常见分子靶向药物治疗推荐.pptVIP

* * Sunitinib malate 顯示能強力抑制所有已知的 PDGF 和 VEGF 受體、KIT、FLT3 和 RET 所介入的多 RTKs。 Sunitinib malate 在低濃度（nanomolar）也能抑制這些受體，顯示其活性強度相當高 Sunitinib malate 能直接和間接地抑制多種腫瘤類型的成長，因為它有抗腫瘤和抗血管增生的活性作用。 * The human epidermal growth factor family of receptors consists of 4 transmembrane proteins with different properties (HER1-4), all involved in regulation of cell proliferation and survival.1-5 The prototype HER member HER1/EGFR (Erb-B1) binds a variety of growth factors, with ligand binding activating tyrosine kinase activity within the cytoplasmic domain and through various signal transduction intermediates.1 HER2 has no known ligand-binding activity, but its tyrosine-kinase activity is transactivated through HER2 interaction with other HER members (heterodimerization), usually following ligand binding to those receptors.3 The HER2 extracellular domains are fixed in an open conformation (exposed domain II loop) that resembles a ligand-activated state, and thus HER2 can constitutively interact functionally with other HER members.6 HER3 lacks inherent tyrosine kinase activity, but ligand binding promotes HER heterodimerization, resulting in complexes (eg, HER2/HER3) with highly proliferative signaling activity.2,4 The HER signaling network, mediated by these receptor interactions, stimulates and regulates not only cell proliferation, but also mobility, adhesion and survival.4,5 The activity of HER2/HER4 dimers is unclear, but may be implicated in providing survival signals to cardiomyocytes.4,5 1. Ritter and Arteaga. Semin Oncol. 2003;30(suppl 1):3. 2. Hung and Lau. Semin Oncol. 1999;26(suppl 12):51. 3. Tzahar and Yarden. Biochim Biophys Acta. 1998;1377:M25. 4. Pinkas-Kramarski et al. EMBO J. 1996;15:2452. 5. Zhao et al. J Biol Chem. 1998;273:10261. 6. Cho et al. Nature. 2003;421:756. * * 手足皮肤反应是指手足部位出现麻木感、烧灼感、红斑、肿胀、皮肤变硬或者起茧、起疱、发干、脱屑及皲裂等，在手足的受力区往往症状更严重。通常在双侧发生，出现于治疗的前6周，尤其是前1-2周。 * 改善手足皮肤反应症状的处理方法，包括： 穿棉袜或软垫 用硫酸镁浸泡皮肤患处 使用含尿素的软膏或乳液涂抹患处 使用芦荟汁涂抹患处 请足疗师治疗 严重者药物减量或暂停 典型的是，重新开始治疗时手足皮