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| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4151 | 160970-54-7 |
| Dose | Unit | Route |
|---|---|---|
| 8 | mg | O |
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.23 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 32 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| CL (Clearance) | 2.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.05 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.60 hours | Lombardo F, Berellini G, Obach RS |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| CL (Clearance) | 2.38 mL/min/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| Vd (Volume of distribution) | 0.71 L/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT3,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,TEK | 27 | |||
| kinase-selectivity-class | AXL | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 8, 2008 | FDA | ACTAVIS LABS UT INC | |
| Jan. 29, 2010 | EMA |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Haematoma | 51.81 | 51.58 | 14 | 291 | 39034 | 90589108 |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Urinary retention | 147.91 | 13.68 | 123 | 15489 | 42091 | 42563632 |
| Reversible airways obstruction | 132.48 | 13.68 | 33 | 15579 | 570 | 42605153 |
| Interstitial lung disease | 77.66 | 13.68 | 118 | 15494 | 78344 | 42527379 |
| Retrograde ejaculation | 54.64 | 13.68 | 16 | 15596 | 519 | 42605204 |
| Granulomatous rosacea | 51.56 | 13.68 | 12 | 15600 | 153 | 42605570 |
| Cerebral infarction | 51.05 | 13.68 | 60 | 15552 | 31109 | 42574614 |
| Mucosal dryness | 50.28 | 13.68 | 20 | 15592 | 1658 | 42604065 |
| Acute kidney injury | 48.35 | 13.68 | 263 | 15349 | 367074 | 42238649 |
| Orthostatic hypotension | 47.02 | 13.68 | 57 | 15555 | 30513 | 42575210 |
| Haematocrit increased | 45.18 | 13.68 | 21 | 15591 | 2546 | 42603177 |
| Ejaculation failure | 43.60 | 13.68 | 15 | 15597 | 826 | 42604897 |
| Left atrial dilatation | 43.37 | 13.68 | 20 | 15592 | 2382 | 42603341 |
| Hyponatraemia | 41.37 | 13.68 | 105 | 15507 | 101357 | 42504366 |
| Inappropriate antidiuretic hormone secretion | 39.71 | 13.68 | 39 | 15573 | 16502 | 42589221 |
| Erectile dysfunction | 37.58 | 13.68 | 46 | 15566 | 24867 | 42580856 |
| Toxicity to various agents | 36.84 | 13.68 | 19 | 15593 | 229117 | 42376606 |
| Presyncope | 36.49 | 13.68 | 43 | 15569 | 22344 | 42583379 |
| Haematuria | 36.16 | 13.68 | 71 | 15541 | 57728 | 42547995 |
| Fall | 35.68 | 13.68 | 175 | 15437 | 234345 | 42371378 |
| Sopor | 35.24 | 13.68 | 33 | 15579 | 13169 | 42592554 |
| Pemphigoid | 35.19 | 13.68 | 31 | 15581 | 11436 | 42594287 |
| Cerebellar ischaemia | 32.12 | 13.68 | 8 | 15604 | 138 | 42605585 |
| Haemoglobin increased | 31.30 | 13.68 | 21 | 15591 | 5185 | 42600538 |
| Histamine level increased | 30.86 | 13.68 | 7 | 15605 | 79 | 42605644 |
| Pneumonia aspiration | 30.70 | 13.68 | 61 | 15551 | 50017 | 42555706 |
| Bradycardia | 30.29 | 13.68 | 84 | 15528 | 85400 | 42520323 |
| Hypoparathyroidism | 30.23 | 13.68 | 11 | 15601 | 714 | 42605009 |
