretin hormone glucagon-like peptide 1, refAbstract=null), Reference(id=1209809072891752641, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/jm9909645, pmid=null, pmcid=null, year=2000, volume=43, issue=null, pageStart=1664, pageEnd=1669, url=null, language=null, rfNumber=[17], rfOrder=16, authorNames=Knudsen LB, Nielsen PF, Huusfeldt PO, journalName=J Med Chem, refType=null, unstructuredReference=
Knudsen LB ,
Nielsen PF ,
Huusfeldt PO et al . Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration[J].
J Med Chem,
2000,
43: 1664-1669., articleTitle=Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration, refAbstract=null), Reference(id=1209809073017581778, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/acs.jmedchem.5b00726, pmid=null, pmcid=null, year=2015, volume=58, issue=null, pageStart=7370, pageEnd=7380, url=null, language=null, rfNumber=[18], rfOrder=17, authorNames=Lau J, Bloch P, Schäffer L, journalName=J Med Chem, refType=null, unstructuredReference=
Lau J ,
Bloch P ,
Schäffer L et al . Discovery of the once-weekly glucagon-like peptide 1(GLP-1) analogue semaglutide[J].
J Med Chem,
2015,
58: 7370-7380., articleTitle=Discovery of the once-weekly glucagon-like peptide 1(GLP-1) analogue semaglutide, refAbstract=null), Reference(id=1209809073126633693, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1038/nrd2030, pmid=null, pmcid=null, year=2006, volume=5, issue=null, pageStart=689, pageEnd=702, url=null, language=null, rfNumber=[19], rfOrder=18, authorNames=Ghofrani HA, Osterloh IH, Grimminger F, journalName=Nat Rev Drug Discov, refType=null, unstructuredReference=
Ghofrani HA ,
Osterloh IH ,
Grimminger F . Sildenafil: from angina to erectile dysfunction to pulmonary hypertension and beyond[J].
Nat Rev Drug Discov,
2006,
5: 689-702., articleTitle=Sildenafil: from angina to erectile dysfunction to pulmonary hypertension and beyond, refAbstract=null), Reference(id=1209809073260851436, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.3233/ADR-200166, pmid=null, pmcid=null, year=2020, volume=4, issue=null, pageStart=91, pageEnd=106, url=null, language=null, rfNumber=[20], rfOrder=19, authorNames=Sanders O, journalName=J Alzheimers Dis Rep, refType=null, unstructuredReference=
Sanders O . Sildenafil for the treatment of Alzheimer's disease: a systematic review[J].
J Alzheimers Dis Rep,
2020,
4: 91-106., articleTitle=Sildenafil for the treatment of Alzheimer's disease: a systematic review, refAbstract=null), Reference(id=1209809073416040697, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1038/s43587-021-00138-z, pmid=null, pmcid=null, year=2021, volume=null, issue=null, pageStart=null, pageEnd=null, url=null, language=null, rfNumber=[21], rfOrder=20, authorNames=Fang J, Zhang P, Zhou Y, journalName=Nat Aging, refType=null, unstructuredReference=
Fang J ,
Zhang P ,
Zhou Y et al . Endophenotype-based in silico network medicine discovery combined with insurance record data mining identifies sildenafil as a candidate drug for Alzheimer's disease[J].
Nat Aging,
2021. DOI:
10.1038/s43587-021-00138-z., articleTitle=Endophenotype-based in silico network medicine discovery combined with insurance record data mining identifies sildenafil as a candidate drug for Alzheimer's disease, refAbstract=null), Reference(id=1209809073663504656, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1016/j.bmc.2010.08.026, pmid=null, pmcid=null, year=2010, volume=18, issue=null, pageStart=6977, pageEnd=6986, url=null, language=null, rfNumber=[22], rfOrder=21, authorNames=Manley P, Stiefl N, Cowan-Jacob S, journalName=Bioorg Med Chem, refType=null, unstructuredReference=
Manley P ,
Stiefl N ,
Cowan-Jacob S et al . Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib[J].
