免疫抑制剂
免疫抑制剂是一类能够降低免疫反应的药物，它们能选择性地作用于特定的免疫反应环节或免疫细胞。免疫是指机体对各种致病物质的反应，这种反应可能对身体有益，增强抵抗力；也可能有害，导致生理机能紊乱或组织损伤（变态反应）。因此，为了减少那些有害的变态反应，我们使用免疫抑制剂来影响免疫过程的相关环节，从而降低机体的免疫反应性。随着治疗各种免疫性疾病和减弱组织不相容性的需求，多种免疫抑制剂已得到发展，并广泛应用于临床。
这些药物种类繁多，常用的包括糖皮质激素类（如泼尼松、氢化泼尼松等）、氮芥类化合物（如环磷酰胺、噻替派、白消安等）和抗代谢药物（如6-巯基嘌呤、硫唑嘌呤、氨甲蝶呤等）。
1. 糖皮质激素糖皮质激素是常用的免疫抑制剂，包括可的松、氢化可的松以及半人工合成的泼尼松（强的松）、氢化泼尼松（强的松龙）、氟美松（地塞米松）等。这类药物主要通过以下机制发挥其免疫抑制作用：①抑制单核吞噬细胞系统的吞噬功能，干扰巨噬细胞的功能；②破坏淋巴组织，尤其是淋巴结的生发中心最为敏感。虽然在异体抗原刺激后常用剂量对抗体合成的抑制不明显，但能显著抑制自身抗体的产生。
糖皮质激素的应用范围很广，主要包括：①治疗自身免疫性疾病如类风湿性关节炎、系统性红斑狼疮、结节性动脉周围炎、皮肌炎、硬皮病和肾病综合征等；②用于组织或器官移植；③治疗过敏性疾病如支气管哮喘、过敏性休克及血管神经性水肿等。
2. 硫唑嘌呤硫唑嘌呤能抑制杀伤细胞和T细胞介导的各种免疫反应（包括混合淋巴细胞反应、异体移植物排斥反应和迟发型超敏反应）。大剂量时，它还能抑制抗体的形成。对原发性免疫反应的抑制作用强于继发性反应，并强烈抑制单核细胞的产生，从而影响吞噬功能；此外，也能改变淋巴细胞的再循环。
临床常用于肾移植患者，并常与皮质甾体类药物联合治疗自身免疫性疾病。
3. 环磷酰胺环磷酰胺是一种选择性的B细胞抑制剂，能抑制各类抗原诱发的抗体合成（包括原发和继发的免疫反应），以及诱导机体对抗原产生耐受性。其主要通过溶解淋巴细胞发挥体液免疫抑制作用。一次注射即可显著减少脾脏、淋巴结等淋巴组织中的细胞数及血中淋巴细胞数。
环磷酰胺对未成熟的细胞有较强的作用，可抑制其增殖能力；但成熟的抗体形成细胞对此不敏感。研究还发现，它能强烈抑制移植物抗宿主反应和迟发型超敏反应，但在致敏前给药却能促进迟发型超敏反应。
在体外环磷酰胺无作用，在体内代谢后才起效。临床上主要用于治疗皮质甾体类药物无效的多种自身免疫性疾病、降低自身抗体滴度以及延长移植器官的存活时间。
| 中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
|---|---|---|---|---|
| 霉酚酸 | mycophenolic acid | 24280-93-1 | C17H20O6 |
|
| 萘莫司他 | nafamostat | 81525-10-2 | C19H17N5O2 |
|
| 莱博雷生 | lemborexant | 1369764-02-2 | C22H20F2N4O2 |
|
| 羟基脲 | N-hydroxyurea | 127-07-1 | CH4N2O2 |
|
| 维利帕尼盐酸盐 | Veliparib dihydrochloride | 912445-05-7 | C13H18Cl2N4O |
|
| 硫唑嘌呤 | Azathioprin | 446-86-6 | C9H7N7O2S |
|
| 环磷酰胺一水合物 | cyclophosphamide | 6055-19-2 | C7H15Cl2N2O2P*H2O |
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| 环磷酰胺 | cyclophosphamide | 50-18-0 | C7H15Cl2N2O2P |
|
| 异环磷酰胺 | ilfosfamide | 3778-73-2 | C7H15Cl2N2O2P |
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| 吡美莫司 | pimecrolimus | 137071-32-0 | C43H68ClNO11 |
|
| 他克莫司 | Tacrolimus | 104987-11-3 | C44H69NO12 |
|
| 丙亚胺 | razoxane | 21416-67-1 | C11H16N4O4 |
|
| N-(3-甲基苯基)-4-(4-吡啶)-2-噻唑胺 | N-(3-methylphenyl)-4-(4-pyridinyl)-1,3-thiazol-2-amine | 315702-99-9 | C15H13N3S |
|
| FK-506一水合物 | Tacrolimus monohydrate | 109581-93-3 | C44H71NO13 |
|
| 8-表他克莫司 | (3S,4R,5S,8S,9E,12S,14S,15R,16S,18R,19R,26aS)-5,19-dihydroxy-14,16-dimethoxy-15,19-epoxy-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-8-(2-propen-1-yl)-4,10,12,18-tetramethyl-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | (3S,4R,5R,8R,9Z,12R,14S,15R,16S,18R,19R,26aS)-8-allyl-5,19-dihydroxy-3-{(E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylvinyl}-14,16-dimethoxy-4,10,12,18-tetramethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3H-15,19-epoxypyrido[2,1-c][1,4]oxazacyclotricosine-1,7,20,21(4H,23H)-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | Antibiotic S 7481F1 | 59865-13-3 | C62H111N11O12 |
|