| Face oedema | 28.74 | 13.68 | 30 | 15582 | 13636 | 42592087 |
| Acute lung injury | 27.97 | 13.68 | 13 | 15599 | 1576 | 42604147 |
| Cerebral haematoma | 27.58 | 13.68 | 20 | 15592 | 5590 | 42600133 |
| Subdural haematoma | 27.52 | 13.68 | 38 | 15574 | 23100 | 42582623 |
| Decreased appetite | 27.15 | 13.68 | 141 | 15471 | 192996 | 42412727 |
| Anaemia | 25.65 | 13.68 | 183 | 15429 | 280095 | 42325628 |
| Hepatitis cholestatic | 25.15 | 13.68 | 24 | 15588 | 9800 | 42595923 |
| Completed suicide | 24.97 | 13.68 | 3 | 15609 | 96462 | 42509261 |
| Tongue oedema | 23.95 | 13.68 | 15 | 15597 | 3295 | 42602428 |
| Hepatic function abnormal | 23.79 | 13.68 | 56 | 15556 | 51511 | 42554212 |
| Hypokalaemia | 22.05 | 13.68 | 67 | 15545 | 71654 | 42534069 |
| Syncope | 21.87 | 13.68 | 83 | 15529 | 99323 | 42506400 |
| Vocal cord paralysis | 21.74 | 13.68 | 10 | 15602 | 1184 | 42604539 |
| Linear IgA disease | 21.73 | 13.68 | 12 | 15600 | 2091 | 42603632 |
| Dysuria | 21.66 | 13.68 | 40 | 15572 | 31056 | 42574667 |
| Tryptase increased | 21.54 | 13.68 | 7 | 15605 | 323 | 42605400 |
| Arrhythmia | 21.06 | 13.68 | 46 | 15566 | 40271 | 42565452 |
| Generalised oedema | 21.02 | 13.68 | 27 | 15585 | 15309 | 42590414 |
| Neutrophil percentage decreased | 20.90 | 13.68 | 7 | 15605 | 355 | 42605368 |
| Neuropathy vitamin B6 deficiency | 20.74 | 13.68 | 3 | 15609 | 0 | 42605723 |
| Lactic acidosis | 20.71 | 13.68 | 49 | 15563 | 45212 | 42560511 |
| Drug ineffective | 20.10 | 13.68 | 142 | 15470 | 630055 | 41975668 |
| Urinary tract infection | 19.50 | 13.68 | 80 | 15532 | 99204 | 42506519 |
| Band neutrophil percentage increased | 19.28 | 13.68 | 5 | 15607 | 102 | 42605621 |
| Angle closure glaucoma | 19.19 | 13.68 | 9 | 15603 | 1113 | 42604610 |
| Rash vesicular | 19.05 | 13.68 | 13 | 15599 | 3300 | 42602423 |
| Atrioventricular block complete | 18.80 | 13.68 | 22 | 15590 | 11342 | 42594381 |
| Hypoproteinaemia | 18.50 | 13.68 | 12 | 15600 | 2800 | 42602923 |
| Blood triglycerides decreased | 18.43 | 13.68 | 5 | 15607 | 122 | 42605601 |
| Confusional state | 18.04 | 13.68 | 114 | 15498 | 167483 | 42438240 |
| Cardiac failure | 17.84 | 13.68 | 82 | 15530 | 106774 | 42498949 |
| Pyelonephritis | 17.78 | 13.68 | 18 | 15594 | 7896 | 42597827 |
| Eosinophil percentage increased | 17.48 | 13.68 | 7 | 15605 | 590 | 42605133 |
| Altered state of consciousness | 17.16 | 13.68 | 35 | 15577 | 29224 | 42576499 |
| Hypovolaemia | 16.98 | 13.68 | 21 | 15591 | 11464 | 42594259 |
| Cystitis interstitial | 16.85 | 13.68 | 5 | 15607 | 170 | 42605553 |
| Mucocutaneous disorder | 16.66 | 13.68 | 5 | 15607 | 177 | 42605546 |
| Lymphopenia | 16.63 | 13.68 | 29 | 15583 | 21534 | 42584189 |
| Rash maculo-papular | 16.51 | 13.68 | 40 | 15572 | 37463 | 42568260 |
| Faecal vomiting | 16.48 | 13.68 | 7 | 15605 | 685 | 42605038 |
| Drug hypersensitivity | 16.31 | 13.68 | 8 | 15604 | 99381 | 42506342 |
| Hypoparathyroidism secondary | 16.09 | 13.68 | 5 | 15607 | 199 | 42605524 |
| Skin disorder | 16.05 | 13.68 | 25 | 15587 | 16919 | 42588804 |
| Hepatocellular injury | 15.92 | 13.68 | 30 | 15582 | 23648 | 42582075 |
