The problem of antimalarial resistance and its implications for drug discovery.

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Thomas Martin Schäfer, Lais Pessanha de Carvalho, Juliana Inoue, Andrea Kreidenweiss, Jana Held
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引用次数: 0

Abstract

Introduction: Malaria remains a devastating infectious disease with hundreds of thousands of casualties each year. Antimalarial drug resistance has been a threat to malaria control and elimination for many decades and is still of concern today. Despite the continued effectiveness of current first-line treatments, namely artemisinin-based combination therapies, the emergence of drug-resistant parasites in Southeast Asia and even more alarmingly the occurrence of resistance mutations in Africa is of great concern and requires immediate attention.

Areas covered: A comprehensive overview of the mechanisms underlying the acquisition of drug resistance in Plasmodium falciparum is given. Understanding these processes provides valuable insights that can be harnessed for the development and selection of novel antimalarials with reduced resistance potential. Additionally, strategies to mitigate resistance to antimalarial compounds on the short term by using approved drugs are discussed.

Expert opinion: While employing strategies that utilize already approved drugs may offer a prompt and cost-effective approach to counter antimalarial drug resistance, it is crucial to recognize that only continuous efforts into the development of novel antimalarial drugs can ensure the successful treatment of malaria in the future. Incorporating resistance propensity assessment during this developmental process will increase the likelihood of effective and enduring malaria treatments.

抗疟药物抗药性问题及其对药物研发的影响。
导言:疟疾仍然是一种毁灭性传染病,每年造成数十万人死亡。几十年来,抗疟药物的抗药性一直威胁着疟疾的控制和消除,如今仍然令人担忧。尽管目前的一线治疗(即青蒿素类复方疗法)依然有效,但东南亚出现的抗药性寄生虫以及非洲出现的更令人震惊的抗药性突变,令人深感忧虑,需要立即引起重视:全面概述了恶性疟原虫获得抗药性的机制。对这些过程的了解提供了宝贵的见解,可用于开发和选择抗药性可能性较低的新型抗疟药物。此外,还讨论了通过使用已获批准的药物在短期内减轻抗疟药物抗药性的策略:专家观点:虽然采用使用已获批准药物的策略可以迅速、经济有效地解决抗疟药物耐药性问题,但必须认识到,只有不断努力开发新型抗疟药物,才能确保今后成功治疗疟疾。在这一研发过程中纳入抗药性倾向评估,将增加有效和持久治疗疟疾的可能性。
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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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