Bioorg Med Chem,
2010,
18: 6977-6986., articleTitle=Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib, refAbstract=null), Reference(id=1209809073822888224, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/jm100395q, pmid=null, pmcid=null, year=2010, volume=53, issue=null, pageStart=4701, pageEnd=4719, url=null, language=null, rfNumber=[23], rfOrder=22, authorNames=Huang WS, Metcalf CA, Sundaramoorthi R, journalName=J Med Chem, refType=null, unstructuredReference=
Huang WS ,
Metcalf CA ,
Sundaramoorthi R et al . Discovery of 3-[2-(imidazo[1, 2-b]pyridazin-3-yl)ethynyl]-4-methyl-
N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant[J].
J Med Chem,
2010,
53: 4701-4719., articleTitle=Discovery of 3-[2-(imidazo[1, 2-b]pyridazin-3-yl)ethynyl]-4-methyl-
N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant, refAbstract=null), Reference(id=1209809074095518002, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, doi=10.1021/jm301581y, pmid=null, pmcid=null, year=2013, volume=56, issue=null, pageStart=879, pageEnd=894, url=null, language=null, rfNumber=[24], rfOrder=23, authorNames=Ren XM, Pan XF, Zhang Z, journalName=J Med Chem, refType=null, unstructuredReference=
Ren XM ,
Pan XF ,
Zhang Z et al . Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinihem[J].
J Med Chem,
2013,
56: 879-894., articleTitle=Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinihem, refAbstract=null)], funds=null, companyList=[AuthorCompany(id=1209809067590152897, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, xref=null, ext=[AuthorCompanyExt(id=1209809067606930114, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, companyId=1209809067590152897, language=EN, country=null, province=null, city=null, postcode=null, companyName=null, departmentName=null, remark=Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China), AuthorCompanyExt(id=1209809067611124419, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, companyId=1209809067590152897, language=CN, country=null, province=null, city=null, postcode=null, companyName=null, departmentName=null, remark=中国医学科学院、北京协和医学院药物研究所, 北京 100050)])], figs=[ArticleFig(id=1209809069687305092, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, language=EN, label=null, caption=null, figureFileSmall=null, figureFileBig=null, tableContent=
| No. | Name | Structure | Target | Company | Approval | Indication |
| 01 | Bicyclol |  | Unknown | Beijing Union Pharmaceutical Factory | 2001-01 | Reducing transaminase in hepatitis patients |
| 02 | Epristeride |  | Steroid type Ⅱ 5α-reductase inhibitor | Jiangsu Lianhuan Pharmaceutical Co. | 2001-01 | Benign prostatic hyperplasia |
| 03 | Butylphthalide |  | Double pore potassium channel inhibitor | China Shiyao Pharmaceutical Group | 2002-09 | Acute ischemic stroke |
| 04 | Sodium glycididazole |  | Unknown | Guangzhou LifeTech Pharmaceutic Co. | 2002-11 | In radiotherapy for solid tumors |
| 05 | Hematoporphyrin |  | Photosensitizer | Chongqing Huading Modern Biopharmaceutics Co. | 2003-09 | Mouth, bladder and other superficial tumors |
| 06 | Tribendimidine |  | Unknown | Shandong Xinhua Pharmaceuticals Co. | 2004-04 | Broad-spectrum intestinal anthelmintic |
| 07 | Boanmycin |  | DNA dependent RNA polymerase inhibitor | Dikang Yaoye | 2004-06 | Head and neck cancer |
| 08 | Allomatrine |  | Unknown | Zhongsheng Phamaceutical Co. | 2005-08 | Malignant trophoblastic tumor |