| Acquired haemophilia | 15.79 | 13.68 | 9 | 15603 | 1666 | 42604057 |
| Psychological trauma | 15.44 | 13.68 | 5 | 15607 | 228 | 42605495 |
| Tricuspid valve disease | 15.38 | 13.68 | 5 | 15607 | 231 | 42605492 |
| Pain | 15.15 | 13.68 | 43 | 15569 | 244805 | 42360918 |
| Hyperbilirubinaemia | 14.95 | 13.68 | 27 | 15585 | 20608 | 42585115 |
| Band neutrophil count increased | 14.83 | 13.68 | 5 | 15607 | 259 | 42605464 |
| Cranial nerve injury | 14.51 | 13.68 | 3 | 15609 | 21 | 42605702 |
| Adenocarcinoma gastric | 14.40 | 13.68 | 8 | 15604 | 1410 | 42604313 |
| Varicose vein ruptured | 14.40 | 13.68 | 4 | 15608 | 107 | 42605616 |
| Hypocalcaemia | 14.17 | 13.68 | 33 | 15579 | 30140 | 42575583 |
| Subacute cutaneous lupus erythematosus | 14.04 | 13.68 | 8 | 15604 | 1480 | 42604243 |
| Rhabdomyolysis | 13.86 | 13.68 | 61 | 15551 | 77958 | 42527765 |
| Agranulocytosis | 13.85 | 13.68 | 33 | 15579 | 30579 | 42575144 |
| Bladder tamponade | 13.71 | 13.68 | 6 | 15606 | 632 | 42605091 |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Urinary retention | 162.45 | 15.26 | 106 | 14519 | 69577 | 110505097 |
| Reversible airways obstruction | 123.91 | 15.26 | 34 | 14591 | 2465 | 110572209 |
| Acute kidney injury | 114.23 | 15.26 | 256 | 14369 | 635174 | 109939500 |
| Interstitial lung disease | 110.67 | 15.26 | 113 | 14512 | 139221 | 110435453 |
| Hyponatraemia | 71.94 | 15.26 | 114 | 14511 | 217539 | 110357135 |
| Retrograde ejaculation | 69.37 | 15.26 | 15 | 14610 | 396 | 110574278 |
| Cerebral infarction | 68.56 | 15.26 | 56 | 14569 | 51782 | 110522892 |
| Haematuria | 65.28 | 15.26 | 67 | 14558 | 82938 | 110491736 |
| Inappropriate antidiuretic hormone secretion | 61.08 | 15.26 | 44 | 14581 | 33807 | 110540867 |
| Granulomatous rosacea | 59.98 | 15.26 | 12 | 14613 | 214 | 110574460 |
| Left atrial dilatation | 55.47 | 15.26 | 20 | 14605 | 3540 | 110571134 |
| Bradycardia | 53.50 | 15.26 | 83 | 14542 | 155434 | 110419240 |
| Anaemia | 53.18 | 15.26 | 176 | 14449 | 546910 | 110027764 |
| Haematocrit increased | 52.47 | 15.26 | 21 | 14604 | 4938 | 110569736 |
| Mucosal dryness | 51.95 | 15.26 | 20 | 14605 | 4243 | 110570431 |
| Orthostatic hypotension | 51.23 | 15.26 | 53 | 14572 | 66196 | 110508478 |
| Pneumonia aspiration | 48.94 | 15.26 | 57 | 14568 | 81176 | 110493498 |
| Presyncope | 44.99 | 15.26 | 43 | 14582 | 48844 | 110525830 |
| Pemphigoid | 43.50 | 15.26 | 29 | 14596 | 19678 | 110554996 |
| Subdural haematoma | 43.26 | 15.26 | 37 | 14588 | 36417 | 110538257 |
| Drug hypersensitivity | 42.73 | 15.26 | 5 | 14620 | 454085 | 110120589 |
| Haemoglobin increased | 40.16 | 15.26 | 21 | 14604 | 9126 | 110565548 |
| Cardiac failure | 39.75 | 15.26 | 81 | 14544 | 187545 | 110387129 |
| Pain | 39.41 | 15.26 | 41 | 14584 | 954914 | 109619760 |
| Decreased appetite | 35.08 | 15.26 | 140 | 14485 | 475706 | 110098968 |
| Alopecia | 34.35 | 15.26 | 4 | 14621 | 364749 | 110209925 |
| Rhabdomyolysis | 34.26 | 15.26 | 59 | 14566 | 120342 | 110454332 |
| Histamine level increased | 34.13 | 15.26 | 7 | 14618 | 142 | 110574532 |
