| Entry |
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| Name | Everolimus (JAN/USAN/INN); Afinitor (TN); Votubia (TN); Zortress (TN) | ||||||||
| Product | AFINITOR (Novartis Pharmaceuticals Corporation), ZORTRESS (Novartis Pharmaceuticals Corporation) | ||||||||
| Generic | EVEROLIMUS (Ascend Laboratories), EVEROLIMUS (Biocon Pharma), EVEROLIMUS (Breckenridge Pharmaceutical), EVEROLIMUS (Hikma Pharmaceuticals USA), EVEROLIMUS (Hikma Pharmaceuticals USA), EVEROLIMUS (Mylan Pharmaceuticals), EVEROLIMUS (Mylan Pharmaceuticals), EVEROLIMUS (Par Pharmaceutical), EVEROLIMUS (Teva Pharmaceuticals USA), EVEROLIMUS (Breckenridge Pharmaceutical) | ||||||||
| Formula | C53H83NO14 | ||||||||
| Exact mass | 957.5814 | ||||||||
| Mol weight | 958.2244 | ||||||||
| Structure |  | ||||||||
| Simcomp | |||||||||
| Class | Antineoplastic DG01597 mTOR inhibitor Metabolizing enzyme substrate DG01633 CYP3A/CYP3A4 substrate DG02913 CYP3A4 substrate Transporter substrate DG01665 ABCB1 substrate | ||||||||
| Remark |
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| Efficacy | Antineoplastic, Immunosuppressant, mTOR inhibitor | ||||||||
| Disease | Breast cancer (HR positive, HER2 negative) [DS:H00031] Pancreatic neuroendocrine tumor [DS:H00045] Renal cell carcinoma [DS:H00021] Tuberous sclerosis complex-associated renal angiomyolipoma [DS:H01691] Tuberous sclerosis complex-associated subependymal giant cell astrocytoma [DS:H01692] Organ rejection in kidney transplantation [DS:H00083] Organ rejection in liver transplantation [DS:H00083] | ||||||||
| Comment | Rapamycin derivative | ||||||||
| Target | MTOR [HSA:2475] [KO:K07203] | ||||||||
| Pathway |
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| Metabolism | Enzyme: CYP3A4 [HSA:1576] Transporter: ABCB1 [HSA:5243] | ||||||||
| Interaction | |||||||||
| Structure map |
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| Brite | Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01E PROTEIN KINASE INHIBITORS L01EG Mammalian target of rapamycin (mTOR) kinase inhibitors L01EG02 Everolimus D02714 Everolimus (JAN/USAN/INN) <JP/US> L04 IMMUNOSUPPRESSANTS L04A IMMUNOSUPPRESSANTS L04AA Selective immunosuppressants L04AA18 Everolimus D02714 Everolimus (JAN/USAN/INN) <JP/US> USP drug classification [BR:br08302] Antineoplastics Molecular Target Inhibitors Everolimus D02714 Everolimus (JAN/USAN/INN) Immunological Agents Immunosuppressants mTOR Inhibitors Everolimus D02714 Everolimus (JAN/USAN/INN) Therapeutic category of drugs in Japan [BR:br08301] 3 Agents affecting metabolism 39 Other agents affecting metabolism 399 Miscellaneous 3999 Others D02714 Everolimus (JAN/USAN/INN) 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D02714 Everolimus (JAN/USAN/INN) Drug groups [BR:br08330] Antineoplastic DG01597 mTOR inhibitor D02714 Everolimus Metabolizing enzyme substrate DG01633 CYP3A/CYP3A4 substrate DG02913 CYP3A4 substrate D02714 Everolimus Transporter substrate DG01665 ABCB1 substrate D02714 Everolimus Drug classes [BR:br08332] Antineoplastic DG01597 mTOR inhibitor D02714 Everolimus Target-based classification of drugs [BR:br08310] Protein kinases Serine/threonine kinases Other MTOR D02714 Everolimus (JAN/USAN/INN) <JP/US> New drug approvals in the USA [br08319.html] New