临床前CDMO研发筛选相关化合物

CDMO是Contract Development and Manufacturing Organization的缩写，即合同定制研发生产组织。它是一种为制药企业及生物技术公司提供医药（特别是创新药）工艺研发及制备、工艺优化、放大生产、注册和验证批生产以及商业化生产等定制服务的机构. 在传统代工基础上增加了研发和工艺优化能力，是高技术壁垒的工艺研发能力与规模生产能力的深度结合. 1, 工艺开发与优化：创新性合成路线设计、工艺参数优化. 2, 中试放大：实验室工艺向规模化生产的转化 3, 注册批生产：支持客户新药申报的验证批生产. 4, 商业化生产：药品上市后的大规模生产供应. 全球医药CDMO行业保持较高景气度。根据弗若斯特沙利文预测：2026年全球CDMO市场规模：预计达1,189亿美元 2033年全球CDMO市场规模：预计达3,385亿美元. CDMO作为医药产业链专业化分工的产物，已经从单纯的CMO代工模式升级为"研发+生产"一体化的高附加值服务。当前，在多肽、ADC、CGT等新型药物赛道的驱动下，全球及中国CDMO市场保持高速增长。中国CDMO企业凭借完整的供应链体系、工程师红利和一体化服务能力，全球市占率有望持续提升，行业正从"成本优势"竞争迈向"体系优势"竞争的新阶段。
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临床前CDMO研发化合物筛选

CAS: 845614-11-1

Bitopertin

中文名称:比托派汀
CAS号:845614-11-1
分子式: C21H20F7N3O4S 分子量: 543.46
产品形式: free base
研发状态: Enrolling by invitation
研发用途: Erythropoietic Protoporphyria
研究机构: Disc Medicine Inc
研发日期: August 31 2023
研发阶段: Phase 2 : Phase 3
Bitopertin (RG1678,RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.

CAS: 845533-86-0

Bedaquiline fumarate

中文名称:贝达喹啉富马酸盐
CAS号:845533-86-0
分子式: C32H31BrN2O2.C4H4O4 分子量: 671.58
产品形式: fumarate
研发状态: Completed
研发用途: Tuberculosis
研究机构: National Institute of Allergy and Infectious Diseases (NIAID)
研发日期: October 21 2011
研发阶段: Phase 1
Bedaquiline fumarate (TMC-207), an oral diarylquinoline, is a bactericidal antimycobacterial drug. It is a proton-translocating ATP synthetase inhibitor.

CAS: 845272-21-1

Varlitinib

CAS号:845272-21-1
分子式: C22H19ClN6O2S 分子量: 466.94
产品形式: free base
研发状态: Completed
研发用途: Biliary Tract Cancer
研究机构: ASLAN Pharmaceuticals
研发日期: December 19 2017
研发阶段: Phase 2
Varlitinib (ARRY334543) is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.

CAS: 84449-90-1

Raloxifene

中文名称: 雷洛昔芬
CAS号:84449-90-1
分子式: C28H27NO4S 分子量: 473.58
产品形式: Free Base
研发状态: Unknown status
研发用途: Selective Estrogen Receptor Modulator
研究机构: Toshihiko Kono; Tomidahama Hospital
研发日期: Jan-12
研发阶段: --
Raloxifene (Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women.

CAS: 844442-38-2

AT7519

中文名称:西多福韦
CAS号:844442-38-2
分子式: C16H17Cl2N5O2 分子量: 382.24
产品形式: Free Base
研发状态: Completed
研发用途: Multiple Myeloma
研究机构: Astex Pharmaceuticals Inc.; Multiple Myeloma Research Consortium
研发日期: Nov-10
研发阶段: Phase 1 : Phase 2
AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2.

CAS: 84371-65-3

Mifepristone (RU486)

中文名称:米非司酮
CAS号:84371-65-3
分子式: C29H35NO2 分子量: 429.59
产品形式: free base
研发状态: Not yet recruiting
研发用途: Female Contraception
研究机构: Leiden University Medical Center; Karolinska Institutet; Women on Waves; Children''s Investment Fund Foundation
研发日期: Sep-24
研发阶段: Phase 3
Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.