| Prostatic specific antigen increased | 34.03 | 15.26 | 21 | 14604 | 12490 | 110562184 |
| Fall | 33.45 | 15.26 | 163 | 14462 | 603319 | 109971355 |
| Sopor | 33.35 | 15.26 | 32 | 14593 | 36514 | 110538160 |
| Syncope | 33.33 | 15.26 | 79 | 14546 | 202457 | 110372217 |
| Joint swelling | 32.79 | 15.26 | 9 | 14616 | 442836 | 110131838 |
| Hepatic function abnormal | 32.58 | 15.26 | 49 | 14576 | 89246 | 110485428 |
| Psychological trauma | 32.20 | 15.26 | 11 | 14614 | 1662 | 110573012 |
| Acute lung injury | 32.15 | 15.26 | 13 | 14612 | 3138 | 110571536 |
| Atrial fibrillation | 31.93 | 15.26 | 84 | 14541 | 229558 | 110345116 |
| Benign prostatic hyperplasia | 31.30 | 15.26 | 23 | 14602 | 18211 | 110556463 |
| Cerebral haematoma | 30.95 | 15.26 | 18 | 14607 | 9614 | 110565060 |
| Hypokalaemia | 30.92 | 15.26 | 72 | 14553 | 182376 | 110392298 |
| Face oedema | 29.96 | 15.26 | 29 | 14596 | 33440 | 110541234 |
| Hepatitis cholestatic | 29.80 | 15.26 | 22 | 14603 | 17544 | 110557130 |
| Lactic acidosis | 29.78 | 15.26 | 48 | 14577 | 92763 | 110481911 |
| Arrhythmia | 29.50 | 15.26 | 41 | 14584 | 69534 | 110505140 |
| Hyperkalaemia | 29.20 | 15.26 | 59 | 14566 | 135737 | 110438937 |
| Platelet count decreased | 28.74 | 15.26 | 81 | 14544 | 230362 | 110344312 |
| Erectile dysfunction | 28.72 | 15.26 | 22 | 14603 | 18534 | 110556140 |
| Ejaculation failure | 27.46 | 15.26 | 7 | 14618 | 381 | 110574293 |
| Haematoma | 27.13 | 15.26 | 36 | 14589 | 58440 | 110516234 |
| Hyperbilirubinaemia | 26.38 | 15.26 | 26 | 14599 | 30645 | 110544029 |
| Generalised oedema | 26.35 | 15.26 | 26 | 14599 | 30678 | 110543996 |
| Drug ineffective | 26.25 | 15.26 | 108 | 14517 | 1520432 | 109054242 |
| Rash maculo-papular | 26.04 | 15.26 | 40 | 14585 | 74182 | 110500492 |
| Altered state of consciousness | 26.00 | 15.26 | 35 | 14590 | 57591 | 110517083 |
| Hypotension | 25.17 | 15.26 | 136 | 14489 | 523713 | 110050961 |
| Arthropathy | 25.06 | 15.26 | 4 | 14621 | 287518 | 110287156 |
| Dysuria | 24.80 | 15.26 | 35 | 14590 | 60196 | 110514478 |
| Toxicity to various agents | 24.21 | 15.26 | 17 | 14608 | 480538 | 110094136 |
| Sinusitis | 23.98 | 15.26 | 5 | 14620 | 296683 | 110277991 |
| Neuropathy vitamin B6 deficiency | 23.79 | 15.26 | 3 | 14622 | 0 | 110574674 |
| Hypovolaemia | 23.70 | 15.26 | 21 | 14604 | 21653 | 110553021 |
| Prostate cancer | 23.65 | 15.26 | 27 | 14598 | 37614 | 110537060 |
| Arthralgia | 23.51 | 15.26 | 42 | 14583 | 779590 | 109795084 |
| Hypoglycaemia | 23.25 | 15.26 | 49 | 14576 | 116055 | 110458619 |
| Atrioventricular block complete | 23.05 | 15.26 | 20 | 14605 | 20062 | 110554612 |
| Vocal cord paralysis | 22.65 | 15.26 | 10 | 14615 | 2996 | 110571678 |
| Thrombocytopenia | 22.06 | 15.26 | 98 | 14527 | 348787 | 110225887 |
| Completed suicide | 21.98 | 15.26 | 3 | 14622 | 242378 | 110332296 |
| Linear IgA disease | 21.95 | 15.26 | 11 | 14614 | 4378 | 110570296 |
| Neutrophil count decreased | 21.89 | 15.26 | 49 | 14576 | 120892 | 110453782 |
| Hepatocellular injury | 21.70 | 15.26 | 30 | 14595 | 50612 | 110524062 |
| Hypoparathyroidism | 21.62 | 15.26 | 8 | 14617 | 1522 | 110573152 |