| 09 | Antofloxacin |  | Topoisomerase II inhibitor | Anhui Globe Pharmaceutical Co. | 2009-04 | Bacterial infections caused chronic bronchitis |
| 10 | Icotinib |  | EGFR inhibitor | Betta Pharmaceuticals Co. | 2011-04 | Advanced or metastatic NSCLC |
| 11 | Imrecoxib |  | COX-2 inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2011-05 | Osteoarthritis pain |
| 12 | Iguratimod |  | NF-κB inhibitor | Sincere | 2011-08 | Nuclear factor NF-κB activation inhibitor |
| 13 | Nimorazole |  | DNA synthase inhibitor | Jiangsu Hansoh Pharmaceutical Group Co. | 2014-02 | Suppurative appendicitis |
| 14 | Allisartan isoproxil |  | Angiotensin II receptor antagonist | Shanghai Allist Pharmaceuticals Co. | 2012-07 | Mild to moderate essential hypertension |
| 15 | Apatinib |  | VEGFR-2 inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2014-12 | Advanced gastric adenocarcinoma |
| 16 | Chidamide |  | HDAC inhibitor | ChipScreen Biosciences | 2014-12 | Peripheral T cell lymphoma |
| 17 | Nemonoxacin |  | Topoisomerase II inhibitor | Zhejiang Medicine Co. | 2016-05 | Bacterial pneumonia |
| 18 | Hemoporfin |  | Photosetical sinsitizer | Shanghai Fudan-Zhangjiang Biopharmaceutical Co. | 2016-12 | Nevus flammeus |
| 19 | Anlotinib |  | VEGFR/PDGFR/FGFR inhibitor | Chia Tai Tianqing Bio-Pharmaceutival Group Co. | 2018-05 | Advanced NSCLC |
| 20 | Albuvirtide |  | HIV fusion inhibitor | Frontier Biotechnologies Inc. | 2018-05 | Aids |
| 21 | Danoprevir |  | NS3/4A protease inhibitor | Ascletis Pharma Inc. | 2018-06 | Hepatitis C |
| 22 | Pyrotinib |  | HER2, EGFR dual inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2018-08 | Metastatic breast cancer |
| 23 | Fruquintinib |  | VEGFR inhibitor | HutchMed | 2018-09 | Colorectal cancer |
| 24 | Benvitimod |  | Cytokine receptor antagonist | Zhonghao Pharmaceutical Co. | 2019-06 | Topical treatment of psoriasis vulgaris |
| 25 | Carrimycin |  | 50S subunit bacterial ribosome | Tonglian Group | 2019-06 | Upper respiratory tract infection |
| 26 | Sodium oligomannate |  | Intestinal flora | Green Valley | 2019-11 | Mild to moderate Alzheimer's disease |
| 27 | Flumatinib |  | Bcr-Abl inhibitor | Hansoh Pharma | 2019-11 | Philadelphia chromosomal positive chronic myeloid leukemia |
| 28 | Remimazolam |  | GABAA receptor antagonist | Jiangsu Hengrui Pharmaceuticals Co. | 2019-11 | A sedative for routine gastroscopy |
| 29 | Coblopasvir |  | NS5A inhibitor | Beijing Kawin Technology Share-Holding Co. | 2020-02 | Chronic hepatitis C in adults |
| 30 | Benzoquinonium bromide |  | M cholinergic receptor antagonist | Silver Valley Pharmaceutical Co. | 2020-03 | Rhinitis-caused runny nose, nasal congestion, nasal itching and sneezing symptoms |
| 31 | Almonertinib |  | EGFR inhibitor | Jiangsu Hansoh Pharmaceutical Group Co. | 1020-03 | Advanced or metastatic NSCLC |
| 32 | Zanubrutinib |  | BTK selective inhibitor | BeiGene | 2020-06 | Chronic lymphocytic leukemia |
| 33 | Ravidasvir |  | NS5A inhibitor | Ascletis Pharma Inc | 2020-07 | Chronic hepatitis C genotype 1B |
| 34 | Edaravone dexborneol |  | Free radical scavenger | Simcere | 2020-07 | Acute ischemic, stroke |
| 35 | Ensartinib |  | ALK inhibitor | Betta Pharmaceuticals Co. | 2920-11 | Advanced or metastatic NSCLC |
| 36 | Fluzoparib |  | PARP inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2020-12 | Recurrent ovarian cancer, fallopian tube cancer |