molecular entities and new therapeutic biological products D02714 New drug approvals in Europe [br08329.html] European public assessment reports (EPAR) authorised medicine D02714 New drug approvals in Japan [br08318.html] Drugs with new active ingredients D02714 New drug approvals in the USA, Europe and Japan [br08328.html] Approval dates by FDA, EMA and PMDA D02714 Drug metabolizing enzymes and transporters [br08309.html] Drug metabolizing enzymes D02714 Drug transporters D02714 Pharmacogenomic biomarkers [br08341.html] Somatic variations in targeted cancer therapies D02714 | ||||||||
| Other DBs |
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| KCF data | ATOM 68 1 N1y N 28.0564 -21.8335 2 C1y C 29.2458 -21.1339 3 C5a C 28.0564 -23.2326 4 C1x C 26.7971 -21.1339 5 C7a C 30.4350 -21.8335 6 C1x C 29.2458 -19.7348 7 C5a C 26.7971 -23.9323 8 O5a O 29.2458 -23.9323 9 C1x C 26.7971 -19.7348 10 O7a O 31.6243 -21.1339 11 O6a O 30.4350 -22.9530 12 C1x C 28.0564 -18.9652 13 C1z C 26.7971 -25.3315 14 O5a O 25.6079 -23.1628 15 C1c C 32.8836 -21.8335 16 O2x O 27.9864 -26.0311 17 C1y C 25.5378 -26.0311 18 O1a O 26.7971 -26.7307 19 C1c C 34.0729 -21.1339 20 C1b C 32.8836 -23.2326 21 C1y C 27.9864 -27.4303 22 C1x C 25.5378 -27.3603 23 C1a C 24.3486 -25.2615 24 C1b C 35.3321 -21.8335 25 C1a C 34.0729 -19.7348 26 C5a C 34.0729 -23.9323 27 C1b C 29.1758 -28.1299 28 C1x C 26.7971 -28.1299 29 C1y C 36.5215 -21.1339 30 C1c C 34.0729 -25.3315 31 O5a O 35.3321 -23.1628 32 C1c C 29.1758 -29.5291 33 C1x C 37.7108 -21.8335 34 C1x C 36.5215 -19.7348 35 C2b C 35.3321 -26.0311 36 C1a C 32.8836 -26.0311 37 C2c C 30.3650 -30.2287 38 O2a O 27.9864 -30.2287 39 C1y C 38.9001 -21.1339 40 C1x C 37.7108 -19.0352 41 C2c C 35.3321 -27.3603 42 C2b C 30.3650 -31.6279 43 C1a C 31.6243 -29.5291 44 C1a C 27.9864 -31.6279 45 C1y C 38.9001 -19.7348 46 O2a O 40.1594 -21.8335 47 C1c C 36.5215 -28.0599 48 C1a C 34.0729 -28.0599 49 C2b C 31.5544 -32.3275 50 O2a O 40.1594 -18.9652 51 C1c C 36.5215 -29.4591 52 O1a O 37.7108 -27.3603 53 C2b C 31.5544 -33.7266 54 C5a C 37.7108 -30.1587 55 O2a O 35.2623 -30.1587 56 C2b C 32.8137 -34.4262 57 C1c C 37.7108 -31.5579 58 O5a O 38.9001 -29.4591 59 C1a C 35.2623 -31.5579 60 C2b C 34.0029 -33.7266 61 C1b C 36.5215 -32.2575 62 C1a C 38.9001 -32.2575 63 C1c C 35.4021 -33.7266 64 C1a C 35.7519 -35.0559 65 C1b C 41.4068 -19.6446 66 C1b C 42.6136 -18.9066 67 O1a O 43.8531 -19.5813 68 C1a C 40.1594 -23.2335 BOND 71 1 1 2 1 2 1 3 1 3 1 4 1 4 2 5 1 #Up 5 2 6 1 6 3 7 1 7 3 8 2 8 4 9 1 9 5 10 1 10 5 11 2 11 6 12 1 12 7 13 1 13 7 14 2 14 10 15 1 15 13 16 1 #Down 16 13 17 1 17 13 18 1 #Up 18 15 19 1 19 15 20 1 20 21 16 1 #Down 21 17 22 1 22 17 23 1 #Up 23 19 24 1 24 19 25 1 #Down 25 20 26 1 26 21 27 1 27 21 28 1 28 24 29 1 29 26 30 1 30 26 31 2 31 27 32 1 32 29 33 1 33 29 34 1 34 30 35 1 35 30 36 1 #Up 36 32 37 1 37 32 38 1 #Up 38 33 39 1 39 34 40 1 40 35 41 2 41 37 42 2 42 37 43 1 43 38 44 1 44 39 45 1 45 39 46 1 #Down 46 41 47 1 47 41 48 1 48 42 49 1 49 45 50 1 #Up 50 47 51 1 51 47 52 1 #Up 52 49 53 2 53 51 54 1 54 51 55 1 #Down 55 53 56 1 56 54 57 1 57 54 58 2 58 55 59 1 59 56 60 2 60 57 61 1 61 57 62 1 #Down 62 60 63 1 63 63 64 1 #Down 64 9 12 1 65 22 28 1 66 40 45 1 67 61 63 1 68 50 65 1 69 65 66 1 70 66 67 1 71 46 68 1 |