| Duodenal ulcer | 21.52 | 15.26 | 19 | 14606 | 19495 | 110555179 |
| Drug interaction | 21.47 | 15.26 | 126 | 14499 | 500057 | 110074617 |
| Neutrophil percentage decreased | 21.32 | 15.26 | 7 | 14618 | 936 | 110573738 |
| Tryptase increased | 21.32 | 15.26 | 7 | 14618 | 936 | 110573738 |
| Mucocutaneous disorder | 20.74 | 15.26 | 5 | 14620 | 216 | 110574458 |
| Acquired haemophilia | 20.63 | 15.26 | 9 | 14616 | 2622 | 110572052 |
| Lymphopenia | 20.62 | 15.26 | 26 | 14599 | 40144 | 110534530 |
| Rheumatoid arthritis | 20.53 | 15.26 | 7 | 14618 | 299606 | 110275068 |
| Contraindicated product administered | 20.44 | 15.26 | 4 | 14621 | 248263 | 110326411 |
| Blood triglycerides decreased | 20.39 | 15.26 | 5 | 14620 | 232 | 110574442 |
| Tongue oedema | 20.30 | 15.26 | 13 | 14612 | 8243 | 110566431 |
| Pneumonia bacterial | 20.27 | 15.26 | 21 | 14604 | 26240 | 110548434 |
| Agranulocytosis | 19.89 | 15.26 | 32 | 14593 | 61728 | 110512946 |
| Hypoparathyroidism secondary | 19.41 | 15.26 | 5 | 14620 | 284 | 110574390 |
| Pericarditis | 19.20 | 15.26 | 3 | 14622 | 219111 | 110355563 |
| Bladder tamponade | 18.83 | 15.26 | 6 | 14619 | 730 | 110573944 |
| Hypoproteinaemia | 18.81 | 15.26 | 11 | 14614 | 5934 | 110568740 |
| Infusion related reaction | 18.52 | 15.26 | 14 | 14611 | 381148 | 110193526 |
| Nasopharyngitis | 18.51 | 15.26 | 15 | 14610 | 394346 | 110180328 |
| Peripheral swelling | 18.19 | 15.26 | 16 | 14609 | 404018 | 110170656 |
| Angle closure glaucoma | 18.18 | 15.26 | 9 | 14616 | 3490 | 110571184 |
| Impaired quality of life | 17.96 | 15.26 | 21 | 14604 | 29996 | 110544678 |
| Faecal vomiting | 17.85 | 15.26 | 7 | 14618 | 1559 | 110573115 |
| Eosinophil percentage increased | 17.78 | 15.26 | 7 | 14618 | 1575 | 110573099 |
| Hyperuricaemia | 17.75 | 15.26 | 15 | 14610 | 14516 | 110560158 |
| Band neutrophil percentage increased | 17.75 | 15.26 | 5 | 14620 | 399 | 110574275 |
| Cerebellar ischaemia | 17.69 | 15.26 | 5 | 14620 | 404 | 110574270 |
| Melaena | 17.38 | 15.26 | 32 | 14593 | 68725 | 110505949 |
| Acidosis | 17.36 | 15.26 | 18 | 14607 | 22513 | 110552161 |
| Eosinophilia | 17.28 | 15.26 | 29 | 14596 | 57907 | 110516767 |
| Hypocalcaemia | 17.25 | 15.26 | 31 | 14594 | 65335 | 110509339 |
| Nausea | 17.05 | 15.26 | 95 | 14530 | 1235595 | 109339079 |
| Tricuspid valve disease | 16.92 | 15.26 | 5 | 14620 | 473 | 110574201 |
| Renal impairment | 16.81 | 15.26 | 59 | 14566 | 188386 | 110386288 |
| Varicose vein ruptured | 16.73 | 15.26 | 4 | 14621 | 167 | 110574507 |
| Bile duct cancer | 16.57 | 15.26 | 6 | 14619 | 1074 | 110573600 |
| Skin disorder | 16.29 | 15.26 | 24 | 14601 | 42889 | 110531785 |
| Bladder transitional cell carcinoma recurrent | 16.12 | 15.26 | 4 | 14621 | 195 | 110574479 |
| Cerebral haemorrhage | 16.12 | 15.26 | 30 | 14595 | 64938 | 110509736 |
| Drug intolerance | 16.11 | 15.26 | 18 | 14607 | 406494 | 110168180 |
| Lower respiratory tract infection | 16.10 | 15.26 | 6 | 14619 | 243100 | 110331574 |
| Adenocarcinoma gastric | 15.94 | 15.26 | 7 | 14618 | 2072 | 110572602 |