| 37 | Ciprofol |  | GABAA receptor agonist | Haisco Pharmaceutical Group Co. | 2020-12 | General anesthetic |
| 38 | Yimitasvir |  | NS5A inhibitor | Sunshine Lake Phama Co. | 2020-12 | Chronic hepatitis C |
| 39 | Orelabrutinib |  | BTK inhibitor | InnoCare | 2020-12 | Adult mantle cell lymphoma |
| 40 | Surufatinib |  | VEGFR and FGFR1 inhibitor | HutchMed | 2020-12 | Neuroendocrine tumors of non-pancreatic origin |
| 41 | Savolitinib |  | Met inhibitor | HutchMed | 2021-06 | NSCLC |
| 42 | Pamiparib |  | PARP-1 and -2 inhibitor | BeiGene | 2021-04 | Ovarian, fallopian tube or primary peritoneal cancer |
| 43 | Furmonertinib |  | EGFR intibitor | Shanghai Allist Pharmaceuticals Co. | 2021-03 | NSCLC |
| 44 | Utidelone |  | Promote tubulin polymerization and stabilize microtubule structure | Beijing Biostare | 2021-03 | Breast cancer |
| 45 | Levornidazole disodium |  | Anti anaerobic bacteria | Yangyze River Pharmaceutical Group Co. | 2021-05 | Bacterial infection |
| 46 | Contezolid |  | Inhibition of 70S initiation complex | MicuRx | 2021-06 | Complex skin and soft tissue infections |
| 47 | Donafenib |  | PDGFR, Raf, VEGFR inhibitor | Suzhou Zelgen Biopharmaceuticals Co. | 2021-06 | Unresectable hepatocellular carcinoma |
| 48 | Herombopag |  | Non-peptide TPO-R agonists | Jiangsu Hengrui Pharmaceuticals Co. | 2021-06 | Primary immune thrombocytopenia |
| 49 | Tenofovir amibufenamide |  | Nucleoside reverse transcriptase inhibitors | Jiangsu Hansoh Pharmaceutical Group Co. | 2021-06 | Chronic hepatitis B |
| 50 | Hybutimibe |  | Selective cholesterol absorption inhibitor | Zhejiang Hisun Pharmaceutical Co. | 2021-06 | Hypercholesterolemia |
| 51 | Ainuovirine |  | Non-nucleoside reverse transcriptase inhibitor | Jiangsu Aidea Pharmaceutical Group Co. | 2021-06 | HIV-1 infection in adults |
| 52 | Azvudine |  | Nucleoside reverse transcriptase inhibitor | Henan Genuine Biotech Co. | 2021-07 | HIV-1 infection |
| 53 | Chiglitazar |  | PPAR agonist | ChipScreen Biosciences | 2021-10 | Type 2 diabetes |
| 54 | Olverembatinib |  | Bcr-AblT315I inhibitor | Ascentage Pharma | 2021-11 | CML |
), ArticleFig(id=1209809069867660180, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, language=CN, label=Table 1, caption=
New chemical entities discovered in China and approved by NMPA during 2001-2021
, figureFileSmall=null, figureFileBig=null, tableContent=
| No. | Name | Structure | Target | Company | Approval | Indication |
| 01 | Bicyclol | | Unknown | Beijing Union Pharmaceutical Factory | 2001-01 | Reducing transaminase in hepatitis patients |
| 02 | Epristeride | | Steroid type Ⅱ 5α-reductase inhibitor | Jiangsu Lianhuan Pharmaceutical Co. | 2001-01 | Benign prostatic hyperplasia |
| 03 | Butylphthalide | | Double pore potassium channel inhibitor | China Shiyao Pharmaceutical Group | 2002-09 | Acute ischemic stroke |
| 04 | Sodium glycididazole | | Unknown | Guangzhou LifeTech Pharmaceutic Co. | 2002-11 | In radiotherapy for solid tumors |
| 05 | Hematoporphyrin | | Photosensitizer | Chongqing Huading Modern Biopharmaceutics Co. | 2003-09 | Mouth, bladder and other superficial tumors |
| 06 | Tribendimidine | | Unknown | Shandong Xinhua Pharmaceuticals Co. | 2004-04 | Broad-spectrum intestinal anthelmintic |
| 07 | Boanmycin | | DNA dependent RNA polymerase inhibitor | Dikang Yaoye | 2004-06 | Head and neck cancer |
