| Entry |
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|---|---|---|---|---|---|---|---|
| Name | Istradefylline (JAN/USAN/INN); Nourianz (TN); Nouriast (TN) | ||||||
| Product | NOURIANZ (Kyowa Kirin) | ||||||
| Formula | C20H24N4O4 | ||||||
| Exact mass | 384.1798 | ||||||
| Mol weight | 384.429 | ||||||
| Structure |  | ||||||
| Class | Neuropsychiatric agent DG01967 Antiparkinson agent DG01613 Xantine-type antiparkinsonian agent Metabolizing enzyme substrate DG01891 CYP1A1 substrate DG01633 CYP3A/CYP3A4 substrate DG02913 CYP3A4 substrate DG02925 CYP3A5 substrate Metabolizing enzyme inhibitor DG02852 CYP3A/CYP3A4 inhibitor DG01522 CYP3A4 inhibitor DG01915 CYP3A5 inhibitor Transporter inhibitor DG01622 ABCB1 inhibitor | ||||||
| Remark |
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| Efficacy | Antiparkinsonian, Adenosine A2A receptor antagonist | ||||||
| Disease | Parkinson's disease [DS:H00057] | ||||||
| Comment | Treatment of the symptoms of Parkinson's disease | ||||||
| Target | ADORA2A [HSA:135] [KO:K04266] | ||||||
| Pathway |
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| Metabolism | Enzyme: CYP1A1 [HSA:1543], CYP3A4 [HSA:1576], CYP3A5 [HSA:1577] | ||||||
| Interaction | CYP inhibition: CYP3A4 [HSA:1576], CYP3A5 [HSA:1577] Transporter inhibition: ABCB1 [HSA:5243] | ||||||
| Structure map |
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| Brite | Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] N NERVOUS SYSTEM N04 ANTI-PARKINSON DRUGS N04C OTHER ANTIPARKINSON DRUGS N04CX Other antiparkinson drugs N04CX01 Istradefylline D04641 Istradefylline (JAN/USAN/INN) <JP/US> USP drug classification [BR:br08302] Antiparkinson Agents Antiparkinson Agents, Other Istradefylline D04641 Istradefylline (JAN/USAN/INN) Therapeutic category of drugs in Japan [BR:br08301] 1 Agents affecting nervous system and sensory organs 11 Agents affecting central nervous system 116 Antiparkinsonian agents 1169 Others D04641 Istradefylline (JAN/USAN/INN) Drug groups [BR:br08330] Neuropsychiatric agent DG01967 Antiparkinson agent DG01613 Xantine-type antiparkinsonian agent D04641 Istradefylline Metabolizing enzyme substrate DG01891 CYP1A1 substrate D04641 Istradefylline DG01633 CYP3A/CYP3A4 substrate DG02913 CYP3A4 substrate D04641 Istradefylline DG02925 CYP3A5 substrate D04641 Istradefylline Metabolizing enzyme inhibitor DG02852 CYP3A/CYP3A4 inhibitor DG01522 CYP3A4 inhibitor D04641 Istradefylline DG01915 CYP3A5 inhibitor D04641 Istradefylline Transporter inhibitor DG01622 ABCB1 inhibitor D04641 Istradefylline Drug classes [BR:br08332] Neuropsychiatric agent DG01967 Antiparkinson agent D04641 Istradefylline Target-based classification of drugs [BR:br08310] G Protein-coupled receptors Rhodopsin family Adenosine ADORA2A D04641 Istradefylline (JAN/USAN/INN) <JP/US> New drug approvals in the USA [br08319.html] New molecular entities and new therapeutic biological products D04641 New drug approvals in Japan [br08318.html] Drugs with new active ingredients D04641 New drug approvals in the USA, Europe and Japan [br08328.html] Approval dates by FDA, EMA and PMDA D04641 Drug metabolizing enzymes and transporters [br08309.html] Drug metabolizing enzymes D04641 Drug transporters D04641 | ||||||
| Other DBs |
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| KCF data | ATOM 28 1 N4y N 14.8400 -16.6600 2 C8y C 14.8400 -18.0600 3 N4y N 13.6500 -18.7600 4 C8y C 12.3900 -18.0600 5 C8y C 12.3900 -16.6600 6 C8y C 13.6500 -15.9600 7 O5x O 13.6500 -14.5600 8 N4y N 11.0585 -16.2274 9 C8y C 10.2356 -17.3600 10 N5x N 11.0585 -18.4926 11 C1a C 10.6297 -14.9078 12 O5x O 16.0553 -18.7551 13 C1b C 13.6672 -20.1599 14 C1a C 14.8751 -20.8376 15 C1b C 16.0553 -15.9649 16 C1a C 17.2437 -16.6577 17 C2b C 8.8200 -17.3600 18 C2b C 8.1200 -16.1476 19 C8y C 6.7202 -16.1476 20 C8x C 6.0297 -14.9520 21 C8x C 4.6297 -14.9522 22 C8y C 3.9299 -16.1647 23 C8y C 4.6203 -17.3602 24 C8x C 6.0203 -17.3601 25 O2a O 2.5200 -16.1648 26 O2a O 3.9205 -18.5727 27 C1a C 2.5202 -18.5729 28 C1a C 1.8179 -17.3812 BOND 30 1 1 2 1 2 2 3 1 3 3 4 1 4 4 5 2 5 5 6 1 6 1 6 1 7 6 7 2 8 5 8 1 9 8 9 1 10 9 10 2 11 4 10 1 12 8 11 1 13 2 12 2 14 3 13 1 15 13 14 1 16 1 15 1 17 15 16 1 18 9 17 1 19 17 18 2 20 18 19 1 21 19 20 2 22 20 21 1 23 21 22 2 24 22 23 1 25 23 24 2 26 19 24 1 27 22 25 1 28 23 26 1 29 26 27 1 30 25 28 1 |