广东化工2023年第6期·82·www.gdchem.com第50卷总第488期奥希替尼药物临床研究进展鲁美琦1,2,窦鹏挥2*,王振3,李林芮1,2(1.佳木斯大学,黑龙江佳木斯154000;2.佳木斯大学附属第一医院放化疗科,黑龙江佳木斯154000;3.哈尔滨医科大学,黑龙江哈尔滨150000)[摘要]奥希替尼作为靶向药物的一种,是表皮生长因子受体基因(epidermalgrowthfactorreceptorEGFR)突变阳性的肺癌患者的第三代特异性酪氨酸激酶抑制剂。它因特异性强,不良反应少等优点,在治疗表皮生长因子受体基因突变阳性的肺癌患者过程中,表现出惊人的治疗效果,使患者的无进展生存期显著延长。本文将从奥希替尼的化学物理性质、化学药理作用、药代动力学、化学作用机制及临床应用等五个方面对其在肺癌的研究进展进行论述。[关键词]非小细胞肺癌;靶向治疗;EGFR突变;酪氨酸激酶抑制剂[中图分类号]TQ[文献标识码]A[文章编号]1007-1865(2023)06-0082-03AdvancesinClinicalResearchofOximertinibLuMeiqi1,2,DouPenghui2*,WangZhen3,LiLinrui1,2(1.JiamusiUniversity,Jiamusi154000;2.DepartmentofRadiotherapyandChemotherapy,theFirstAffiliatedHospitalofJiamusiUniversity,Jiamusi154000;3.HarbinMedicalUniversity,Harbin150000,China)Abstract:Asoneofthetargeteddrugs,oximertinibisthethirdgenerationspecifictyrosinekinaseinhibitoroflungcancerpatientswithpositivemutationsofepidermalgrowthfactorreceptorgene.Becauseofitsstrongspecificityandfewadversereactions,ithasshownamazingtherapeuticeffectsinthetreatmentoflungcancerpatientswithpositivemutationsofepidermalgrowthfactorreceptorgene,andsignificantlyprolongedtheprogressionfreesurvivalperiodofpatients.Thisarticlewilldiscusstheresearchprogressofoximertinibinlungcancerfromfiveaspects:chemicalandphysicalproperties,chemicalandpharmacologicaleffects,pharmacokinetics,chemicalmechanismofactionandclinicalapplication.Keywords:non-smallcelllungcancer;targetingtherapy;EGFRmutation;tyrosinekinaseinhibitors1奥希替尼药物化学成分理化性质及特点甲磺酸奥希替尼片(商品名称:泰瑞沙),化学名称为N-(2-{2-二甲氨基乙基-甲氨基}-4-甲氧基-5-{[4-(1-甲基-1H-吲哚-3-基)嘧啶-2-基]氨基}苯基)-2-丙烯酰胺,分子式:C28H33N7O2,分子量为426。甲磺酸奥希替尼片的活性成分是甲磺酸奥...