| 08 | Allomatrine | | Unknown | Zhongsheng Phamaceutical Co. | 2005-08 | Malignant trophoblastic tumor |
| 09 | Antofloxacin | | Topoisomerase II inhibitor | Anhui Globe Pharmaceutical Co. | 2009-04 | Bacterial infections caused chronic bronchitis |
| 10 | Icotinib | | EGFR inhibitor | Betta Pharmaceuticals Co. | 2011-04 | Advanced or metastatic NSCLC |
| 11 | Imrecoxib | | COX-2 inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2011-05 | Osteoarthritis pain |
| 12 | Iguratimod | | NF-κB inhibitor | Sincere | 2011-08 | Nuclear factor NF-κB activation inhibitor |
| 13 | Nimorazole | | DNA synthase inhibitor | Jiangsu Hansoh Pharmaceutical Group Co. | 2014-02 | Suppurative appendicitis |
| 14 | Allisartan isoproxil | | Angiotensin II receptor antagonist | Shanghai Allist Pharmaceuticals Co. | 2012-07 | Mild to moderate essential hypertension |
| 15 | Apatinib | | VEGFR-2 inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2014-12 | Advanced gastric adenocarcinoma |
| 16 | Chidamide | | HDAC inhibitor | ChipScreen Biosciences | 2014-12 | Peripheral T cell lymphoma |
| 17 | Nemonoxacin | | Topoisomerase II inhibitor | Zhejiang Medicine Co. | 2016-05 | Bacterial pneumonia |
| 18 | Hemoporfin | | Photosetical sinsitizer | Shanghai Fudan-Zhangjiang Biopharmaceutical Co. | 2016-12 | Nevus flammeus |
| 19 | Anlotinib | | VEGFR/PDGFR/FGFR inhibitor | Chia Tai Tianqing Bio-Pharmaceutival Group Co. | 2018-05 | Advanced NSCLC |
| 20 | Albuvirtide | | HIV fusion inhibitor | Frontier Biotechnologies Inc. | 2018-05 | Aids |
| 21 | Danoprevir | | NS3/4A protease inhibitor | Ascletis Pharma Inc. | 2018-06 | Hepatitis C |
| 22 | Pyrotinib | | HER2, EGFR dual inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2018-08 | Metastatic breast cancer |
| 23 | Fruquintinib | | VEGFR inhibitor | HutchMed | 2018-09 | Colorectal cancer |
| 24 | Benvitimod | | Cytokine receptor antagonist | Zhonghao Pharmaceutical Co. | 2019-06 | Topical treatment of psoriasis vulgaris |
| 25 | Carrimycin | | 50S subunit bacterial ribosome | Tonglian Group | 2019-06 | Upper respiratory tract infection |
| 26 | Sodium oligomannate | | Intestinal flora | Green Valley | 2019-11 | Mild to moderate Alzheimer's disease |
| 27 | Flumatinib | | Bcr-Abl inhibitor | Hansoh Pharma | 2019-11 | Philadelphia chromosomal positive chronic myeloid leukemia |
| 28 | Remimazolam | | GABAA receptor antagonist | Jiangsu Hengrui Pharmaceuticals Co. | 2019-11 | A sedative for routine gastroscopy |
| 29 | Coblopasvir | | NS5A inhibitor | Beijing Kawin Technology Share-Holding Co. | 2020-02 | Chronic hepatitis C in adults |
| 30 | Benzoquinonium bromide | | M cholinergic receptor antagonist | Silver Valley Pharmaceutical Co. | 2020-03 | Rhinitis-caused runny nose, nasal congestion, nasal itching and sneezing symptoms |
| 31 | Almonertinib | | EGFR inhibitor | Jiangsu Hansoh Pharmaceutical Group Co. | 1020-03 | Advanced or metastatic NSCLC |
| 32 | Zanubrutinib | | BTK selective inhibitor | BeiGene | 2020-06 | Chronic lymphocytic leukemia |
| 33 | Ravidasvir | | NS5A inhibitor | Ascletis Pharma Inc | 2020-07 | Chronic hepatitis C genotype 1B |
| 34 | Edaravone dexborneol | | Free radical scavenger | Simcere | 2020-07 | Acute ischemic, stroke |
| 35 | Ensartinib | | ALK inhibitor | Betta Pharmaceuticals Co. | 2920-11 | Advanced or metastatic NSCLC |
