抗代謝藥是一類與正常代謝物或輔酶結構相似的化合物,主要通過與合成正常代謝物所必需的酶結合,從而干擾核酸的合成,抑制腫瘤細胞的生長和增殖。某些抗代謝物還具有反饋抑制作用,能夠阻斷代謝物前體的合成。常見的抗代謝藥包括抗葉酸、抗嘌呤及抗嘧啶等,它們主要作用于細胞周期的S期,屬于典型的細胞周期特異性藥物。
由于腫瘤組織與正常組織在代謝過程上的差異不大,因此這類藥物的選擇性較差,對諸如骨髓、胃腸道黏膜、生殖系統和毛發等增殖較快的正常組織也具有一定的毒性。盡管多數抗代謝藥主要抑制細胞DNA合成,但由于它們的作用點不同,各藥物之間通常不會產生交叉耐藥性。
| 中文名稱 | 英文名稱 | CAS號 | 化學式 |
|---|---|---|---|
| 雷替曲塞 | N-[5-[N-[(3,4-dihydro-2-methyl-4-oxy-6-quinazolinyl)-methyl]-N-methylamino]-2-thenoyl]-L-glutamic acid | 112887-68-0 | C21H22N4O6S |
| 阿糖胞苷 | arabinosyl cytosine | 147-94-4 | C9H13N3O5 |
| 阿扎胞苷雜質20 | α-L-cytosine arabinoside | 65-46-3 | C9H13N3O5 |
| 阿扎胞苷雜質20 | 1-β-L-arabinofuranosyl cytosine | 65-46-3 | C9H13N3O5 |
| 重酒石酸長春瑞濱 | vinorelbine ditartrate | 125317-39-7 | 2C4H6O6*C45H54N4O8 |
| 脫氧助間型霉素 | 2'-deoxycoformycin | 53910-25-1 | C11H16N4O4 |
| 肌苷二醛 | inosinedialdehyde | 23590-99-0 | C10H10N4O5 |
| 米替福星 | hexadecylphosphocholine | 58066-85-6 | C21H46NO4P |
| 磷酸氟達拉濱 | fludarabine phosphate | 75607-67-9 | C10H13FN5O7P |
| 鹽酸阿糖胞苷 | cytarabine hydrochloride | 69-74-9 | C9H13N3O5*ClH |
| 鹽酸環胞苷 | ancitabine hydrochloride | 10212-25-6 | C9H11N3O4*ClH |
| 鹽酸吉西他濱 | gemcitabine hydrochloride | 122111-03-9 | C9H11F2N3O4*ClH |
| 甲氨蝶呤 | Methotrexate | 59-05-2 | C20H22N8O5 |
| 甲異靛 | Meisoindigo | 97207-47-1 | C17H12N2O2 |
| 氨基蝶呤 | aminopterin | 54-62-6 | C19H20N8O5 |
| 氟達拉濱 | Fludarabine | 21679-14-1 | C10H12FN5O4 |
| 替莫唑胺 | temozolomide | 85622-93-1 | C6H6N6O2 |
| 替加氟 | (R)-5-fluoro-1-(tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione | 37076-68-9 | C8H9FN2O3 |
| 替加氟 | tegafur | 17902-23-7 | C8H9FN2O3 |
| 安西他濱 | cyclocitidine | 31698-14-3 | C9H11N3O4 |
| 安啶 | 4'-(9-acridinylamino) methanesulfon-m-anisidine | 51264-14-3 | C21H19N3O3S |
| 奈拉濱 | nelarabine | 121032-29-9 | C11H15N5O5 |
| 吉西他濱 | Gemcitabine | 95058-81-4 | C9H11F2N3O4 |
| 去氧氟尿苷 | doxifluridine | 3094-09-5 | C9H11FN2O5 |
| 卡莫氟 | carmofur | 61422-45-5 | C11H16FN3O3 |
| 克羅拉濱 | clofarabine | 123318-82-1 | C10H11ClFN5O3 |
| 伊沙匹隆 | ixabepilone | 219989-84-1 | C27H42N2O5S |
| 乙嘧替氟 | 3-<3-(6-benzoyloxy-3-cyano-2-pyridyloxycarbonyl)benzoyl>-1-ethoxymethyl-5-fluorouracil | 110690-43-2 | C28H19FN4O8 |
| 6-硫鳥嘌呤 | thioguanin | 154-42-7 | C5H5N5S |
| 5-氟脫氧尿苷雜質 | 2'-deoxy-5-fluorouridine 5'-phosphate | 50-91-9 | C9H11FN2O5 |
