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Chemical Optimization Designed to Increase the in vivo Efficacy of HM-27 for the

旨在提高 HM-27 体内功效的化学优化

基本信息

批准号：
8395611
负责人：
Lori A Hazlehurst
金额：
$ 15.62万
依托单位：
MODULATION THERAPEUTICS, 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 2013-08-28
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8395611
关键词：
Affinity Amino Acid Sequence Antibodies Antineoplastic Agents Apoptotic Binding Biological Assay Biological Availability Biological Markers Biotin Bone Diseases Bone Marrow Businesses CD44 gene Cancer Center Cell Death Cell Line Cell membrane Cells Characteristics Chemicals Clinical Clinical Data Clinical Research Clinical Trials Collaborations Collecting Cell Data Development Doctor of Pharmacy Dose Drug Kinetics Employee Extracellular Domain FDA approved Fibronectins Funding Goals Grant Half-Life Hematologic Neoplasms Hematopoietic Home environment Homing Human Immune Implant In Vitro Inhibitory Concentration 50 Label Laboratories Lead Length Licensing MSX1 gene Malignant - descriptor Malignant Neoplasms Measurement Measures Mediation Melphalan Modeling Multiple Myeloma Mus Necrosis Normal Cell Pathway interactions Patients Peptide Hydrolases Peptide Sequence Determination Peptides Pharmaceutical Preparations Pharmacodynamics Pharmacologic Substance Phase Phase I Clinical Trials Reagent Recombinants Relapse Request for Applications Research Personnel Resistance Route Safety Site Solid Neoplasm Surface Surface Plasmon Resonance Technology Testing Therapeutic Therapeutic Uses Toxic effect Variant analog arm cell killing cell stroma clinical efficacy commercialization design drug candidate improved in vitro Assay in vivo killings loris novel peptide analog peptidomimetics pre-clinical protein protein interaction scaffold small molecule tumor tumor growth

项目摘要

DESCRIPTION (provided by applicant): This application requests funds to aid in obtaining the necessary additional preclinical data needed for commercialization of a promising new and novel drug candidate for the treatment of multiple myeloma. A small business, Modulation Therapeutics Incorporated, has licensed this technology from the Moffitt Cancer Center and its employee, Dr. Priyesh Jain, in collaboration with Dr. Mark McLaughlin and Dr. Lori Hazlehurst at Moffitt Cancer Center and aided by co-investigator Richard Lush, PharmD, are proposing to synthesize analogs expected to have better bioavailability and that improve or maintain direct binding affinities for CD44 and in vitro IC50 activity. We will measure preliminary PK studies, and confirmatory in vitro and in vivo 5TGM1 MM tumor growth inhibition studies in Phase 1 of the grant. PUBLIC HEALTH RELEVANCE: This application requests funds to aid a new small business, Modulation Therapeutics Incorporated, in obtaining the necessary additional pre-clinical data needed for commercialization of a promising new and novel drug candidate for the treatment of multiple myeloma. The new drug candidate kills human multiple myeloma tumors, the second most common hematological malignancy in humans, in immune-compromised mice implanted with the human tumor at does that show no obvious toxicity to the mice.

描述(由申请人提供)：本申请请求资金，以帮助获得必要的额外临床前数据，以商业化一种有前途的治疗多发性骨髓瘤的新药候选药物。一家小型企业，调制治疗公司，已经从莫菲特癌症中心及其员工Priyesh Jain博士那里获得了这项技术的许可，与Moffitt癌症中心的Mark McLaughlin博士和Lori Hazlehurst博士合作，并在共同研究员Richard Lush的帮助下，PharmD正在提议合成有望具有更好生物利用度的类似物，这些类似物可以改善或保持与CD44的直接结合亲和力和体外IC50活性。我们将在拨款的第一阶段测量初步的PK研究，并在体外和体内进行5TGM1 MM肿瘤生长抑制的确证研究。公共卫生相关性：这项申请请求资金帮助一家新的小型企业，调制治疗公司，获得必要的额外临床前数据，以商业化一种有前途的治疗多发性骨髓瘤的新药和新药。这种新的候选药物可以在免疫功能低下的小鼠体内杀死人类多发性骨髓瘤肿瘤，这种肿瘤是人类第二常见的血液系统恶性肿瘤，植入这种肿瘤对小鼠没有明显的毒性。