| 36 | Fluzoparib | | PARP inhibitor | Jiangsu Hengrui Pharmaceuticals Co. | 2020-12 | Recurrent ovarian cancer, fallopian tube cancer |
| 37 | Ciprofol | | GABAA receptor agonist | Haisco Pharmaceutical Group Co. | 2020-12 | General anesthetic |
| 38 | Yimitasvir | | NS5A inhibitor | Sunshine Lake Phama Co. | 2020-12 | Chronic hepatitis C |
| 39 | Orelabrutinib | | BTK inhibitor | InnoCare | 2020-12 | Adult mantle cell lymphoma |
| 40 | Surufatinib | | VEGFR and FGFR1 inhibitor | HutchMed | 2020-12 | Neuroendocrine tumors of non-pancreatic origin |
| 41 | Savolitinib | | Met inhibitor | HutchMed | 2021-06 | NSCLC |
| 42 | Pamiparib | | PARP-1 and -2 inhibitor | BeiGene | 2021-04 | Ovarian, fallopian tube or primary peritoneal cancer |
| 43 | Furmonertinib | | EGFR intibitor | Shanghai Allist Pharmaceuticals Co. | 2021-03 | NSCLC |
| 44 | Utidelone | | Promote tubulin polymerization and stabilize microtubule structure | Beijing Biostare | 2021-03 | Breast cancer |
| 45 | Levornidazole disodium | | Anti anaerobic bacteria | Yangyze River Pharmaceutical Group Co. | 2021-05 | Bacterial infection |
| 46 | Contezolid | | Inhibition of 70S initiation complex | MicuRx | 2021-06 | Complex skin and soft tissue infections |
| 47 | Donafenib | | PDGFR, Raf, VEGFR inhibitor | Suzhou Zelgen Biopharmaceuticals Co. | 2021-06 | Unresectable hepatocellular carcinoma |
| 48 | Herombopag | | Non-peptide TPO-R agonists | Jiangsu Hengrui Pharmaceuticals Co. | 2021-06 | Primary immune thrombocytopenia |
| 49 | Tenofovir amibufenamide | | Nucleoside reverse transcriptase inhibitors | Jiangsu Hansoh Pharmaceutical Group Co. | 2021-06 | Chronic hepatitis B |
| 50 | Hybutimibe | | Selective cholesterol absorption inhibitor | Zhejiang Hisun Pharmaceutical Co. | 2021-06 | Hypercholesterolemia |
| 51 | Ainuovirine | | Non-nucleoside reverse transcriptase inhibitor | Jiangsu Aidea Pharmaceutical Group Co. | 2021-06 | HIV-1 infection in adults |
| 52 | Azvudine | | Nucleoside reverse transcriptase inhibitor | Henan Genuine Biotech Co. | 2021-07 | HIV-1 infection |
| 53 | Chiglitazar | | PPAR agonist | ChipScreen Biosciences | 2021-10 | Type 2 diabetes |
| 54 | Olverembatinib | | Bcr-AblT315I inhibitor | Ascentage Pharma | 2021-11 | CML |
), ArticleFig(id=1209809070056403876, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, language=EN, label=null, caption=null, figureFileSmall=null, figureFileBig=null, tableContent=
| Compound | i.v. Administration | | s.c. Administration |
| CL /L·h-1·kg-1 | Vd /L·kg-1 | t1/2 /h | tmax /h | MRT /h | F /% |
| Liraglutide | 0.003 8 | 0.067 4 | 12.4 | | 7 | 23.0 | 66 |
| Semaglutide | 0.001 6 | 0.101 9 | 46.1 | 12 | 63.6 | 94 |
), ArticleFig(id=1209809070215787444, tenantId=1146029695717560320, journalId=1189982191388893191, articleId=1209788326459077145, language=CN, label=Table 2, caption=
Pharmacokinetic evaluation in Gőttingen mini-pigs following administration of semaglutide (27, 2 nmol·kg-1 i.v. or 2 nmol·kg-1 s.c.) and liraglutide (26, 0.5 nmol·kg-1 i.v. or 1.0 nmol·kg-1 s.c.)
, figureFileSmall=null, figureFileBig=null, tableContent=
| Compound | i.v. Administration | | s.c. Administration |
| CL /L·h-1·kg-1 | Vd /L·kg-1 | t1/2 /h | tmax /h | MRT /h | F /% |
| Liraglutide | 0.003 8 | 0.067 4 | 12.4 | | 7 | 23.0 | 66 |
| Semaglutide | 0.001 6 | 0.101 9 | 46.1 | 12 | 63.6 | 94 |
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