| 5-氟-4-羥基嘧啶 | 5-fluoro-3H-pyrimidin-4-one | 671-35-2 | C4H3FN2O |
| 5-氟-2'-脫氧脲核苷 | 5-Fluoro-2'-deoxyuridine | 50-91-9 | C9H11FN2O5 |
| 2-(2-氨基-6-甲氧基嘌呤-9-基)-5-(羥基甲基)四氫呋喃-3,4-二醇 | <i>O</i><sup>6</sup>-methyl-guanosine | 7803-88-5 | C11H15N5O5 |
| —— | Diglycolaldehyde, .α.-(hydroxymethyl)-.α.'-(6-hydroxy-9H-purin-9-yl)- | 6614-62-6 | C10H10N4O5 |
| —— | (1S,3S,7R,10S,11S,12S,16R)-7,11-Dihydroxy-8,8,10,12,16-pentamethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione | 219989-84-1 | C27H42N2O5S |
| —— | 2,3-dihydroxybutanedioic acid;methyl 11-acetyloxy-12-ethyl-4-(16-ethyl-12-methoxycarbonyl-1,10-diazatetracyclo[12.3.1.03,11.04,9]octadeca-3(11),4,6,8,15-pentaen-12-yl)-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate | 125317-39-7 | C53H66N4O20 |
| —— | (3S,4S,5R)-2-(2-amino-6-methoxypurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol | 121032-29-9 | C11H15N5O5 |
| —— | CO-Vidarabine | 53910-25-1 | C11H16N4O4 |
| —— | (8R)-3-[(4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7,8-dihydro-4H-imidazo[4,5-d][1,3]diazepin-8-ol | 53910-25-1 | C11H16N4O4 |
| —— | N-[4-(9-acridinylmethyl)-3-methoxyphenyl]methanesulfonamide | 51264-14-3 | C22H20N2O3S |
| —— | 1-[(4S,5R)-3,4-dihydroxy-5-methyl-2-oxolanyl]-5-fluoropyrimidine-2,4-dione | 3094-09-5 | C9H11FN2O5 |
| —— | vinorelbine L-tartrate | 125317-39-7 | C53H66N4O20 |
| —— | 5-DFUR (Doxifluridine) 98% | 3094-09-5 | C9H11FN2O5 |
| —— | 1-[(2R,4R,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoropyrimidine-2,4-dione | 3094-09-5 | C9H11FN2O5 |
| —— | vinorelbine D-tartrate | 125317-39-7 | C53H66N4O20 |
| —— | 5'-dFUrd | 3094-09-5 | C9H11FN2O5 |
| —— | (2R,3R)-2,3-dihydroxybutanedioic acid;methyl (1R,10S,11R,12R,19R)-11-acetyloxy-12-ethyl-4-[(12S,14R)-16-ethyl-12-methoxycarbonyl-1,10-diazatetracyclo[12.3.1.03,11.04,9]octadeca-3(11),4,6,8,15-pentaen-12-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate | 125317-39-7 | C53H66N4O20 |
| —— | 1-[(3S,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoropyrimidine-2,4-dione | 3094-09-5 | C9H11FN2O5 |
| —— | Vinorelbine Tartrate | 125317-39-7 | C53H66N4O20 |
| —— | 1-[(2S,3S,4R,5S)-3,4-Dihydroxy-5-methyltetrahydrofuran-2-YL]-5-fluoropyrimidine-2,4(1H,3H)-dione | 3094-09-5 | C9H11FN2O5 |