pharmacodynamics

Oritinib (SH-1028) 是一种 EGFR 抑制剂，对 EGFR (wt)、EGFR (L858R)、EGFR (L861Q)、EGFR (L858R/T790M)、EGFR (d746-750) 的 IC50 分别为 18、0.7、4、0.1、1.4 和 0.89 nM , EGFR (d746-750/T790M), 分别。奥瑞替尼可用于治疗非小细胞肺癌的研究。

N-desmethyl Enzalutamide (N-desmethyl MDV 3100) 是一种 Enzalutamide 的主要活性代谢物，具有与 Enzalutamide 相似的一级和二级药效功效，并在与 Enzalutamide 大致相同的血浆浓度下循环。

Ivacaftor-D9 是Ivacaftor的氘代化合物，可用于同位素示踪。Ivacaftor是一种有效和可口服的CFTR 调节剂，可应用于囊性纤维化相关的机制与药效研究。

BMS-344577, a lactam derivative based on arylguanidine, is a potent oral active FXA inhibitor with excellent susceptibility in vitro, good pharmacokinetics, and pharmacodynamics in animal models.

Edoxaban impurity 6 is an impurity of Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention[1][2]. [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.[2]. Mendell J, Lee F, Chen S, The Effects of the Antiplatelet Agents, Aspirin and Naproxen, on Pharmacokinetics and Pharmacodynamics of the Anticoagulant Edoxaban, a Direct Factor Xa Inhibitor. J Cardiovasc Pharmacol. 2013 Apr 23.

Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853

Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrolyzing to pharmacologically active MLN2238 (ixazomib), is a next-generation proteasome inhibitor with demonstrated preclinical and clinical antimyeloma activity. MLN9708, compared with bortezomib, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinical studies.

The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double-blind, multicentre, Phase Ib study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical efficacy of the selective SYK inhibitor GSK2646264 in active CLE lesions

NNMT-IN-4（compound 38），一种选择性、非竞争性且具有膜通透性的烟酰胺N-甲基转移酶（NNMT）抑制剂，在体外生化及细胞实验中的IC50值为42 nM和38 nM。该抑制剂展现出良好的PK/PD关系和安全性，同时具备优秀的口服生物利用度和药物制剂性质，适合作为NNMT活性研究的体内化学探针。

Crefmirlimab (IAB22M2C) 是一种人源化抗 CD8 单克隆抗体片段 (minibody)，专为 PET成像 而设计。该产物能以高亲和力特异性结合 CD8+ T 细胞表面的 CD8 受体，当其被放射性核素（如 89Zr）标记后，可作为 无创影像学生物标志物，用于在临床前模型和临床研究中实时、动态地追踪体内T细胞（特别是CD8+ T细胞）的分布、浸润及迁移。它是评估T细胞衔接疗法（如GUCY2C-CD3双抗PF-07062119）药效动力学和研究肿瘤免疫微环境的关键工具

Anti-CD20 Antibody (mAb 1.5.3) 是一种全人源IgG1抗体，能够在体外增强促细胞凋亡 (apoptosis) 活性，并介导补体依赖性细胞毒作用和抗体依赖性细胞毒作用。在各种肿瘤异种移植模型中，Anti-CD20 Antibody (mAb 1.5.3) 展示了优异的抗肿瘤活性。此外，在灵长类药效动力学模型中，尤其是在淋巴结和骨髓中，该抗体表现出显著的B细胞耗竭特性。Anti-CD20 Antibody (mAb 1.5.3) 适用于B细胞恶性肿瘤的研究。