| Systemic lupus erythematosus | 15.67 | 15.26 | 7 | 14618 | 254331 | 110320343 |
| Squamous cell carcinoma of skin | 15.57 | 15.26 | 15 | 14610 | 17188 | 110557486 |
| Cranial nerve injury | 15.54 | 15.26 | 3 | 14622 | 44 | 110574630 |
| Paraneoplastic syndrome | 15.30 | 15.26 | 6 | 14619 | 1336 | 110573338 |
| Subretinal fluid | 15.29 | 15.26 | 6 | 14619 | 1338 | 110573336 |
None
| Source | Code | Description |
|---|---|---|
| ATC | G04CA04 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists |
| FDA MoA | N0000000099 | Adrenergic alpha-Antagonists |
| FDA EPC | N0000175553 | alpha-Adrenergic Blocker |
| MeSH PA | D000317 | Adrenergic alpha-Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D058668 | Adrenergic alpha-1 Receptor Antagonists |
| MeSH PA | D064804 | Urological Agents |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Benign prostatic hyperplasia | indication | 266569009 | |
| Orthostatic hypotension | contraindication | 28651003 | |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Cataract surgery | contraindication | 110473004 | |
| Intraoperative floppy iris syndrome | contraindication | 418801006 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.41 | acidic |
| pKa2 | 7.96 | Basic |
| pKa3 | 4.09 | Basic |
None
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-1A adrenergic receptor | GPCR | ANTAGONIST | Ki | 10.44 | CHEMBL | CHEMBL | |||
| D(2) dopamine receptor | GPCR | Ki | 6 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.17 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.09 | CHEMBL | |||||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.33 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.68 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 6.32 | CHEMBL | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.11 | CHEMBL | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.14 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | Ki | 5.45 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 6.43 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1D | GPCR | Ki | 7.04 | CHEMBL | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.44 | CHEMBL | |||||
| D(4) dopamine receptor | GPCR | Ki | 5.80 | CHEMBL | |||||
| Alpha-1D adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.70 | IUPHAR | ||||
| Alpha-1B adrenergic receptor | GPCR | ANTAGONIST | Ki | 7.70 | IUPHAR | ||||
| Beta-2 adrenergic receptor | GPCR | Ki | 7.48 | CHEMBL | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 9.10 | CHEMBL |
| ID | Source |
|---|---|
| 4028100 | VUID |
| N0000177928 | NUI |
| D01965 | KEGG_DRUG |
| 4028100 | VANDF |
| C1870115 | UMLSCUI |
| CHEBI:135929 | CHEBI |
| CHEMBL24778 | ChEMBL_ID |
| DB06207 | DRUGBANK_ID |
| C095285 | MESH_SUPPLEMENTAL_RECORD_UI |
| 493 | IUPHAR_LIGAND_ID |
| 8043 | INN_ID |
| CUZ39LUY82 | UNII |
| 5312125 | PUBCHEM_CID |
| 720825 | RXNORM |
| 159000 | MMSL |
| 26009 | MMSL |
| 299655 | MMSL |
| d07354 | MMSL |
| 012969 | NDDF |
| 441605002 | SNOMEDCT_US |
| 442042006 | SNOMEDCT_US |
| A1EMV | PDB_CHEM_ID |
