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: 850879-09-3

Amuvatinib (MP-470)

中文名称:N-(1,3-苯并二氧戊环-5-基甲基)-4-苯并呋喃并[3,2-d]嘧啶-4-基-1-哌嗪硫代甲酰胺
CAS号:850879-09-3
分子式: C23H21N5O3S 分子量: 447.51
产品形式: free base
研发状态: Completed
研发用途: Small Cell Lung Carcinoma
研究机构: Astex Pharmaceuticals Inc.
研发日期: May-11
研发阶段: Phase 2
Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.

CAS: 850876-88-9

Danoprevir (ITMN-191)

中文名称:丹诺普韦
CAS号:850876-88-9
分子式: C35H46FN5O9S 分子量: 731.83
产品形式: free base
研发状态: Completed
研发用途: Healthy Volunteer
研究机构: Hoffmann-La Roche
研发日期: Nov-12
研发阶段: Phase 1
Danoprevir (ITMN-191, RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.

CAS: 850649-62-6

Alogliptin (SYR-322) benzoate

中文名称:阿格列汀苯甲酸盐
CAS号:850649-62-6
分子式: C18H21N5O2.C7H6O2 分子量: 461.51
产品形式: benzoate
研发状态: Completed
研发用途: Healthy Volunteers
研究机构: Takeda
研发日期: May 26 2018
研发阶段: Phase 1
Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.

CAS: 850649-61-5

Alogliptin

中文名称: 阿格列汀
CAS号:850649-61-5
分子式: C18H21N5O2 分子量: 339.39
产品形式: Dipeptidyl Peptidase-4
研发状态: Completed
研发用途: Healthy Volunteers
研究机构: Takeda
研发日期: May 26 2018
研发阶段: Phase 1
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.

CAS: 850140-73-7

Afatinib (BIBW2992) Dimaleate

中文名称:双马来酸盐阿法替尼
CAS号:850140-73-7
分子式: C24H25ClFN5O3.2C4H4O4 分子量: 717.18
产品形式: Dimaleate
研发状态: Recruiting
研发用途: Advanced Solid Tumor; Unresectable Solid Tumor; Metastatic Solid Tumor; Cholangiocarcinoma
研究机构: Massachusetts General Hospital; Boehringer Ingelheim; Incyte Corporation
研发日期: July 1 2024
研发阶段: Phase 1
Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.

CAS: 850140-72-6

Afatinib (BIBW2992)

中文名称:阿法蒂尼(BIBW2992)
CAS号:850140-72-6
分子式: C24H25ClFN5O3 分子量: 485.94
产品形式: Free Base
研发状态: Recruiting
研发用途: Advanced Solid Tumor; Unresectable Solid Tumor; Metastatic Solid Tumor; Cholangiocarcinoma
研究机构: Massachusetts General Hospital; Boehringer Ingelheim; Incyte Corporation
研发日期: July 1 2024
研发阶段: Phase 1
Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.