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: 168555-66-6

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

中文名称:康普瑞汀磷酸二钠
CAS号:168555-66-6
分子式: C18H19O8P.2Na 分子量: 440.29
产品形式: Disodium salt
研发状态: Terminated
研发用途: Platinum Resistant Ovarian Cancer
研究机构: Mateon Therapeutics
研发日期: Jun-16
研发阶段: Phase 2 : Phase 3
Fosbretabulin (Combretastatin A4 Phosphate, CA4P, CA 4DP) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Fosbretabulin disodium induces mitotic arrest and apoptosis in endothelial cells. Phase 3.

CAS: 168316-95-8

Spinosad

中文名称:多杀菌素
CAS号:168316-95-8
分子式: C41H65NO10 分子量: 731.96
产品形式: free base
研发状态: Completed
研发用途: Scabies
研究机构: ParaPRO LLC; Concentrics Research
研发日期: May 2 2017
研发阶段: Phase 3
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete, is a biological neurotoxic insecticide with a broader action spectrum, targeting the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system.

CAS: 168273-06-1

Rimonabant (SR141716)

中文名称: 利莫纳班
CAS号:168273-06-1
分子式: C22H21Cl3N4O 分子量: 463.79
产品形式: free base
研发状态: Completed
研发用途: Pain
研究机构: University Hospital Clermont-Ferrand
研发日期: Sep-08
研发阶段: Phase 1
Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.

CAS: 1681017-83-3

Venadaparib(IDX-1197)

CAS号:1681017-83-3
分子式: C23H23FN4O2 分子量: 406.45
产品形式: free base
研发状态: Completed
研发用途: Healthy Male
研究机构: Idience Co. Ltd.
研发日期: January 16 2022
研发阶段: Phase 1
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.

CAS: 168079-32-1

Lixivaptan (VPA-985)

中文名称:利赛伐坦
CAS号:168079-32-1
分子式: C27H21ClFN3O2 分子量: 473.93
产品形式: Free base
研发状态: Terminated
研发用途: Polycystic Kidney Disease Adult
研究机构: Palladio Biosciences; Centessa Pharmaceuticals plc
研发日期: February 10 2022
研发阶段: Phase 3
Lixivaptan (VPA-985, CRTX 080, WAY VPA 985) is an oral, non-peptide, selective V2 receptor vasopressin antagonist with IC50s of 1.2 nM and 2.3 nM for human V2 receptor and rat V2 receptor, respectively.

CAS: 167933-07-5

Flibanserin

中文名称: 氟立班丝氨
CAS号:167933-07-5
分子式: C20H21F3N4O 分子量: 390.40
产品形式: free base
研发状态: Active not recruiting
研发用途: Breast Cancer; Hyposexual Desire Disorder
研究机构: Memorial Sloan Kettering Cancer Center
研发日期: September 14 2018
研发阶段: --
Flibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.