Preclinical development of novel small molecule malaria drugs that overcome drug

克服药物障碍的新型小分子疟疾药物的临床前开发

• 批准号: 8647555
• 负责人: DAVID H PEYTON
• 金额: $ 98.91万
• 依托单位: DESIGNMEDIX, INC.
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-09-01 至 2017-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8647555
• 关键词: Abbreviations; Antimalarials; Artemisinins; Award; Back; Carrier Proteins; Child; Chloroquine; Chloroquine resistance; Clinical Research; Clinical Trials; Combined Modality Therapy; Development; Disease; Dose; Drug Kinetics; Drug resistance; Ethers; Evaluation; Failure; Funding; Gene Proteins; Goals; Gold; Health; Human; Hybrids; In Vitro; Inhibitory Concentration 50; Institutes; Intravenous; Investigational Drugs; Lead; Lethal Dose 50; Link; Malaria; Monkeys; Multi-Drug Resistance; Mutate; Neuraxis; Oral; Parasites; Pathway interactions; Pharmaceutical Preparations; Pharmacodynamics; Pharmacologic Substance; Pharmacology; Phase; Plasmodium falciparum; Positioning Attribute; Preclinical Drug Development; Preclinical Testing; Predisposition; Pregnant Women; Property; Rattus; Research Contracts; Resistance; Small Business Technology Transfer Research; Staging; Structure-Activity Relationship; Toxic effect; Tropical Disease; Universities; Vacuole; Verapamil; artemisinine; base; chemosensitizing agent; design; drug candidate; drug development; flexibility; forgetting; in vivo; innovation; killings; microbial alkaline proteinase inhibitor; novel; pre-clinical; preclinical evaluation; preclinical study; public health relevance; research clinical testing; resistant strain; response; small molecule; trait; vaccine development

DESCRIPTION (provided by applicant): The worldwide health problem created by malaria has been made more difficult by the spread of drug- resistant parasites. We have developed an orally available and inexpensive class of novel drugs that act against both chloroquine-resistant and chloroquine-sensitive malaria. This project carries on preclinical development of a drug candidate that has been selected from this innovative class of potent antimalarials designed to overcome drug resistance. The candidate will be advanced through the ultimate stages of preclinical testing. Thus, pharmacokinetics, pharmacodynamics, pharmacology, and toxicity evaluations will be performed in both rats and monkeys. The overall goal will be completion of preclinical studies leading to approval of an Investigative New Drug (IND) application for the drug to be used in a Phase 1 human clinical trial.

描述（由申请人提供）：由于耐药寄生虫的传播，疟疾造成的全球健康问题变得更加困难。我们开发了一种可口服且价格低廉的新型药物，对氯喹耐药疟疾和氯喹敏感疟疾都起作用。该项目进行一种候选药物的临床前开发，该候选药物是从这类创新的强效抗疟药中挑选出来的，旨在克服耐药性。候选人将通过临床前测试的最后阶段。因此，将在大鼠和猴子身上进行药代动力学、药效学、药理学和毒性评估。总体目标将是完成临床前研究，从而批准调查性新药（IND）申请，用于1期人体临床试验。