| —— | (1R,9S,12S,13R,14R,17R,18Z,21R,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-12-[1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | 30-ethyl-33-[(E,1S,2S)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone | 59865-13-3 | C62H111N11O12 |
|
| —— | FK-506 (Tacrolimus) | 104987-11-3 | C44H69NO12 |
|
| —— | S-Neoral | 59865-13-3 | C62H111N11O12 |
|
| —— | (1R,9S,12S,13R,14S,17R,18Z,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | (3R,6R,9R,15R,18R,21R,24R,30R)-30-ethyl-33-[(E,2S)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone | 59865-13-3 | C62H111N11O12 |
|
| —— | cyclo[Abu-Sar-D-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 59865-13-3 | C62H111N11O12 |
|
| —— | (1R,9S,12S,13R,14S,17R,18E,21S,23S,24S,25S,27R)-12-[(E)-1-[(1R,3R,4R)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-D-N(Me)Leu-D-N(Me)Val-D-N(Me)Bmt(E)] | 59865-13-3 | C62H111N11O12 |
|
| —— | cyclo[DL-Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 59865-13-3 | C62H111N11O12 |
|
| —— | (1R,12S,13R,14S,17S,18E,21R,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-DL-N(Me)Val-N(Me)Bmt(E)] | 59865-13-3 | C62H111N11O12 |
|
| —— | (1R)-1,14-dihydroxy-12-[1-(4-hydroxy-3-methoxycyclohexyl)prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | (1R,9S,12S,13S,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | (18E)-12-[(E)-1-(4-chloro-3-methoxycyclohexyl)prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | cyclosporin A | 59865-13-3 | C62H111N11O12 |
|
| —— | Cyclosporine A | 59865-13-3 | C62H111N11O12 |
|
| —— | (3S,6R,9R,12R,15R,18S,24S,30S,33R)-30-ethyl-33-[(E,1S)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone | 59865-13-3 | C62H111N11O12 |
|
| —— | (1R,9S,12S,13S,14S,17R,18Z,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | tacrolimus | 104987-11-3 | C44H69NO12 |
|
| —— | (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | Ambap5429 | 104987-11-3 | C44H69NO12 |
|
| —— | (1R,9S,12S,13S,14S,17R,21S,23S,24R,25S,27R)-12-[1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
| —— | (1S,9R,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | (1R,9S,14S,18E,21S,23S,24R)-1,14-dihydroxy-12-[(E)-1-[(3R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 104987-11-3 | C44H69NO12 |
|
| —— | FK506 | 104987-11-3 | C44H69NO12 |
|
| —— | acide mycophenolique | 483-60-3 | C17H20O6 |
|
| —— | cyclosporin A | 59865-13-3 | C62H111N11O12 |
|
| —— | cyclosporine A | 59865-13-3 | C62H111N11O12 |
|
| —— | 2-cyano-3-(3,4-dihydroxyphenyl)-N-(2-phenylethyl)prop-2-enamide | 134036-52-5 | C18H16N2O3 |
|
| —— | Restasis | 59865-13-3 | C62H111N11O12 |
|
| —— | 12-[1-(4-Chloro-3-methoxycyclohexyl)prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | 137071-32-0 | C43H68ClNO11 |
|
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