权益分类	功能权益	普通用户	{{item.name}}会员
{{category.name}}	{{benefitItem.name}}

Selective Matrix Metalloproteinase Inhibitors For Osteoarthritis

用于骨关节炎的选择性基质金属蛋白酶抑制剂

基本信息

批准号：
8383774
负责人：
IRVING SUCHOLEIKI
金额：
$ 37.4万
依托单位：
AQUILUS PHARMACEUTICALS, INC.
依托单位国家：
美国
项目类别：
财政年份：
2012
资助国家：
美国
起止时间：
2012-09-01 至 2014-08-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8383774
关键词：
Accounting Acetaminophen Address Affect Arthralgia Arthritis Biological Availability Cartilage Clinic Degenerative polyarthritis Diagnosis Disease Disease Progression Dose Drug Kinetics Drug Prescriptions Exhibits Gait Gelatinase A Goals Injury Institutes Intravenous Joints Knee joint Marketing Matrix Metalloproteinase Inhibitor Medial Modeling Musculoskeletal Diseases Musculoskeletal System National Institute of Arthritis and Musculoskeletal and Skin Diseases Non-Steroidal Anti-Inflammatory Agents Office Visits Operative Surgical Procedures Oral Oral Administration Pain Pain management Pharmaceutical Preparations Pharmacologic Substance Phase Plasma Primary Care Physician Proteins Public Health Rattus Reading Replacement Arthroplasty Research Rodent Rodent Model Running Series Small Business Innovation Research Grant Staining method Stains Synvisc Testing Tissues Tolonium chloride Visual Work allodynia animal efficacy animal pain collagenase 3 disorder prevention gait examination improved inhibitor/antagonist male novel osteochondral tissue scale up skin disorder

项目摘要

DESCRIPTION (provided by applicant): Aquilus Pharmaceuticals, Inc. proposes to evaluate the effects of two novel matrix metalloproteinase (MMP) inhibitors in both the medial meniscal tear (MMT) and monoiodoacetate (MIA) rat models of osteoarthritis (OA) with pain read-outs. The goals for Phase I are to scale-up the synthesis of the allosteric, MMP-13 and dual active MMP-2/-9 inhibitors, determine their pharmacokinetics (PK) and run animal efficacy studies in both the MMT and MIA-rat models of OA. The ultimate goal of the proposed work is to evaluate whether a selective MMP inhibitor can be developed for the treatment of OA. PUBLIC HEALTH RELEVANCE: Osteoarthritis (OA) affects an estimated 20 million people and accounts for roughly 25% of office visits to primary care physicians and half of all nonsteroidal anti-inflammatory drug (NSAID) prescriptions for pain. Within the OA pain therapy market there remains a substantial unmet need for drugs that not only reduce joint pain but also treat the disease itself. Currently, there are no diseases modifying drugs in the market to treat Osteoarthritc pain. Aquilus Pharmaceuticals will test a series of highly potent inhibitors of proteins responsible for cartilage degradation in two OA animal pain models. If successful, Aquilus Pharmaceuticals will be able to rapidly bring to the clinic a first in class drug that not only can reduce pain associated with OA but also possibly halt or slow down the disease progression and the eventual need for joint replacement surgery.

描述（由申请人提供）：Aquilus Pharmaceuticals，Inc.提出评估两种新型基质金属蛋白酶（MMP）抑制剂在内侧膝关节撕裂（MMT）和单碘乙酸盐（MIA）骨关节炎（OA）大鼠模型中的作用，并伴有疼痛读数。I期的目标是扩大变构、MMP-13和双重活性MMP-2/-9抑制剂的合成，确定它们的药代动力学（PK），并在MMT和MIA-大鼠OA模型中进行动物疗效研究。拟议工作的最终目标是评估是否可以开发一种选择性MMP抑制剂用于治疗OA。公共卫生相关性：骨关节炎（OA）影响估计2000万人，约占初级保健医生办公室就诊的25%，占所有非甾体抗炎药（NSAID）疼痛处方的一半。在OA疼痛治疗市场中，对于不仅减轻关节疼痛而且治疗疾病本身的药物仍然存在大量未满足的需求。目前，市场上没有治疗骨关节炎疼痛的疾病修饰药物。Aquilus制药公司将在两种OA动物疼痛模型中测试一系列负责软骨降解的蛋白质的高效抑制剂。如果成功，Aquilus制药公司将能够迅速为临床带来一流的药物，不仅可以减少与OA相关的疼痛，还可能阻止或减缓疾病进展，并最终需要关节置换手术。