Novartis Institutes for BioMedical Research, Inc., Infectious Diseases, Cambridge, MA 02139, USA.
Expert Opin Investig Drugs. 2010 Jan;19(1):1-21. doi: 10.1517/13543780903473150.
Of the many drugs dropped from development in 2008, 27 were under development for therapy or prophylaxis of infectious diseases. The majority of these were for diseases of viral etiology (15 agents), while nine were antibacterials and the remaining three were directed against fungal and protozoan pathogens. The antiviral agents were primarily against HIV and hepatitis C virus, together with agents against hepatitis B virus and West Nile virus. The antibacterial agents were mostly from known classes (carbapenems, fluoroquinolones, oxazolidinones), but also included several novel compounds and approaches. With regard to drug type, 19 were small-molecule therapeutics, seven were biologics comprising five vaccines and two antibodies, and one was a high-molecular-weight polymer. Each of these agents is briefly reviewed and the reasons for failure are discussed.
在 2008 年停止研发的众多药物中,有 27 种处于传染病治疗或预防药物的研发阶段。其中大多数是针对病毒性病因的疾病(15 种制剂),9 种是抗菌药物,其余 3 种针对真菌和原生动物病原体。抗病毒药物主要针对 HIV 和丙型肝炎病毒,以及乙型肝炎病毒和西尼罗河病毒的药物。抗菌药物主要来自已知类别(碳青霉烯类、氟喹诺酮类、恶唑烷酮类),但也包括几种新型化合物和方法。就药物类型而言,有 19 种是小分子治疗药物,7 种是生物制剂,包括 5 种疫苗和 2 种抗体,还有 1 种是高分子聚合物。简要综述了每种药物,并讨论了失败的原因。