| CUZ39LUY82 | INXIGHT DRUGS |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Silodosin | Human Prescription Drug Label | 1 | 27241-144 | CAPSULE | 4 mg | ORAL | ANDA | 25 sections |
| Silodosin | Human Prescription Drug Label | 1 | 27241-145 | CAPSULE | 8 mg | ORAL | ANDA | 25 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-635 | CAPSULE | 4 mg | ORAL | ANDA | 30 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-636 | CAPSULE | 8 mg | ORAL | ANDA | 30 sections |
| Silodosin | Human Prescription Drug Label | 1 | 33342-384 | CAPSULE | 4 mg | ORAL | ANDA | 26 sections |
| Silodosin | Human Prescription Drug Label | 1 | 33342-385 | CAPSULE | 8 mg | ORAL | ANDA | 26 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-777 | CAPSULE | 4 mg | ORAL | ANDA | 25 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-778 | CAPSULE | 8 mg | ORAL | ANDA | 25 sections |
| Silodosin | Human Prescription Drug Label | 1 | 46708-405 | CAPSULE | 4 mg | ORAL | ANDA | 25 sections |
| Silodosin | Human Prescription Drug Label | 1 | 46708-406 | CAPSULE | 8 mg | ORAL | ANDA | 25 sections |
| RAPAFLO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6173 | CAPSULE | 8 mg | ORAL | NDA | 24 sections |
| SILODOSIN | Human Prescription Drug Label | 1 | 59651-095 | CAPSULE | 4 mg | ORAL | ANDA | 26 sections |
| SILODOSIN | Human Prescription Drug Label | 1 | 59651-096 | CAPSULE | 8 mg | ORAL | ANDA | 26 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1420 | CAPSULE | 8 mg | ORAL | ANDA | 25 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1421 | CAPSULE | 4 mg | ORAL | ANDA | 25 sections |
| Silodosin | Human Prescription Drug Label | 1 | 62332-405 | CAPSULE | 4 mg | ORAL | ANDA | 26 sections |
| Silodosin | Human Prescription Drug Label | 1 | 62332-406 | CAPSULE | 8 mg | ORAL | ANDA | 26 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-740 | CAPSULE | 4 mg | ORAL | ANDA | 24 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-740 | CAPSULE | 4 mg | ORAL | ANDA | 24 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-741 | CAPSULE | 8 mg | ORAL | ANDA | 24 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-741 | CAPSULE | 8 mg | ORAL | ANDA | 24 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1420 | CAPSULE | 8 mg | ORAL | ANDA | 25 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1421 | CAPSULE | 4 mg | ORAL | ANDA | 25 sections |
| Silodosin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-3128 | CAPSULE | 8 mg | ORAL | ANDA | 26 sections |
| SILODOSIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2446 | CAPSULE | 4 mg | ORAL | ANDA | 17 sections |
| SILODOSIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2447 | CAPSULE | 8 mg | ORAL | ANDA | 17 sections |
| SILODOSIN | Human Prescription Drug Label | 1 | 72205-009 | CAPSULE | 4 mg | ORAL | ANDA | 26 sections |
| SILODOSIN | Human Prescription Drug Label | 1 | 72205-010 | CAPSULE | 8 mg | ORAL | ANDA | 26 sections |
| SILODOSIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-090 | CAPSULE | 8 mg | ORAL | ANDA | 26 sections |
| SILODOSIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-351 | CAPSULE | 4 mg | ORAL | ANDA | 26 sections |