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: 138071-82-6

Gadobutrol

中文名称:钆布醇
CAS号:138071-82-6
分子式: C18H31GdN4O9 分子量: 604.71
产品形式: Free Base
研发状态: Enrolling by invitation
研发用途: Enhancing Brain Lesions
研究机构: Subtle Medical
研发日期: June 16 2023
研发阶段: Phase 1
Gadobutrol (Gadovist, Gadavist,ZK 135079) is a non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is usedfor tissue contrast enhancement in magnetic resonance imaging (MRI).

CAS: 1380575-43-8

Ceritinib dihydrochloride

中文名称:双盐酸盐色瑞替尼
CAS号:1380575-43-8
分子式: C28H38Cl3N5O3S 分子量: 631.06
产品形式: Dihydrochloride
研发状态: Terminated
研发用途: Non-small Cell Lung Cancer
研究机构: University of California San Francisco; Novartis Pharmaceuticals; University of California Davis
研发日期: September 9 2017
研发阶段: Phase 1
Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity.

CAS: 1380288-87-8

Pinometostat (EPZ5676)

中文名称:匹诺司他
CAS号:1380288-87-8
分子式: C30H42N8O3 分子量: 562.71
产品形式: free base
研发状态: Completed
研发用途: Leukemia; Acute Myeloid Leukemia; Acute Lymphocytic Leukemia; Acute Leukemias
研究机构: Epizyme Inc.; Celgene Corporation; Ipsen
研发日期: May-14
研发阶段: Phase 1
Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

CAS: 1380087-89-7

Pelabresib (CPI-0610)

中文名称:BET溴区抑制剂(CPI-0610)
CAS号:1380087-89-7
分子式: C20H16ClN3O2 分子量: 365.81
产品形式: Free Base
研发状态: Completed
研发用途: Advanced Malignancies; Solid Tumor; Hematological Malignancy
研究机构: Constellation Pharmaceuticals
研发日期: July 20 2021
研发阶段: Phase 1
Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

CAS: 137862-53-4

Valsartan (CGP-48933)

中文名称:缬沙坦
CAS号:137862-53-4
分子式: C24H29N5O3 分子量: 435.52
产品形式: free base
研发状态: Recruiting
研发用途: Heart Failure With Reduced Ejection Fraction
研究机构: Universidade do Porto; Unidade de Investigação e Desenvolvimento Cardiovascular (UnIC); Rede de Investigação em Saúde
研发日期: August 4 2023
研发阶段: Phase 4
Valsartan (CGP-48933) is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.

CAS: 1377239-83-2

PBTZ169

中文名称:2-(4-(环己基甲基)哌嗪-1-基)-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮
CAS号:1377239-83-2
分子式: C20H23F3N4O3S 分子量: 456.48
产品形式: Free base
研发状态: Completed
研发用途: Tuberculosis Pulmonary
研究机构: Innovative Medicines for Tuberculosis; Bill and Melinda Gates Foundation
研发日期: February 21 2019
研发阶段: Phase 1
PBTZ169 (macozinone), an antibiotic with antimycobacterial activity, is an irreversible inhibitor of DprE1.